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Ion Channels & Transporters / Related Products
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ALX-420-037 Revised 11-Feb-08
Icilin
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SYNONYMS AG 3-5
3,6-Dihydro-1-(2-hydroxyphenyl)-4-(3-nitrophenyl)-2(1H)-pyrimidinone
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Neuroactive Agents Other Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-420-037-M001   1 mg 10.00 USD Add To Cart
ALX-420-037-M005   5 mg 32.00 USD Add To Cart
ALX-420-037-M025   25 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C16H13N3O4
MW: 311.3
CAS NUMBER: 36945-98-9
PURITY: ≥98% (1H-NMR)
APPEARANCE: Light yellow solid.
SOLUBILITY: Soluble in DMSO (100mM).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Cooling agent. Strongly activates TRPM8 (cold menthol receptor 1; CMR1) and TRPA1 (at 10- to 100-fold higher concentration). Induces currents in TRPM8 expressing HEK 293 cells (EC50=0.36mM) more potently than menthol (Prod. No. ALX-420-042) or low temperatures.
Product Specific Literature References
AG-3-5: a chemical producing sensations of cold: E.T. Wei and D.A. Seid; J. Pharm. Pharmacol. 35, 110 (1983) Abstract
Identification of a cold receptor reveals a general role for TRP channels in thermosensation: D.D. McKemy, et al.; Nature 416, 52 (2002) Abstract
TRPM8 activation by menthol, icilin, and cold is differentially modulated by intracellular pH: D.A. Andersson, et al.; J. Neurosci. 24, 5364 (2004) Abstract; Full Text
The super-cooling agent icilin reveals a mechanism of coincidence detection by a temperature-sensitive TRP channel: H.H. Chuang, et al.; Neuron 43, 859 (2004) Abstract
Icilin activates the {delta}-subunit of the human epithelial Na+ channel.: H. Yamamura; Mol. Pharmacol. 68, 1142 (2005) Abstract
Sensing with TRP channels: T. Voets, et al.; Nat. Chem. Biol. 1, 85 (2005), Review Abstract
Analgesia mediated by the TRPM8 cold receptor in chronic neuropathic pain: C.J. Proudfoot, et al.; Curr. Biol. 16, 1591 (2006) Abstract
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Further Categories Containing This Product:
TRP Channels Other Products
 
 
ALX-550-062 Revised 11-Jan-07
IDRA 21
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SYNONYMS 7-Chloro-3-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine-S,S-dioxide
PRODUCT LINE Neurobiology
PRODUCT CATEGORY AMPA Receptors / Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-550-062-M005   5 mg 60.00 USD Add To Cart
ALX-550-062-M025   25 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C8H9ClN2O2S
MW: 232.7
CAS NUMBER: 22503-72-6
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol, methanol or dilute aqueous base.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Analog of cyclothiazide (Prod. No. ALX-550-338). Inhibits AMPA receptor desensitization. Crosses the blood-brain barrier more readily than cyclothiazide (Prod. No. ALX-550-338) and diazoxide (Prod. No. ALX-550-260) and is a more potent cognitive enhancing drug.
Product Specific Literature References
Modulation of AMPA/kainate receptors by analogues of diazoxide and cyclothiazide in thin slices of rat hippocampus: M. Bertolino, et al.; Receptors Channels 1, 267 (1993) Abstract
7-Chloro-3-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine S,S-dioxide (IDRA 21), a congener of aniracetam, potently abates pharmacologically induced cognitive impairments in patas monkeys: D.M. Thompson, et al.; PNAS 92, 7667 (1995) Abstract
7-Chloro-3-methyl-3-4-dihydro-2H-1,2,4 benzothiadiazine S,S-dioxide (IDRA 21): a benzothiadiazine derivative that enhances cognition by attenuating DL-alpha-amino-2,3-dihydro-5-methyl-3-oxo-4-isoxazol: I. Zivkovic, et al.; J. Pharmacol. Exp. Ther. 272, 300 (1995) Abstract
Effect of the AMPA receptor modulator IDRA 21 on LTP in hippocampal slices: A. Arai, et al.; Neuroreport 7, 2211 (1996) Abstract
7-Chloro-3-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine S,S-dioxide: a partial modulator of AMPA receptor desensitization devoid of neurotoxicity: F. Impagnatiello, et al.; PNAS 94, 7053 (1997) Abstract
The diazoxide derivative 7-chloro-3-methyl-3,4-dihydro-2H-1,2,4-benzothiadiazine-S,S-dioxide augments AMPA- and GABA-mediated synaptic responses in cultured hippocampal neurons: K.A. Yamada, et al.; Neurobiol. Dis. 5, 196 (1998) Abstract
The diazoxide derivative IDRA 21 enhances ischemic hippocampal neuron injury: K.A. Yamada, et al.; Ann. Neurol. 43, 664 (1998) Abstract
 
