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R-7966 Ramatroban, Free Acid, >99% Prices Reduced (June 2010)

[Baynas] [BAY u3405]

R-7966PR

Note: Our Euro, Pound, and Yen prices are revised regularly to account for currency exchange rate fluctuations.

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M.W. 416.47

C₂₁H₂₁FN₂O₄S

[116649-85-5]

M.I. 14: 8100

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO. Disposal: A

Ramatroban showed significant inhibitory effects on the binding of 3H-labeled PGD2 to the CRTH2 receptor, with IC50 of 100 nM. Ramatroban inhibited PGD2-induced Ca2+ mobilization in CRTH2 transfectants with an IC50 of 30 nM and inhibited the PGD2-induced migration of eosinophils concentration-dependently (IC50 = 170 nM). Sugimoto, H., 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).

Ramatroban reduced peribronchial eosinophilia and mucus cell hyperplasia and thus reduced symptoms of asthma. Uller, L., et al. "Antagonism of the prostaglandin D2 receptor CRTH2 attenuates asthma pathology in mouse eosinophilic airway inflammation." Respir. Res. 8: 16 (2007).

Ramatroban blocked the action of 8-iso-prostaglandin F2α and improved the vascular response to acetylcholine in hypercholesterolemic rabbits. Ishizuka, T., et al. "Ramatroban, a TP receptor antagonist, improves vascular responses to acetylcholine in hypercholesterolemic rabbits in vivo." Eur. J. Pharmacol. 468: 27-35 (2003).

Ramatroban had anti-ischemic and antivasoconstrictor properties in vivo, apparently by binding to platelet and smooth muscle thromboxane receptors. Fiedler, V.B., et al. "Effects of the novel thromboxane antagonist Bay U 3405 on experimental coronary artery disease." Stroke 21: IV149-151 (1990).

Ramatroban is the active ingredient in the drug sold in Japan under the trade name Baynas®. This drug has been approved in at least one country for use in patients with coronary artery disease and asthma. NOTE: The ramatroban product sold by LC Laboratories is NOT Baynas® and is NOT for human use.

Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.

This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

Not available in some countries; not available to some institutions; not available for some uses.

(R)-Ramatroban, Free Acid