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DP2 Antagonist I
(4-Chloro-2-((2-methyl-5-(propylsulfonyl)phenyl)ethynyl)phenoxy)acetic Acid, CRTH2 Antagonist I, GPR44 Antagonist I
A 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.
产品信息
Form White powder
Primary Target DP2
Primary Target Ki 2 nM
Molar mass 406.88
Protect from Light 是的
Packaged under inert gas 是的
Cell permeable 是的
Reversible 是的
Purity ≥98% by HPLC
Solubility DMSO
商店和运输信息
Storage +2°C to +8°C
Ship Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Standard Handling |