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A-317491

Catalog No. TQ0002 CAS 475205-49-3

Synonyms: ABT 202

A-317491 (ABT 202) is a non-nucleotide P2X3 ( Ki: 22 nM) and P2X2/3 receptor (Ki: 9 nM) antagonist, which inhibits calcium flux mediated by the receptors.

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A-317491, CAS 475205-49-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
5 mg	In stock	$ 64.00
10 mg	In stock	$ 98.00
25 mg	In stock	$ 198.00
50 mg	In stock	$ 328.00
100 mg	In stock	$ 493.00
1 mL * 10 mM (in DMSO)	In stock	$ 80.00

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Purity: 96.1%

Biological Description

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Storage & Solubility Information

Description	A-317491 (ABT 202) is a non-nucleotide P2X3 ( Ki: 22 nM) and P2X2/3 receptor (Ki: 9 nM) antagonist, which inhibits calcium flux mediated by the receptors.
Targets&IC50	P2X3:22 nM(Ki, cell free), P2X2:9 nM (Ki, cell free)
In vitro	A-317491 blocks recombinant human and rat P2X3 and P2X2/3 receptor-mediated calcium flux (Ki = 22-92 nM) and is highly selective (IC50 >10 μM) over other P2 receptors and other ion channels, neurotransmitter receptors, and enzymes [1].
In vivo	A-317491 dose-dependently reduces complete Freund's adjuvant-induced thermal hyperalgesia in the rat (ED50: 30 μmol/kg s.c.). A-317491 is most potent in attenuating both thermal hyperalgesia and mechanical allodynia after chronic nerve constriction injury (ED50: 10-15 μmol/kg s.c.). Although active in chronic pain models, A-317491 is ineffective in reducing nociception in animal models of acute pain, postoperative pain, and visceral pain (ED50 >100 μmol/kg s.c.) [1]. A-317491 is effective in reducing pain associated behavior in several animal models of inflammatory and neuropathic pain when administered systemically [2].

Synonyms	ABT 202
Molecular Weight	565.57
Formula	C33H27NO8
CAS No.	475205-49-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 47 mg/mL (83.10 mM)

Ethanol: 90 mg/mL (159.13 mM)

H2O: < 0.1 mg/mL (insoluble)

References and Literature

1. Jarvis MF,et al. A-317491, a novel potent and selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, reduces chronic inflammatory and neuropathic pain in the rat. Proc Natl Acad Sci U S A. 2002 Dec 24;99(26):17179-84. 2. Wu G, et al. A-317491, a selective P2X3/P2X2/3 receptor antagonist, reverses inflammatory mechanical hyperalgesia through action at peripheral receptors in rats. Eur J Pharmacol. 2004 Nov 3;504(1-2):45-53. 3. Hansen RR, Nasser A, Falk S, et al. Chronic administration of the selective P2X3, P2X2/3 receptor antagonist, A-317491, transiently attenuates cancer-induced bone pain in mice. Eur J Pharmacol. 2012 Aug 5;688(1-3):27-34.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Neuronal Signaling Compound Library Bioactive Compounds Library Max Bioactive Compound Library NO PAINS Compound Library Anti-Cancer Compound Library Ion Channel Inhibitor Library

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Keywords

A-317491 475205-49-3 Membrane transporter/Ion channel Neuroscience P2X Receptor ABT 202 flux calcium Inhibitor neuropathic inhibit ABT202 P2X2/3 A317491 P2X3 ABT-202 P2XRs pain A 317491 inflammatory inhibitor

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