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ALX-430-096

Revised 24-Feb-05

A77 1726
SYNONYMS	N-(4-Trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide 2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Tyrosine Kinase Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-430-096-M005		5 mg	45.00 USD
ALX-430-096-M025		25 mg	180.00 USD

Product Specification

FORMULA:	C₁₂H₉F₃N₂O₂
MW:	270.2
CAS NUMBER:	108605-62-5
PURITY:	≥98%
APPEARANCE:	White solid.
SOLUBILITY:	Soluble in DMSO.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	Protect from light. Keep under inert gas.

Product Description

Physiologically active metabolite of the immunosuppressive drug leflunomide (Prod. No. ALX-430-095). Inhibits the activity of dihydrorotate dehydrogenase and of protein tyrosine kinases. Blocks TNF-mediated NF-κB activation in a dose- and time-dependent manner. Also inhibits the activity of cyclooxygenase-2 (COX-2) in vitro and in vivo.

Product Specific Literature References

Inhibition of the epidermal growth factor receptor tyrosine kinase activity by leflunomide: T. Mattar, et al.; FEBS Lett. 334, 161 (1993) Abstract
Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide: X. Xu, et al.; J. Biol. Chem. 270, 12398 (1995) Abstract; Full Text
The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase: J.P. Davis, et al.; Biochemistry 35, 1270 (1996) Abstract
Two activities of the immunosuppressive metabolite of leflunomide, A77 1726. Inhibition of pyrimidine nucleotide synthesis and protein tyrosine phosphorylation: X. Xu, et al.; Biochem. Pharmacol. 52, 527 (1996) Abstract
The immunosuppressive metabolite of leflunomide, A77 1726, affects murine T cells through two biochemical mechanisms: R.T. Elder, et al.; J. Immunol. 159, 22 (1997) Abstract
In vivo mechanism by which leflunomide controls lymphoproliferative and autoimmune disease in MRL/MpJ-lpr/lpr mice: X. Xu, et al.; J. Immunol. 159, 167 (1997) Abstract
Immunosuppressive leflunomide metabolite (A77 1726) blocks TNF-dependent nuclear factor-kappa B activation and gene expression: S.K. Manna & B.B. Aggarwal; J. Immunol. 162, 2095 (1999) Abstract
A771726, the active metabolite of leflunomide, directly inhibits the activity of cyclo-oxygenase-2 in vitro and in vivo in a substrate-sensitive manner: L.C. Hamilton, et al.; Br. J. Pharmacol. 127, 1589 (1999) Abstract

Further Categories Containing This Product:

Immunomodulators Other Products • COX Inhibitors • NF-kB Pathway Inhibitors

ALX-440-046

Revised 07-Sep-06

4-Amino-(6R)-5,6,7,8-tetrahydro-L-biopterin . dihydrochloride
SYNONYMS	4-Amino-(6R)-BH₄ . 2HCl
PRODUCT LINE	Nitric Oxide Pathway
PRODUCT CATEGORY	NOS Inhibitors (NOS Induction & Enzyme Activity)

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-440-046-M005		5 mg	370.00 USD

Product Specification

FORMULA:	C₉H₁₆N₆O₂ . 2HCl
MW:	240.3 . 73.0
PURITY:	≥99%
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Stable for several years when stored at -20°C. Sensitive to oxidation, especially in neutral and alkaline solutions. Solutions must be stored at -20°C or colder immediately after preparation. Use oxygen free water with the lowest possible pH. Ascorbic acid, DTT or other antioxidants may be added in order to increase stability.

Product Description

Potent, reversible inhibitor of nitric oxide synthases (NOS) at their pterin-site. Inhibits the formation of nitric oxide (NO) by nNOS (NOS I) with IC₅₀=1.1µM for arginine (Prod. No. ALX-101-004) and IC₅₀=1.3µM for N^G-hydroxy-L-arginine (Prod. No. ALX-106-004). Prolongs allograft survival in vivo and rescues rats from septic shock. Immunosuppressant.

