[CAS NO. 475205-49-3]  A-317491

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PRODUCTS SPECIFICATIONS [475205-49-3]

Catalog
SLK-S8519
Brand
Selleck
CAS
475205-49-3

DESCRIPTION [475205-49-3]

Overview

MDLMFCD28044314
Molecular Weight565.57
Molecular FormulaC33H27NO8
SMILESO=C(C1=CC(C(N(CC2=CC=CC(OC3=CC=CC=C3)=C2)[C@H]4CCCC5=C4C=CC=C5)=O)=C(C(O)=O)C=C1C(O)=O)O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM1.7681 mL8.8406 mL17.6813 mL
5 mM0.3536 mL1.7681 mL3.5363 mL
10 mM0.1768 mL0.8841 mL1.7681 mL
50 mM0.0354 mL0.1768 mL0.3536 mL

Description

A-317491 is a novel potent and selective non-nucleotide antagonist of and receptors with Ki values of 22 nM and 9 nM for human and receptors.

Targets

Human P2X2/3 [1]
(Cell-free assay)
Human P2X3 [1]
(Cell-free assay)
Rat P2X3 [1]
(Cell-free assay)
Rat P2X2/3 [1]
(Cell-free assay)
9 nM(Ki)22 nM(Ki)22 nM(Ki)92 nM(Ki)

In vitro

A-317491 potently 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 neurotransmitter receptors, ion channels, and enzymes. A-317491 does not undergo any detectable metabolism (oxidation or glucuronidation) in in vitro assays using human and rat liver microsomes.

In vivo

A-317491 dose-dependently (ED50 = 30 μmol/kg s.c.) reduces complete Freund's adjuvant-induced thermal hyperalgesia in the rat. A-317491 is most potent (ED50 = 10-15 μmol/kg s.c.) in attenuating both thermal hyperalgesia and mechanical allodynia after chronic nerve constriction injury. Although active in chronic pain models, A-317491 is ineffective (ED50 >100 μmol/kg s.c.) in reducing nociception in animal models of acute pain, postoperative pain, and visceral pain. Preliminary pharmacokinetic studies in rats indicate that 10 μmol/kg A-317491 had high (≈80%) systemic bioavailability after s.c. dosing (estimated plasma concentration = 15 μg/ml, >99% protein bound) and a half-life in plasma of 11 h. A-317491 is effective in reducing pain associated behavior in several animal models of inflammatory and neuropathic pain when administered systemically. A-317491 does not significantly penetrate into the CNS.