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G-Protein Coupled Receptor Signalling
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ALX-155-007 Revised 24-Feb-05
ETB-Receptor Antagonist [IRL-1038]
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SYNONYMS [Cys11-Cys15]-Endothelin-1 (11-21)
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Endothelins [ETs] & Endothelin Receptors/Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-155-007-PC05   0.5 mg* 110.00 USD Add To Cart
ALX-155-007-P001   1 mg* 190.00 USD Add To Cart
Product Specification
SEQUENCE: H-Cys-Val-Tyr-Phe-Cys-His-Leu-Asp-Ile-Ile-Trp-OH
(Disulfide bonds between Cys1-Cys5)
FORMULA: C68H92N14O15S2
MW: 1409.7
QUANTITY: *Sold as net peptide weight.
PURITY: ≥97%
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Antagonist for the ETB receptor with a controversial pattern of activity.
Product Specific Literature References
A potent and specific agonist, Suc-[Glu9,Ala11,15]-endothelin-1(8-21), IRL 1620, for the ETB receptor: M. Takai, et al.; BBRC 184, 953 (1992) Abstract
An endothelin B receptor-selective antagonist: IRL 1038, [Cys11-Cys15]- endothelin-1(11-21) [retracted in: FEBS Lett 1994 Mar 28;342(1):103]: Y. Urade, et al.; FEBS Lett. 311, 12 (1992) Abstract
Endothelin: progress in pharmacology and physiology: W.G. Haynes, et al.; TIPS 14, 225 (1993), (Review) Abstract
An endothelin B receptor-selective antagonist: IRL 1038, [Cys11- Cys15]- endothelin-1(11-21): Y. Urade, et al.; FEBS Lett. 342, 103 (1994) Abstract
Further Categories Containing This Product:
Peptides
 
 
ALX-155-018 Revised 23-Oct-07
ETB-Receptor Antagonist [RES-701-1]
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Endothelins [ETs] & Endothelin Receptors/Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-155-018-MC05   0.5 mg 130.00 USD Add To Cart
ALX-155-018-M001   1 mg 200.00 USD Add To Cart
Product Specification
SEQUENCE: Gly-Asn-Trp-His-Gly-Thr-Ala-Pro-Asp-Trp-Phe-Phe-Asn-Tyr-Tyr-Trp-OH
(Beta peptide bond between Gly1and Asp9).
FORMULA: C103H115N23O23
MW: 2043.2
PEPTIDE CONTENT: 75-90%
PURITY: ≥97% (HPLC)
FORMULATION: Lyophilized.
SOLUBILITY: Soluble in DMSO (5mg/ml); dilute with 0.6ml distilled water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
Inhibits selectively the ET-1 binding to the ETB receptor.
Product Specific Literature References
RES-701-1, a novel and selective endothelin type B receptor antagonist produced by Streptomyces sp. RE-701. I. Characterization of producing strain, fermentation, isolation, physico-chemical and biological properties: Y. Morishita, et al.; J. Antibiot. 47, 269 (1994) Abstract
Subtypes of endothelin ETA and ETB receptors mediating venous smooth muscle contraction: S.A. Sudjarwo, et al.; BBRC 200, 627 (1994) Abstract
J.X. He, et al.; Bioorg. Med. Chem. Lett. 5, 621 (1995)
Further Categories Containing This Product:
Peptides
 
 
ALX-155-019 Revised 02-Dec-04
ETB-Receptor Antagonist [RES-701-3]
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Endothelins [ETs] & Endothelin Receptors/Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-155-019-MC05   0.5 mg 130.00 USD Add To Cart
ALX-155-019-M001   1 mg 240.00 USD Add To Cart
Product Specification
SEQUENCE: Gly-Asn-Trp-His-Gly-Thr-Ser-Pro-Asp-Trp-Phe-Phe-Asn-Tyr-Tyr-Trp-OH
(Beta peptide bond between Gly1and Asp9).
FORMULA: C103H115N23O24
MW: 2059.2
PURITY: ≥97%
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Further Categories Containing This Product:
Peptides
 
 
ALX-550-324 Revised 28-Jan-05
(2S)-α-Ethylglutamic acid
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SYNONYMS EGLU
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic)/Related Products
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ALX-550-324-M001   1 mg 35.00 USD Add To Cart
ALX-550-324-M005   5 mg 95.00 USD Add To Cart
Product Specification
FORMULA: C7H13NO4
MW: 175.2
PURITY: ≥98%
APPEARANCE: White solid.
SOLUBILITY: Soluble in dilute aqueous base.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Group II mGluR antagonist.
Product Specific Literature References
Potent antagonists at the L-AP4- and (1S,3S)-ACPD-sensitive presynaptic metabotropic glutamate receptors in the neonatal rat spinal cord: D.E. Jane, et al.; Neuropharmacology 35, 1029 (1996) Abstract
Group 1 and 2 metabotropic glutamate receptors play differential roles in hippocampal long-term depression and long-term potentiation in freely moving rats: D. Manahan-Vaughan; J. Neurosci. 17, 3303 (1997) Abstract
Bidirectional synaptic plasticity in the rat basolateral amygdala: characterization of an activity-dependent switch sensitive to the presynaptic metabotropic glutamate receptor antagonist 2S-alpha-eth: H. Li, et al.; J. Neurosci. 18, 1662 (1998) Abstract
Induction of long-lasting depression by (+)-alpha-methyl-4-carboxyphenylglycine and other group II mGlu receptor ligands in the dentate gyrus of the hippocampus in vitro: L. Huang, et al.; Eur. J. Pharmacol. 366, 151 (1999) Abstract
Pharmacological agents acting at subtypes of metabotropic glutamate receptors: D.D. Schoepp, et al.; Neuropharmacology 38, 1431 (1999), (Review) Abstract
 