Product Specific Literature References

Tetrahydrobiopterin binding to macrophage inducible nitric oxide synthase: heme spin shift and dimer stabilization by the potent pterin antagonist 4-amino-tetrahydrobiopterin: B. Mayer, et al.; Biochemistry 36, 8422 (1997) Abstract
Allosteric modulation of rat brain nitric oxide synthase by the pterin-site enzyme inhibitor 4-aminotetrahydrobiopterin: S. Pfeiffer, et al.; Biochem. J. 328, 349 (1997) Abstract; Full Text
Preferential inhibition of inducible nitric oxide synthase in intact cells by the 4-amino analogue of tetrahydrobiopterin: K. Schmidt, et al.; Eur. J. Biochem. 259, 25 (1999) Abstract; Full Text
Protection against endotoxemia in rats by a novel tetrahydrobiopterin analogue: S. Bahrami, et al.; Shock 13, 386 (2000) Abstract
Inhibition of endotoxin-induced vascular hyporeactivity by 4-amino-tetrahydrobiopterin: H.D. Gibraeil, et al.; Br. J. Pharmacol. 131, 1757 (2000) Abstract
The 4-amino analogue of tetrahydrobiopterin efficiently prolongs murine cardiac-allograft survival: G. Brandacher, et al.; J. Heart Lung Transplant. 20, 747 (2001) Abstract
A 4-amino analogue of tetrahydrobiopterin attenuates endotoxin-induced hemodynamic alterations and organ injury in rats: F. Fitzal, et al.; Shock 18, 158 (2002) Abstract
Biopterin analogues: novel nitric oxide synthase inhibitors with immunosuppressive action: E.R. Werner and G. Werner-Felmayer; Curr. Drug Metab. 3, 119 (2002), (Review) Abstract
Single-turnover of nitric-oxide synthase in the presence of 4-amino-tetrahydrobiopterin: proposed role for tetrahydrobiopterin as a proton donor: M. Sorlie, et al.; J. Biol. Chem. 278, 48602 (2003) Abstract; Full Text
Ability of tetrahydrobiopterin analogues to support catalysis by inducible nitric oxide synthase: formation of a pterin radical is required for enzyme activity: A.R. Hurshman, et al.; Biochemistry 42, 13287 (2003) Abstract
CO exchange of the oxyferrous complexes of endothelial nitric-oxide synthase oxygenase domain in the presence of 4-amino-tetrahydrobiopterin: S. Marchal, et al.; J. Inorg. Biochem. 98, 1217 (2004) Abstract
Tetrahydropteridines suppress gene expression and induce apoptosis of activated RAW264.7 cells via formation of hydrogen peroxide: G. Thoeni, et al.; Free Radic. Biol. Med. 37, 375 (2004) Abstract
Tetrahydro-4-aminobiopterin attenuates dendritic cell-induced T cell priming independently from inducible nitric oxide synthase: G. Thoeni, et al.; J. Immunol. 174, 7584 (2005) Abstract; Full Text

Further Categories Containing This Product:

Immunomodulators Other Products

ALX-340-049

Revised 03-Dec-07

N-Arachidonoyldopamine
SYNONYMS	N-Arachidonoyl-3-hydroxytyramine NADA AA-DA
PRODUCT LINE	Neurobiology
PRODUCT CATEGORY	Endocannabinoids

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-340-049-M001		1 mg	20.00 USD
ALX-340-049-M005		5 mg	35.00 USD

Product Specification

FORMULA:	C₂₈H₄₁NO₃
MW:	439.6
CAS NUMBER:	199875-69-9
PURITY:	≥99% (HPLC)
APPEARANCE:	Lyophilized.
SOLUBILITY:	Soluble in methanol, 100% ethanol or DMSO.
SHIPPING:	SHIPPED ON DRY ICE
LONG TERM STORAGE:	-20°C
HANDLING:	Packaged under inert gas.

Product Description

Endogenous, specific ligand for the CB₁ receptor (CB₁: K_i=250nM; CB₂: K_i=12µM) [1] and TRPV1 [2] (EC₅₀=50nM) found in nervous tissues [3, 4]. Immunosuppressant inhibiting T cell proliferation and phosphorylation of the NF-κB p65 subunit [5]. Potent vasorelaxant [6] and inhibitor of HIV-1 [7].

