300266 Sigma-AldrichDP2 Antagonist II - Calbiochem

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.

Revision	12-April-2013 JSW
Synonyms	(R)-(5-Chloro-1'-(5-chloro-2-fluorobenzyl)-2,2',5'-trioxospiro(indole-3,3→-pyrrolidin)-1(2H)-yl)acetic acid, CRTH2 Antagonist II, GPR44 Antagonist II
Description	The (R) enantiomer of 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 = 5.3 and 5.0 nM against 1.5 nM PGD2 for human & murine DP2 binding, respectively), exhibiting much reduced or little potency against a panel of more than 50 other receptors and ion channels, including PGD2 receptor DP1, PGE receptors (EP2, EP3, EP4), and PGF receptor FP (IC50 >30 µM). Effectively inhibits DP2-dependent chemotaxis of primary human eosinophils (IC50 = 100 nM; chemotractant = 100 nM DK-PGD2) in vitro. Shown to exhibit higher Caco-2 permeability than DP2 Antagonist I (Cat. No. 300264; Papp in unit of 10-6 cm/s = 26.4 vs. 5.2, respectively), but less oral bioavailability (32% in rat for Inhibitor II vs. 80% in mice for Inhibitor I with same oral dosage of 5 mg/kg).
Form	White powder
Intert gas (Yes/No)	Packaged under inert gas
Chemical formula	C₂₀H₁₃Cl₂FN₂O₅
Structure formula
Purity	≥93% by HPLC
Solubility	DMSO (100 mg/ml)
Storage	Protect from light +2°C to +8°C
Do Not Freeze	Yes
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity	Standard Handling
References	Crosignani, S., et al. 2008. J Med Chem. 51, 2227.