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300264 DP2 Antagonist I - Calbiochem

300264
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Descripción

Replacement Information

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Número de referenciaEmbalaje Cant./Env.
300264-2MG Frasco de vidrio 2 mg
Description
OverviewA cell-permeable alkynylphenoxyacetic acid that acts as a high affinity antagonist against the G protein-coupled PGD2 (Cat. No. 538909) receptor CRTH2/DP2 (Ki = 2.0 and 2.4 nM against 1.5 nM PGD2 for human & murine DP2 binding, respectively), exhibiting much reduced potency against DP1 (Ki = 1.58 µM; IC50 = 10 µM), PGE receptor EP2 (54% inhibition at 10 µM), and little or no activity toward 49 other receptors and ion channels. Effectively inhibits PGD2-induced cellular activation (IC50 = 32 and 80 nM, respectively, using CHO-CRTH2 or human whole blood) in vitro and is efficacious in alleviating airway eosinophil infiltration in OVA- (Cat. No. 32467) sensitized mice (30 mg/kg; p.o.) in vivo with good oral bioavailability.
Catalogue Number300264
Brand Family Calbiochem®
Synonyms(4-Chloro-2-((2-methyl-5-(propylsulfonyl)phenyl)ethynyl)phenoxy)acetic Acid, CRTH2 Antagonist I, GPR44 Antagonist I
References
ReferencesCrosignani, S., et al. 2011. J Med Chem. 54, 7299.
Product Information
FormWhite powder
Hill FormulaC₂₀H₁₉ClO₅S
Chemical formulaC₂₀H₁₉ClO₅S
ReversibleY
Structure formula ImageStructure formula Image
Applications
Biological Information
Primary TargetDP2
Primary Target K<sub>i</sub>2 nM
Purity≥98% 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

Documentation

Referencias bibliográficas

Visión general referencias
Crosignani, S., et al. 2011. J Med Chem. 54, 7299.
Ficha técnica

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.

Revision19-March-2013 JSW
Synonyms(4-Chloro-2-((2-methyl-5-(propylsulfonyl)phenyl)ethynyl)phenoxy)acetic Acid, CRTH2 Antagonist I, GPR44 Antagonist I
DescriptionA cell-permeable alkynylphenoxyacetic acid that acts as a high affinity antagonist against the G protein-coupled PGD2 (Cat. No. 538909) receptor CRTH2/DP2 (Ki = 2.0 and 2.4 nM against 1.5 nM PGD2 for human & murine DP2 binding, respectively), inhibiting AR (aldose reductase) only at higher concentrations (IC50 = 172 nM) and exhibiting much reduced potency against PGD2 receptor DP1 (Ki = 1.58 µM; IC50 = 10 µM), PGE receptor EP2 (54% binding inhibition at 10 µM), and little or no activity toward 49 other receptors and ion channels (IC50 >10 µM). Effectively inhibits PGD2-induced cellular activation (IC50 = 32 and 80 nM, respectively, using CHO-CRTH2 or human whole blood) in vitro and is efficacious in alleviating airway eosinophil infiltration in OVA- (Cat. No. 32467) sensitized mice (3.1- and 5.8-fold of control, respectively, with or without 30 mg/kg oral dosages 1 h before and 7 h after each of three daily 30-min OVA aerosol challenges) in vivo with good oral bioavailability (t1/2 = 3.9; AUC = 3730 ng·h/mL; 5 mg/kg p.o.).
FormWhite powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₂₀H₁₉ClO₅S
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (100 mg/ml)
Storage +2°C to +8°C
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.
Toxicity Standard Handling
ReferencesCrosignani, S., et al. 2011. J Med Chem. 54, 7299.