Product Specific Literature References

[1] N-acyl-dopamines: novel synthetic CB(1) cannabinoid-receptor ligands and inhibitors of anandamide inactivation with cannabimimetic activity in vitro and in vivo: T. Bisogno, et al.; Biochem. J. 351, 817 (2000) Abstract; Full Text
[2] Actions of two naturally occurring saturated N-acyldopamines on transient receptor potential vanilloid 1 (TRPV1) channels: L. De Petrocellis, et al.; Br. J. Pharmacol. 143, 251 (2004) Abstract; Full Text
[3] An endogenous capsaicin-like substance with high potency at recombinant and native vanilloid VR1 receptors: S.M. Huang, et al.; PNAS 99, 8400 (2002) Abstract
[4] Arachidonyl dopamine as a ligand for the vanilloid receptor VR1 of the rat: A. Toth, et al.; Life Sci. 73, 487 (2003) Abstract
[5] Immunosuppressive activity of endovanilloids: N-arachidonoyl-dopamine inhibits activation of the NF-kappa B, NFAT, and activator protein 1 signaling pathways: R. Sancho, et al.; J. Immunol. 172, 2341 (2004) Abstract
[6] Characterisation of the vasorelaxant properties of the novel endocannabinoid N-arachidonoyl-dopamine (NADA): S.E. O'Sullivan, et al.; Br. J. Pharmacol. 141, 803 (2004) Abstract
[7] Mechanisms of HIV-1 inhibition by the lipid mediator N-arachidonoyldopamine: R. Sancho, et al.; J. Immunol. 175, 3990 (2005) Abstract
Synthesis and biological evaluation of novel amides of polyunsaturated fatty acids with dopamine: V. Bezuglov, et al.; Bioorg. Med. Chem. Lett. 11, 447 (2001) Abstract
Modulation of trigeminal sensory neuron activity by the dual cannabinoid-vanilloid agonists anandamide, N-arachidonoyl-dopamine and arachidonyl-2-chloroethylamide: T.J. Price, et al.; Br. J. Pharmacol. 141, 1118 (2004) Abstract
Mechanisms of HIV-1 Inhibition by the Lipid Mediator N-Arachidonoyldopamine: R. Sancho, et al.; J. Immunol. 175, 3990 (2005) Abstract

Further Categories Containing This Product:

Immunomodulators Other Products • Endovanilloids

ALX-350-128

Revised 03-Apr-08

Chetomin
SYNONYMS	Chaetomin
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Immunomodulators

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-128-M001		1 mg	185.00 USD
ALX-350-128-M005		5 mg	495.00 USD

Product Specification

FORMULA:	C₃₁H₃₀N₆O₆S₄
MW:	710.9
CAS NUMBER:	1403-36-7
SOURCE/HOST:	Isolated from Chaetomium species.
PURITY:	≥98% (HPLC)
APPEARANCE:	Off-white to fawn solid.
SOLUBILITY:	Soluble in DMSO, ethyl acetate or pyridine; fairly soluble in methanol, 100% ethanol; insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HAZARD:	TOXIC.
IDENTITY:	Determined by ¹H-NMR.

Product Description

Dithiodiketopiperazine inhibitor of HIF-1 formation by disrupting the binding of p300 to both HIF-1α and HIF-2α. Inhibitor of tumor growth. Potent immunosuppressor. Antibacterial.

Product Specific Literature References

The structure of chetomin: A.G. McInnes, et al.; JACS 98, 6741 (1976) Abstract
Effects of chetomin on growth and acidic fermentation products of rumen bacteria: W.C. Jen and G.A. Jones; Can. J. Microbiol. 29, 1399 (1983) Abstract
Small molecule blockade of transcriptional coactivation of the hypoxia-inducible factor pathway: A.L. Kung, et al.; Cancer Cell 6, 33 (2004) Abstract
Immunomodulatory constituents from an Ascomycete, Chaetomium seminudum: H. Fujimoto, et al.; J. Nat. Prod. 67, 98 (2004) Abstract
Effects of HIF-1 inhibition by chetomin on hypoxia-related transcription and radiosensitivity in HT 1080 human fibrosarcoma cells: A. Staab, et al.; BMC Cancer 7, 213 (2007) Abstract; Full Text

Further Categories Containing This Product:

