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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

CAY10471

Cayman Chemical Item Number 10006735

(CAS 627865-18-3)

CAY10471 (CAS 627865-18-3)

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Description

The biological effects of prostaglandin D2 are transduced by at least two 7-transmembrane G-protein coupled receptors, designated DP1 and CRTH2/DP2. BAY-u3405 (Ramatroban) is an approved human medication for the treatment of allergic rhinitis that has documented activity as an antagonist of both the TP and CRTH2/DP2 receptors.1,2 CAY10471 is an analog of BAY-u3405 which contains modifications that increase both its potency and selectivity for the human CRTH2/DP2 receptor.3 CAY10471 binds to the human CRTH2/DP2, DP1, and TP receptors with Ki values of 0.6, 1200, and >10,000 nM, respectively.3

1 Sugimoto, H., Shichijo, M., Iino, T., et al. An orally bioavailable small molecule antagonist of CRTH2, Ramatroban (BAY u3405), inhibits prostaglandin D2-induced eosinophil migration in vitro. J Pharmacol Exp Ther 305 347-352 (2003).

2 McKenniff, M.G., Norman, P., Cuthbert, N.J., et al. BAY u3405, a potent and selective thromboxane A2 receptor antagonist on airway smooth muscle in vitro.. Br J Pharmacol 104(3) 585-590 (1991).

3 Ulven, T., and Kostenis, E. Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. J Med Chem 48(4) 897-900 (2005).

Formal Name (+)-​3-​[[(4-​fluorophenyl)sulfonyl]methylamino]-​1,​2,​3,​4-​tetrahydro-​9H-​carbazole-​9-​acetic acid
CAS Number 627865-18-3
Molecular Formula C21H21FN2O4S
Formula Weight 416.5
Formulation A crystalline solid
Purity ≥98%
λmax 227, 284 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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CN(S(C1=CC=C(F)​C=C1)​(=O)​=O)​C(CC2)​CC3=C2N(CC(O)​=O)​C4=CC=CC=C43

Background Reading

Sugimoto, H., Shichijo, M., Iino, T., et al. An orally bioavailable small molecule antagonist of CRTH2, Ramatroban (BAY u3405), inhibits prostaglandin D2-induced eosinophil migration in vitro. J Pharmacol Exp Ther 305 347-352 (2003).

McKenniff, M.G., Norman, P., Cuthbert, N.J., et al. BAY u3405, a potent and selective thromboxane A2 receptor antagonist on airway smooth muscle in vitro.. Br J Pharmacol 104(3) 585-590 (1991).

Ulven, T., and Kostenis, E. Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. J Med Chem 48(4) 897-900 (2005).

CAY10471 is available in the following screening library:

Size Price Quantity Subtotal
1 mg $54.00 $0.00
5 mg $243.00 $0.00
10 mg $432.00 $0.00
50 mg $1,890.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

Please contact our Sales Department for a quote or to purchase.

Pricing updated 2012-02-12. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

Related Products

BAY-u3405
BW A868C
CAY10648 Exclusive

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