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505478 A317491 - CAS 475205-49-3 - Calbiochem

505478
  
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
475205-49-3C₃₃H₂₇NO₈•xH2O•xNa
Description
Overview

This product has been discontinued.



A potent, selective, and competitive non-nucleotide antagonist of P2X3 and P2X2/3 receptors that blocks receptor-mediated Ca2+ flux (Ki = 22 and 92 nM for rat P2X3 and P2X2/3 receptor and 22 and 9 nM for human P2X3 and P2X2/3 receptor, respectively). Its R-enantiomer has significantly reduced activity at these receptors. Exhibits high selectivity over other purinergic receptors. Shown to reduce thermal and mechanical hyperalgesia in rat models (ED50 = 10-15 µM/kg, s.c). Its anti-nociceptive effects have a rapid on-set and persist for up to 5 hours after sub-cutaneous administration. Also shown to block dorsal root ganglion currents in a dose-dependent manner (IC50 = 15 nM).

Catalogue Number505478
Brand Family Calbiochem®
Synonyms(S)-5-((3-phenoxybenzyl)(1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)benzene-1,2,4-tricarboxylic acid, P2X3 Purinergic Receptors Antagonist, A317491, P2X2/3 Purinergic Receptors Antagonist, A317491, A 317491
References
ReferencesJarvis, MF. et al. 2002. Proc. Natl. Acad. Sci. USA 99, 17179.
Product Information
CAS number475205-49-3
FormWhite powder
Hill FormulaC₃₃H₂₇NO₈•xH2O•xNa
Chemical formulaC₃₃H₂₇NO₈•xH2O•xNa
Hygroscopic Hygroscopic
Structure formula ImageStructure formula Image
Applications
Biological Information
Primary TargetP2X3
Primary Target K<sub>i</sub>22nM
Purity≥99% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
505478 0

Documentation

A317491 - CAS 475205-49-3 - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Jarvis, MF. et al. 2002. Proc. Natl. Acad. Sci. USA 99, 17179.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision30-August-2013 JSW
Synonyms(S)-5-((3-phenoxybenzyl)(1,2,3,4-tetrahydronaphthalen-1-yl)carbamoyl)benzene-1,2,4-tricarboxylic acid, P2X3 Purinergic Receptors Antagonist, A317491, P2X2/3 Purinergic Receptors Antagonist, A317491, A 317491
DescriptionA potent, selective, and competitive non-nucleotide antagonist of P2X3 and P2X2/3 receptors that blocks receptor-mediated Ca2+ flux (Ki = 22 and 92 nM for rat P2X3 and P2X2/3 receptor and 22 and 9 nM for human P2X3 and P2X2/3 receptor, respectively). Its R-enantiomer has significantly reduced activity at these receptors. Exhibits high selectivity over other purinergic receptors. Shown to reduce thermal and mechanical hyperalgesia in rat models (ED50 = 10-15 µM/kg, s.c). Its anti-nociceptive effects have a rapid on-set and persist for up to 5 hours after sub-cutaneous administration. Also shown to block dorsal root ganglion currents in a dose-dependent manner (IC50 = 15 nM).
FormWhite powder
CAS number475205-49-3
Chemical formulaC₃₃H₂₇NO₈•xH2O•xNa
Structure formulaStructure formula
Purity≥99% by HPLC
SolubilityH₂O (50 mg/ml)
Storage Protect from light
-20°C
Hygroscopic
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesJarvis, MF. et al. 2002. Proc. Natl. Acad. Sci. USA 99, 17179.