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500486 CXCR3 Antagonist - Calbiochem

500486
  
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Přehled

Replacement Information

Tabulka spec. kláve

Empirical Formula
C₂₂H₁₆F₂N6O₂S
Description
OverviewAn arylsulfonamide derivative that acts as a CXCR3 antagonist (IC50 = 192 nM against CXCL10-induced chemotaxis of hCXCR3-overexpressing L1.2 cells) with good aqueous solubility (>100 µM at pH 7.4). Shown to be orally available in mice (83% bioavailability; t1/2 = 1 h; 10 mg/kg p.o.) in vivo and display a medium intrinsic clearance (CIint = 17 µL/min/mg) in in vitro mouse liver microsome stability test.

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number500486
Brand Family Calbiochem®
Synonyms4-cyano-N-(3-fluoro-4-(1H-tetrazol-5-yl)benzyl)-N-(2-fluorobenzyl)benzenesulfonamide, AS612568, EMD1205395, CD183 Antagonist, GPR9 Antagonist
References
ReferencesCrosignani, S., et al. 2010. Bioorg. Med. Chem. Lett. 20, 3614.
Product Information
FormYellow solid
Hill FormulaC₂₂H₁₆F₂N6O₂S
Chemical formulaC₂₂H₁₆F₂N6O₂S
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetCXCR3
Primary Target IC<sub>50</sub>192 nM
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
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
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Katalogové číslo GTIN
500486 0

Documentation

CXCR3 Antagonist - Calbiochem MSDS

Title

Safety Data Sheet (SDS) 

References

Přehled odkazů
Crosignani, S., et al. 2010. Bioorg. Med. Chem. Lett. 20, 3614.
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.

Revision21-November-2014 JSW
Synonyms4-cyano-N-(3-fluoro-4-(1H-tetrazol-5-yl)benzyl)-N-(2-fluorobenzyl)benzenesulfonamide, AS612568, EMD1205395, CD183 Antagonist, GPR9 Antagonist
DescriptionAn arylsulfonamide derivative that acts as a CXCR3 antagonist (IC50 = 192 nM against CXCL10-induced chemotaxis of hCXCR3-overexpressing L1.2 cells) with good aqueous solubility (>100 µM at pH 7.4). Shown to be orally available in mice (83% bioavailability; t1/2 = 1 h; 10 mg/kg p.o.) in vivo and display a medium intrinsic clearance (CIint = 17 µL/min/mg) in in vitro mouse liver microsome stability test.
FormYellow solid
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₂H₁₆F₂N6O₂S
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (50 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
ReferencesCrosignani, S., et al. 2010. Bioorg. Med. Chem. Lett. 20, 3614.