Ramatroban-d₄  (Synonyms: 雷马曲班-d₄; BAY u3405-d₄)

Ramatroban-d₄ is deuterium labeled Ramatroban. Ramatroban is a selective thromboxane A2 (TxA2, IC50=14 nM) antagonist, which also antagonizes CRTH2 (IC50=113 nM) by inhibiting PGD2 binding.

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

420.49

C₂₁H₁₇D₄FN₂O₄S

116649-85-5

雷马曲班-d₄

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.  [Content Brief]

  [2]. Stearns BA, et al. Novel tricyclic antagonists of the prostaglandin D₂ receptor DP2 with efficacy in a murine modelof allergic rhinitis. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4647-51.  [Content Brief]

  [3]. 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. 2003 Apr;305(1):347-52.  [Content Brief]

  [4]. Haba R, et al. Central CRTH2, a second prostaglandin D₂ receptor, mediates emotional impairment in the lipopolysaccharide and tumor-induced sickness behavior model. J Neurosci. 2014 Feb 12;34(7):2514-23.  [Content Brief]