Immunomodulators Other Products • Antitumor Agents (Anti-proliferative) • Hypoxia-inducible Factor [HIF]/Related Products • Antitumor Antibiotics

ALX-581-210

Revised 14-Feb-07

Cord Factor (endotoxin-free grade)
SYNONYMS	Trehalose 6,6’-dimycolate (endotoxin-free grade) TDM (endotoxin-free grade)
PRODUCT LINE	Immunology
PRODUCT CATEGORY	Immunomodulators Other Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-581-210-M001		1 mg	235.00 USD

Product Specification

CAS NUMBER:	61512-20-7
SOURCE/HOST:	Isolated from M. tuberculosis.
PURITY:	Single spot (TLC)
FORMULATION:	Lyophilized.
ENDOTOXIN CONTENT:	<0.002EU/µg (LAL test; BioWhittaker)
SOLUBILITY:	Soluble in chloroform:methanol:water (90:10:1) (5mg/ml), hexane or isopropanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C

Product Description

Immunomodulatory compound. Induces activation of macrophages independent of TLR2 or TLR4.

Product Specific Literature References

The chemical structure of the cord factor of Mycobacterium tuberculosis: H. Noll, et al.; Biochim. Biophys. Acta 20, 299 (1956) Abstract
Development of a trehalose 6,6’-dimycolate model which explains cord formation by Mycobacterium tuberculosis: C.A. Behling, et al.; Infect. Immun. 61, 2296 (1993) Abstract
Extravascular coagulation and fibrinolysis in murine lung inflammation induced by the mycobacterial cord factor trehalose-6,6’-dimycolate: R.L. Perez, et al.; Am. J. Respir. Crit. Care Med. 149, 510 (1994) Abstract
Immunological properties of trehalose dimycolate (cord factor) and other mycolic acid-containing glycolipids: R. Ryll, et al.; Microbiol. Immunol. 45, 801 (2001), Review Abstract
Mycobacterial glycolipid cord factor trehalose 6,6’-dimycolate causes a decrease in serum cortisol during the granulomatous response: J.K. Actor, et al.; Neuroimmunomodulation 10, 270 (2002) Abstract
Influence of trehalose 6,6’-dimycolate (TDM) during mycobacterial infection of bone marrow macrophages: J. Indrigo, et al.; Microbiology 148, 1991 (2002) Abstract
Cord factor trehalose 6,6’-dimycolate (TDM) mediates trafficking events during mycobacterial infection of murine macrophages: J. Indrigo, et al.; Microbiology 149, 2049 (2003) Abstract
Failure of CD1D-/- mice to elicit hypersensitive granulomas to mycobacterial cord factor trehalose 6,6’-dimycolate: T.V. Guidry, et al.; J. Interferon Cytokine Res. 24, 362 (2004) Abstract
Requisite role for complement C5 and the C5a receptor in granulomatous response to mycobacterial glycolipid trehalose 6,6’-dimycolate: C.W. Borders, et al.; Scand. J. Immunol. 62, 123 (2005) Abstract
In vivo activity of released cell wall lipids of Mycobacterium bovis bacillus Calmette-Guerin is due principally to trehalose mycolates: R.E. Geisel, et al.; J. Immunol. 174, 5007 (2005) Abstract
Macrophage scavenger receptor down-regulates mycobacterial cord factor-induced proinflammatory cytokine production by alveolar and hepatic macrophages: Y. Ozeki, et al.; Microb. Pathog. 40, 171 (2006) Abstract
Interferon-gamma independent formation of pulmonary granuloma in mice by injections with trehalose dimycolate (cord factor), lipoarabinomannan and phosphatidylinositol mannosides isolated from Mycobacterium tuberculosis: H. Takimoto, et al.; Clin. Exp. Immunol. 144, 134 (2006) Abstract