 
ALX-350-302 Revised 14-Dec-07
Imperatorin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Apoptosis Inducers & Inhibitors
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ALX-350-302-M002   2 mg 70.00 USD Add To Cart
Product Specification
FORMULA: C16H14O4
MW: 270.3
PURITY: ≥99% (HPLC)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in DMSO or dimethyl formamide; slightly soluble in methanol or water. Almonst insoluble in 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
The furanocoumarins heraclenin (Prod. No. ALX-350-303) and imperatorin (Prod. No. ALX-350-302) inhibit T cell-receptor-mediated proliferation in human primary T cells in a concentration-dependent manner. Both compounds also induce apoptosis. While imperatorin induces DNA fragmentation at the G1/S phase of the cell cycle, heraclenin induces DNA fragmentation at the G2/M phases of the cell cycle, thus despite a close structural similarity they induce apoptosis in mechanistically different ways. Imperatorin inhibits HIV-1 replication as well as the expression of ICAM-1 in U937 foam cells. Inhibits voltage-dependent calcium channel.
Product Specific Literature References
Expression of intercellular adhesion molecule-1 in U937 foam cells and inhibitory effect of imperatorin: P.Y. Yang, et al.; Acta Pharmacol. Sin. 23, 327 (2002) Abstract
Imperatorin, a furanocoumarin from Angelica dahurica (Umbelliferae), induces cytochrome c-dependent apoptosis in human promyelocytic leukaemia, HL-60 Cells: H.O. Pae, et al.; Pharmacol. Toxicol. 91, 40 (2002) Abstract
Coumarins from Opopanax chironium. New dihydrofuranocoumarins and differential induction of apoptosis by imperatorin and heraclenin: G. Appendino, et al.; J. Nat. Prod. 67, 532 (2004) Abstract
Imperatorin inhibits T-cell proliferation by targeting the transcription factor NFAT: N. Marquez, et al.; Planta Med. 70, 1016 (2004) Abstract
Imperatorin inhibits HIV-1 replication through an Sp1-dependent pathway: R. Sancho, et al.; J. Biol. Chem. 279, 37349 (2004) Abstract; Full Text
Imperatorin induces vasodilatation possibly via inhibiting voltage dependent calcium channel and receptor-mediated Ca2+ influx and release: J.Y. He, et al.; Eur. J. Pharmacol. 573, 170 (2007) Abstract
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Further Categories Containing This Product:
DNA Fragmentation & Chromatin Condensation • Natural Products - Antiviral / anti-HIV Agents • CD11a, CD18 [LFA-1] & CD54 [ICAM-1], CD102 [ICAM-2], CD50 [ICAM-3] / Related Products • Ca2+ Channels Other Products • HIV / AIDS / Related Products
 
 
ALX-350-122 Revised 07-Apr-08
6’-Iodononivamide
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SYNONYMS 6-Iodonordihydrocapsaicin
N-(4-Hydroxy-6-iodo-
3-methoxybenzyl)nonanamide
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Neurotoxins
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ALX-350-122-M005   5 mg 60.00 USD Add To Cart
ALX-350-122-M010   10 mg 95.00 USD Add To Cart
Product Specification
FORMULA: C17H26INO3
MW: 419.3
PURITY: ≥99% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in 100% ethanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Potent competitive TRPV1 antagonist (IC50=10nM against 100nM capsaicin; Prod. No. ALX-550-066). Convenient replacement for capsazepine (Prod. No. ALX-550-145) in most of the in vitro preparations currently used to assess the activity of putative vanilloid receptor agonists.
Product Specific Literature References
Halogenation of a capsaicin analogue leads to novel vanilloid TRPV1 receptor antagonists: G. Appendino, et al.; Br. J. Pharmacol. 139, 1417 (2003) Abstract
The taming of capsaicin. Reversal of the vanilloid activity of N-acylvanillamines by aromatic iodination: G. Appendino, et al.; J. Med. Chem. 48, 4663 (2005) Abstract
Further Categories Containing This Product:
TRPV1 Agonists and Antagonists / Related Products
 
 
ALX-550-389 Revised 11-Apr-08
5’-Iodo-resiniferatoxin
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SYNONYMS I-RTX
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Neurological Research
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ALX-550-389-M001   1 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C37H39IO9
MW: 754.6
PURITY: ≥97% (HPLC)
APPEARANCE: White amorphous solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC.

