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505418 AF353 - CAS 927887-18-1 - Calbiochem

505418
  
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
927887-18-1C₁₄H₁₈ClIN₄O₂
Description
OverviewA novel, potent, orally bioavailable antagonist of P2X3/P2X2/3 receptors (pIC50 = 8 in human and rat; pIC50 = 7.3 for human P2X2/3 receptor). Shown to be highly brain penetrant with a brain to plasma ratio of 6. Blocks agonist-evoked intracellular Ca2+ flux and inward currents in nanomolar range (10 nM to 1 µM) in cell lines recombinantly expressing human P2X3 and P2X2/3 receptors. Exhibits desirable pharmacokinetic properties (t1/2 = 1.63 h and Tmax = 30 min).
Catalogue Number505418
Brand Family Calbiochem®
SynonymsP2X3 Purinergic Receptor Antagonist, AF353, P2X2/3 Purinergic Receptor Antagonist, AF353
Application Data
References
ReferencesGever, J. R., et al. 2010. Br. J. Pharmacol. 160, 1387.
Product Information
CAS number927887-18-1
FormLight brown powder
Hill FormulaC₁₄H₁₈ClIN₄O₂
Chemical formulaC₁₄H₁₈ClIN₄O₂
ReversibleY
Applications
Biological Information
Primary TargetP2X3
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 +2°C to +8°C
Protect from Light Protect from light
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 Identification Number
Catalog Number GTIN
505418

Documentation

AF353 - CAS 927887-18-1 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Gever, J. R., et al. 2010. Br. J. Pharmacol. 160, 1387.
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
SynonymsP2X3 Purinergic Receptor Antagonist, AF353, P2X2/3 Purinergic Receptor Antagonist, AF353
Application Data
DescriptionA novel, potent, orally bioavailable antagonist of P2X3/P2X2/3 receptors (pIC50 = 8 in human and rat; pIC50 = 7.3 for human P2X2/3 receptor). Shown to be highly brain penetrant with a brain to plasma ratio of 6. Blocks agonist-evoked intracellular Ca2+ flux and inward currents in nanomolar range (10 nM to 1 µM) in cell lines recombinantly expressing human P2X3 and P2X2/3 receptors. Exhibits desirable pharmacokinetic properties (t1/2 = 1.63 h and Tmax = 30 min).
FormLight brown powder
CAS number927887-18-1
Chemical formulaC₁₄H₁₈ClIN₄O₂
Purity≥99% by HPLC
SolubilityDMSO (10 mg/ml)
Storage Protect from light
+2°C to +8°C
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
ReferencesGever, J. R., et al. 2010. Br. J. Pharmacol. 160, 1387.