General Information

BACKGROUND/TECHNICAL INFORMATION

In vitro stimulation of macrophages
Purified Cord Factor was used to stimulate either mouse RAW 264.7 cells or bone marrow-derived macrophages. Cord Factor was suspended at a concentration of 1mg/ml in isopropanol and sonicated in a bath sonicator for 5 min. This suspension was incubated at 60°C for 10 min. and sonication repeated. The resulting solution was layered onto 24-well tissue culture plates at the indicated concentrations and incubated at 37°C in order to ensure complete evaporation of the solvent. Control wells were layered with solvent without Cord Factor and incubated at 37°C. To this layer of Cord Factor, either RAW 264.7 cells or bone marrow-derived macrophages were added at a concentration of 10⁶ cells in 100µl of medium and incubated at 37°C for 24 hours before activation e.g. TNF-α production was measured in the supernatant.
Alternatively, Cord Factor was suspended at a concentration of 0.2 or 2mg/ml in hexane. Of the resulting solution 50µl were layered onto 96-well tissue culture plates at the indicated concentrations of 1 or 10µg/well, respectively and the solvent completely evaporated. Control wells were layered with solvent without Cord Factor and incubated at 37°C. To this layer of Cord Factor, either RAW 264.7 cells or bone marrow-derived macrophages were added at a concentration of 10⁶ cells in 100µl of medium and incubated at 37°C for 24 hours before activation e.g. TNF-α production was measured in the supernatant.

In vivo pulmonary granuloma formation in mice
For in vivo experiments 10µg Cord Factor per mouse were applied i.v. in a water/oil/water emulsion.

Please also see our Product Flyer "Cord Factor - Endotoxin-free grade".

Further Categories Containing This Product:

Fatty Acids

ALX-420-043

Revised 22-May-08

FTY720
SYNONYMS	2-Amino-2-[2-(4-octylphenyl)ethyl]-1,3-propanediol . HCl Fingolimod . HCl
PRODUCT LINE	Immunology
PRODUCT CATEGORY	Immunomodulators Other Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-420-043-M001		1 mg	40.00 USD
ALX-420-043-M005		5 mg	190.00 USD

Product Specification

FORMULA:	C₁₉H₃₃NO₂ . HCl
MW:	307.5 . 36.5
CAS NUMBER:	162359-56-0
PURITY:	≥98%
APPEARANCE:	White to off-white crystalline solid.
SOLUBILITY:	20mg/ml soluble in 100% ethanol, DMSO or dimethyl formamide; sparingly soluble in aqueous buffers.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	We do not recommend storing aqueous solutions for more than one day.

Product Description

Analog of myriocin (Prod. No. ALX-350-274). Novel immune modulator that alters migration and homing of lymphocytes. Acts as a potent agonist of sphingosine 1-phosphate receptors (S1P) after phosphorylation by sphingosine kinase. Also inhibits cytosolic phospholipase A₂ independently of sphingosine 1-phosphate receptors.

Product Specific Literature References

The immune modulator FTY720 targets sphingosine 1-phosphate receptors: V. Brinkmann, et al.; J. Biol. Chem. 277, 21453 (2002) Abstract; Full Text
The immunosuppressant drug FTY720 inhibits cytosolic phospholipase A2 independently of sphingosine-1-phosphate receptors: S.G. Payne, et al.; Blood 109, 1077 (2007) Abstract
FTY720, a new alternative for treating blast crisis chronic myelogenous leukemia and Philadelphia chromosome-positive acute lymphocytic leukemia: P. Neviani, et al.; J. Clin. Invest. 117, 2408 (2007) Abstract; Full Text

Related Products

ALX-350-274

Myriocin

Further Categories Containing This Product:

PLA2 Inhibitors

ALX-158-005

Revised 06-Sep-07

Hymenistatin
PRODUCT LINE	Immunology
PRODUCT CATEGORY	Immunomodulators Other Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-158-005-M001		1 mg	230.00 USD
ALX-158-005-MC05		0.5 mg	390.00 USD

Product Specification

SEQUENCE:	cyclo(Pro-Pro-Tyr-Val-Pro-Leu-Ile-Ile)
FORMULA:	C₄₇H₇₂N₈O₉
MW:	893.2
PURITY:	≥97%
APPEARANCE:	White solid.
SOLUBILITY:	Soluble in methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Immunosuppressive. The effects in the humoral and cellular immune responses are comparable with that of cyclosporin A (Prod. No. ALX-380-002). Comparison of the influence of hymenistatin I and cyclosporin A on cytokine production suggests that the mechanism of the interaction with the immunological system are substantially different for the two compounds tested.