 
ALX-290-002 Revised 13-Dec-04
S-Farnesylated Cysteine Tetrapeptide
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Farnesylation/Isoprenylation Reagents
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ALX-290-002-M001   1 mg 45.00 USD Add To Cart
ALX-290-002-M005   5 mg 150.00 USD Add To Cart
Product Specification
SEQUENCE: Ac-Cys(farnesyl)-Val-Ile-Met-OH
FORMULA: C36H62N4O6S2
MW: 711.0
PURITY: ≥95%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in chloroform.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic. Protect from light and oxygen.
Product Description
Tetrapeptide substrate for the protein endoprotease that cleaves the modified protein at the isoprenylated cysteine residue.
Product Specific Literature References
Inhibitors of the isoprenylated protein endoprotease: Y.-T. Ma, et al.; Biochemistry 32, 2386 (1993) Abstract
 
 
ALX-290-003 Revised 30-Jun-08
Farnesylpyrophosphate . triammonium salt
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SYNONYMS FPP . 3NH4
3,7,11-Trimethyl-2,6,10-dodecatrien-1-ol pyrophosphate . 3NH4
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Farnesylation/Isoprenylation Reagents
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ALX-290-003-C200   200 µg 62.00 USD Add To Cart
Product Specification
FORMULA: C15H25O7P2 . 3NH4
MW: 379.3 . 54.1
CAS NUMBER: 13058-04-3
PURITY: ≥98% (TLC)
APPEARANCE: Liquid. Solution in 0.25M ammonium bicarbonate containing 70% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY:

Store solutions at -20°C for up to 3 months.

HANDLING: Protect from light and moisture.

Product Description
Farnesyl donor in enzymatic protein farnesylation catalyzed by farnesyltransferase.
Product Specific Literature References
Tautomycin from the bacterium Streptomyces verticillatus. Another potent and specific inhibitor of protein phosphatases 1 and 2A: C. MacKintosh & S. Klumpp; FEBS Lett. 277, 137 (1990) Abstract
M. Ubukata, et al.; J. C. S. Chem. Commun. 244 (1990)
Divalent cation and prenyl pyrophosphate specificities of the protein farnesyltransferase from rat brain, a zinc metalloenzyme: Y. Reiss, et al.; J. Biol. Chem. 267, 6403 (1992) Abstract; Full Text
Inhibitors of Ras farnesyltransferases: F. Tamanoi; TIBS 18, 349 (1993), (Review) Abstract
Farnesyltransferase inhibitors: Ras research yields a potential cancer therapeutic: J.B. Gibbs, et al.; Cell 77, 175 (1994) Abstract
 
 
ALX-290-004 Revised 25-Oct-06
Farnesylthioacetic acid
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SYNONYMS FTA
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Farnesylation/Isoprenylation Reagents
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ALX-290-004-M005   5 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C17H28O2S
MW: 296.5
CAS NUMBER: 135784-48-4
PURITY: ≥98%
APPEARANCE: Yellow viscous oil.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Solutions are stable for up to 6 months when stored at -20°C. Product is not sterile.
HANDLING: Protect from light.

Product Description
Potent and specific inhibitor of methyl esterification of farnesylated proteins (e.g. the γ subunit of transducin). This compound is not a methyltransferase substrate.
Product Specific Literature References
Identifying the recognition unit for G protein methylation: E.W. Tan, et al.; J. Biol. Chem. 266, 10719 (1991) Abstract; Full Text
 
 
ALX-290-005 Revised 10-Aug-05
Farnesyltransferase Inhibitor
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SYNONYMS B581
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Farnesylation/Isoprenylation Reagents
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ALX-290-005-M001   1 mg 85.00 USD Add To Cart
ALX-290-005-M005   5 mg 320.00 USD Add To Cart
Product Specification
SEQUENCE: N-[(2S)-((2R)-Amino-3-mercaptopropylamino)-3-methylbutyl]-Phe-Met-OH
FORMULA: C22H38N4O3S2
MW: 470.7
PURITY: ≥96%
APPEARANCE: White powder.
SOLUBILITY: Soluble in water or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic.