Product Description
Binds to TRPV1 receptors expressed in HEK 293 cells (Ki=5.8nM) and to native rat TRPV1 receptors (Ki=4.8nM). At least 40-fold more potent than capsazepine (Prod. No. ALX-550-145). Blocks capsaicin-induced currents in oozytes expressing TRPV1 (IC50=3.9nM). Potently blocks pain responses elicited by capsaicin (Prod. No. ALX-550-066) in vivo.
Product Specific Literature References
Iodo-resiniferatoxin, a new potent vanilloid receptor antagonist: P. Wahl, et al.; Mol. Pharmacol. 59, 9 (2001) Abstract; Full Text
Functional properties of the high-affinity TRPV1 (VR1) vanilloid receptor antagonist (4-hydroxy-5-iodo-3-methoxyphenylacetate ester) iodo-resiniferatoxin: G.R. Seabrook, et al.; J. Pharmacol. Exp. Ther. 303, 1052 (2002) Abstract; Full Text
Synthesis and in vitro evaluation of a novel iodinated resiniferatoxin derivative that is an agonist at the human vanilloid VR1 receptor: M.E. McDonnell, et al.; Bioorg. Med. Chem. Lett. 12, 1189 (2002) Abstract
Neurogenic responses mediated by vanilloid receptor-1 (TRPV1) are blocked by the high affinity antagonist, iodo-resiniferatoxin: M. Rigoni, et al.; Br. J. Pharmacol. 138, 977 (2003) Abstract; Full Text
Participation of the spinal TRPV1 receptors in formalin-evoked pain transduction: a study using a selective TRPV1 antagonist, iodo-resiniferatoxin: Y. Kanai, et al.; J. Pharm. Pharmacol. 58, 489 (2006) Abstract
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Further Categories Containing This Product:
TRPV1 Agonists and Antagonists / Related Products • Resiniferatoxin-type Phorboid Vanilloids
 
 
ALX-450-006 Revised 07-Apr-08
Ionomycin (free acid)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Ionophores
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ALX-450-006-M001   1 mg 75.00 USD Add To Cart
ALX-450-006-M005   5 mg 290.00 USD Add To Cart
Product Specification
FORMULA: C41H72O9
MW: 709.0
CAS NUMBER: 56092-81-0
SOURCE/HOST: Isolated from Streptomyces conglobatus.
PURITY: ≥90%
APPEARANCE: Pale-yellow oil.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions are stable for 1 year when stored at +4°C.
HANDLING: Protect from light. Keep under inert gas.
HAZARD: HARMFUL.

Product Description
Potent and selective calcium ionophore. Ca2+/ionomycin complex forms between pH 7-9.5 which has intense UV absorption. Induces apoptotic neuronal degeneration in embryonic cortical neurons and cell cycle arrest at G1 phase.
Product Specific Literature References
Characterization of ionomycin as a calcium ionophore: C.M. Liu & T.E. Herman; J. Biol. Chem. 253, 5892 (1978) Abstract; Full Text
Structure of ionomycin - a novel diacidic polyether antibiotic having high affinity for calcium ions: B.K. Toeplitz at al.; JACS 101, 3344 (1979)
Demonstration of a calcium requirement for secretory protein processing and export. Differential effects of calcium and dithiothreitol: G. Kuznetsov, et al.; J. Biol. Chem. 267, 3932 (1992) Abstract; Full Text
Potentiation of calcium- and caffeine-induced calcium release by cyclic ADP-ribose: H.C. Lee; J. Biol. Chem. 268, 293 (1993) Abstract; Full Text
Contrasting effect of transforming growth factor type beta 1 (TGF-beta 1) on proliferation and interleukin-2 receptor expression in activated and rapidly cycling immature (CD3-CD4-CD8-) thymocytes: A. Dupuy d'Angeac, et al.; J. Cell. Physiol. 154, 44 (1993) Abstract
Ca2+ ionophore-induced apoptosis on cultured embryonic rat cortical neurons: N. Takei & Y. Endo; Brain Res. 652, 65 (1994) Abstract
Differential activation of a calcium-dependent endonuclease in human B lymphocytes. Role in ionomycin-induced apoptosis: K.M. Aagaard-Tillery & D.F. Jelinek; J. Immunol. 155, 3297 (1995) Abstract
ctivation of stress response by ionomycin in rat hepatoma cells: A. S. Sreedhar & U. K. Srinivas; J. Cell. Biochem. 86, 154 (2002) Abstract
Ionomycin downregulates beta-catenin/Tcf signaling in colon cancer cell line: C.H. Park, et al.; Carcinogenesis 26, 1929 (2005) Abstract
Further Categories Containing This Product:
Antibiotics - Apoptosis Inducers & Inhibitors • Antibiotics for Cell Cycle Research • Cell Cycle Blockers & Inhibitors / Related Products
 