Product Specific Literature References

Immunosuppressive activity of hymenistatin I: M. Cebrat, et al.; Peptides 17, 191 (1996) Abstract

Further Categories Containing This Product:

Peptides

ALX-430-095

Revised 23-Jan-08

Leflunomide
SYNONYMS	HWA486 5-Methylisoxazole-4-(4-trifluoromethylcarboxanilide) N-(4-Trifluoromethylphenyl)-5-methylisoxazol-4-carboxamide
PRODUCT LINE	Immunology
PRODUCT CATEGORY	Immunomodulators Other Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-430-095-M010		10 mg	15.00 USD
ALX-430-095-M050		50 mg	40.00 USD
ALX-430-095-G001		1 g	380.00 USD

Product Specification

FORMULA:	C₁₂H₉F₃N₂O₂
MW:	270.2
CAS NUMBER:	75706-12-6
MERCK INDEX:	14: 5432
RTECS:	NY2354200
PURITY:	≥99% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in DMSO or methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	Keep under inert gas. Protect from light.
HAZARD:	HARMFUL.

Product Description

Immunosuppressive drug that inhibits T and B cell responses in vivo. Inhibitor of tyrosine phosphorylation (tyrosine kinase inhibitor), of dihydroorotate dehydrogenase, an enzyme for de novo pyrimidine synthesis, of TNF-dependent NF-κB activation, and of COX-2. The physiological activity of leflunomide is attributed mainly to its metabolite A77 1726 (Prod. No. ALX-430-096).

Product Specific Literature References

Immunopharmacological profile of a novel isoxazol derivative, HWA 486, with potential antirheumatic activity-I. Disease modifying action on adjuvant arthritis of the rat: R.R. Bartlett & R. Schleyerbach; Int. J. Immunopharmacol. 7, 7 (1985) Abstract
Leflunomide (HWA 486), a novel immunomodulating compound for the treatment of autoimmune disorders and reactions leading to transplantation rejection: R.R. Bartlett, et al.; Agents Actions 32, 10 (1991) Abstract
Inhibition of the epidermal growth factor receptor tyrosine kinase activity by leflunomide: T. Mattar, et al.; FEBS Lett. 334, 161 (1993) Abstract
Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide: X. Xu, et al.; J. Biol. Chem. 270, 12398 (1995) Abstract; Full Text
Molecular mechanisms of action of new xenobiotic immunosuppressive drugs: tacrolimus (FK506), sirolimus (rapamycin), mycophenolate mofetil and leflunomide: T.R. Brazelton & R.E. Morris; Curr. Opin. Immunol. 8, 710 (1996) Abstract
The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase: J.P. Davis, et al.; Biochemistry 35, 1270 (1996) Abstract
Regulation of B cell function by the immunosuppressive agent leflunomide: K.F. Siemasko, et al.; Transplantation 61, 635 (1996) Abstract
Two activities of the immunosuppressive metabolite of leflunomide, A77 1726. Inhibition of pyrimidine nucleotide synthesis and protein tyrosine phosphorylation: X. Xu, et al.; Biochem. Pharmacol. 52, 527 (1996) Abstract
Potencies of leflunomide and HR325 as inhibitors of prostaglandin endoperoxide H synthase-1 and -2: comparison with nonsteroidal anti- inflammatory drugs: A.P. Curnock, et al.; J. Pharmacol. Exp. Ther. 282, 339 (1997) Abstract
In vivo mechanism by which leflunomide controls lymphoproliferative and autoimmune disease in MRL/MpJ-lpr/lpr mice: X. Xu, et al.; J. Immunol. 159, 167 (1997) Abstract
Leflunomide, a novel immunomodulating agent, prevents the development of allergic sensitization in an animal model of allergic asthma: E. Eber, et al.; Clin. Exp. Allergy 28, 376 (1998) Abstract
Species-related inhibition of human and rat dihydroorotate dehydrogenase by immunosuppressive isoxazol and cinchoninic acid derivatives: W. Knecht & M. Löffler; Biochem. Pharmacol. 56, 1259 (1998) Abstract
Inhibition of JAK3 and STAT6 tyrosine phosphorylation by the immunosuppressive drug leflunomide leads to a block in IgG1 production: K.F. Siemasko, et al.; J. Immunol. 160, 1581 (1998)