Product Description
Stable, membrane permeable inhibitor of farnesyltransferase. Has 30-fold higher selectivity for farnesyltransferase over geranylgeranyltransferase. Potential anticancer drug.
Product Specific Literature References
Peptidomimetic inhibitors of Ras farnesylation and function in whole cells: A.M. Garcia, et al.; J. Biol. Chem. 268, 18415 (1993) Abstract; Full Text
 
 
ALX-550-413 Revised 23-May-06
Fenobam
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PRODUCT LINE Neurobiology
PRODUCT CATEGORY Glutamate Receptors (Metabotropic)/Related Products
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ALX-550-413-M005   5 mg 60.00 USD Add To Cart
ALX-550-413-M025   25 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C11H11ClN4O2
MW: 266.7
CAS NUMBER: 57653-26-6
PURITY: ≥98% (1H-NMR)
APPEARANCE: Off-white to pale orange solid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
IDENTITY: Determined by 1H-NMR and 13C-NMR.

Product Description
Potent and selective non-competitive mGluR5 antagonist that displays inverse agonist properties; blocks mGluR5 constitutive activity in vitro (IC50=87nM). Acts at an allosteric modulatory site shared with MPEP (Prod. No. ALX-550-368) and binds mGluR5 with Kd values of 54nM and 31nM for rat and human receptors respectively. Displays anxiolytic activity following oral administration in vivo.
Product Specific Literature References
Novel non-benzodiazepine anxiolytics: M.E. Goldberg, et al.; Neuropharmacology 22, 1499 (1983) Abstract
In vitro and in vivo metabolism of the antianxiolytic agent fenobam in the rat: W.N. Wu, et al.; J. Pharm. Sci. 84, 185 (1995) Abstract
Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity: R.H. Porter, et al.; J. Pharmacol. Exp. Ther. 315, 711 (2005) Abstract
Phenyl ureas of creatinine as mGluR5 antagonists. A structure-activity relationship study of fenobam analogues: A. Wallberg et al.; Bioorg. Med. Chem. Lett. 16, 1142 (2006) Abstract
Related Products
Further Categories Containing This Product:
Anxiolytic Agents/Related Products
 
 
ALX-380-052 Revised 16-Oct-07
Fusaric acid
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SYNONYMS 5-Butylpicolinic acid
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics Other Products
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ALX-380-052-M050   50 mg 20.00 USD Add To Cart
Product Specification
FORMULA: C10H13NO2
MW: 179.2
CAS NUMBER: 536-69-6
MERCK INDEX: 14: 4314
SOURCE/HOST: Isolated from Gibberella fujikuroi.
PURITY: ≥99%
APPEARANCE: White solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: TOXIC.

 

Product Description
Antibiotic. Inhibitor of dopamine β-hydroxylase.
Product Specific Literature References
Biochemistry of the bakanaefungus. I. Fusarinic acid, a new product of the bakanae fungus: T. Yubata, et al.; J. Agric. Chem. Soc. Jpn. 10, 1059 (1934)
Pharmacological activities of fusaric acid (5-butylpicolinic acid): H. Wang & T.B. Ng; Life Sci. 65, 849 (1999), Review Abstract
Further Categories Containing This Product:
Dopaminergics & Dopamine Receptors/Related Products
 
 
ALX-157-003 Revised 03-Mar-05
Galanin (human)
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PRODUCT LINE Obesity & Adipokines
PRODUCT CATEGORY Galanin & Galanin Receptor/Related Products
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ALX-157-003-PC05   0.5 mg* 190.00 USD Add To Cart
ALX-157-003-P001   1 mg* 280.00 USD Add To Cart
Product Specification
SEQUENCE: H-Gly-Trp-Thr-Leu-Asn-Ser-Ala-Gly-Tyr-Leu-Leu-Gly-Pro-His-Ala-Val-Gly-Asn-His-Arg-Ser-Phe-Ser-Asp-Lys-Asn-Gly-Leu-Thr-Ser-OH
FORMULA: C139H210N42O43
MW: 3157.4
CAS NUMBER: 119418-04-1
QUANTITY: *Sold as net peptide weight.
PURITY: ≥98%
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Specific Literature References
Galanin: profile of a new neuropeptide: L.W. Haynes; TIPS 7, 214 (1986), (Review)
Galanin - a newly isolated biologically active neuropeptide: A. Rökaeus; Trends Neurosci. 10, 158 (1987)
Galanin and the endocrine pancreas: B. Ahren, et al.; FEBS Lett. 229, 233 (1988) Abstract
Galanin. A selective inhibitor of insulin secretion?: J. Dupré; Pancreas 3, 119 (1988) Abstract
Co-existence of galanin and acetylcholine: is galanin involved in memory processed and dementia?: J.N. Crawley & G.L. Wenk; TINS 12, 278 (1989) Abstract
Inhibitory action of galanin on gastric acid secretion in pentobarbital-anesthetized rats: W.J. Rossowski & D.H. Coy; Life Sci. 44, 1807 (1989) Abstract
Galanin in the porcine pancreas: T. Messell, et al.; Regul. Pept. 28, 161 (1990)