 
ALX-450-007 Revised 20-Aug-08
Ionomycin . calcium salt
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Ionophores
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ALX-450-007-M001   1 mg 80.00 USD Add To Cart
ALX-450-007-M005   5 mg 320.00 USD Add To Cart
Product Specification
FORMULA: C41H70O9 . Ca
MW: 707.0 . 40.1
CAS NUMBER: 56092-82-1
SOURCE/HOST: Isolated from Streptomyces conglobatus.
PURITY: ≥97%
APPEARANCE: White solid.
SOLUBILITY: 10mg/ml soluble in DMSO or 100% ethanol, 5mg/ml soluble in methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: HARMFUL.

Product Description
For technical information and literature references see Ionomycin (free acid) (Prod. No. ALX-450-006).
Further Categories Containing This Product:
Antibiotics - Apoptosis Inducers & Inhibitors • Antibiotics for Cell Cycle Research • Cell Cycle Blockers & Inhibitors / Related Products
 
 
ALX-550-356 Revised 19-May-06
Isovelleral
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PRODUCT LINE Neurobiology
PRODUCT CATEGORY TRPV1 Agonists and Antagonists / Related Products
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ALX-550-356-M001   1 mg 45.00 USD Add To Cart
ALX-550-356-M005   5 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C15H20O2
MW: 232.3
CAS NUMBER: 37841-91-1
PURITY: ≥99%
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in organic solvents.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: IRRITANT.

Product Description
Antagonist with different binding profiles towards the vanilloid receptor 1 (TRPV1).
Product Specific Literature References
Fungal extractives I. structure of a sesquiterpene dialdehyde from Lactarius by computer simulation of the nmr spectrum: G. Magnusson, et al.; THL 13, 1105 (1972), (Isolation)
Comparison of the antimicrobial and cytotoxic activities of twenty unsaturated sesquiterpene dialdehydes from plants and mushrooms: H. Anke & O. Sterner; Planta Med. 57, 344 (1991) Abstract
The stimulation of capsaicin-sensitive neurones in a vanilloid receptor-mediated fashion by pungent terpenoids possessing an unsaturated 1,4-dialdehyde moiety: A. Szallasi, et al.; Br. J. Pharmacol. 119, 283 (1996) Abstract
The preparation and bioactivities of (-)-isovelleral: M. Jonassohn, et al.; Bioorg. Med. Chem. 5, 1363 (1997) Abstract
 
 
ALX-550-296 Revised 28-Jun-07
JYL-79
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SYNONYMS 2-(3,4-Dimethylbenzyl)-3-{[(4-hydroxy-3-methoxy-benzyl)amino]carbothioyl}propyl pivalate
Vanilloid Receptor Agonist 23
PRODUCT LINE Neurobiology
PRODUCT CATEGORY TRPV1 Agonists and Antagonists / Related Products
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ALX-550-296-M001   1 mg 80.00 USD Add To Cart
ALX-550-296-M005   5 mg 320.00 USD Add To Cart
Product Specification
FORMULA: C26H36N2O4S
MW: 472.6
PURITY: ≥98%
APPEARANCE: Off-white to yellow sticky solid.
SOLUBILITY: Soluble in methanol, 100% ethanol, DMSO or other organic solvents; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description

Potent TRPV1 agonist (Ki=19nM). About 300-fold more potent than capsaicin (Prod. No. ALX-550-066). RTX binding affinity (Ki=17.4nM), agonism (calcium influx; EC50=1.97nM).
Product Specific Literature References
N-(3-Acyloxy-2-benzylpropyl)-N'-(4-hydroxy-3-methoxybenzyl) thiourea derivatives as potent vanilloid receptor agonists and analgesics: J. Lee, et al.; Bioorg. Med. Chem. 9, 19 (2001) Abstract
Phenolic modification as an approach to improve the pharmacology of the 3-acyloxy-2-benzylpropyl homovanillic amides and thioureas, a promising class of vanilloid receptor agonists and analgesics: J. Lee, et al.; Bioorg. Med. Chem. 10, 1171 (2002) Abstract
 
 
ALX-550-390 Revised 28-Jun-07
JYL-273