Sarpogrelate-d3 hydrochloride(Synonyms: MCI-9042-d3)

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Sarpogrelate-d3 hydrochloride (Synonyms: MCI-9042-d3)

Sarpogrelate-d3 hydrochloride (MCI-9042-d3) 是 Sarpogrelate hydrochloride 的氘代物。Sarpogrelate hydrochloride (MCI-9042) 是一种选择性的 5-HT2R 拮抗剂，对 5-HT2A，5-HT2B，和 5-HT2C 受体的 pKi 值分别为 8.52、6.57 和 7

Sarpogrelate-d3 hydrochloride(Synonyms: MCI-9042-d3)

Sarpogrelate-d3 hydrochloride Chemical Structure

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生物活性

Sarpogrelate-d3 hydrochloride (MCI-9042-d3) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2– and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3].

体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

468.99

Formula

C24H29D3ClNO6
中文名称

盐酸沙格雷酯 d3 (盐酸盐)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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

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

    [2]. Rashid M, et, al. Identification of the binding sites and selectivity of sarpogrelate, a novel 5-HT2 antagonist, to human 5-HT2A, 5-HT2B and 5-HT2C receptor subtypes by molecular modeling. Life Sci. 2003 May 30;73(2):193-207.

    [3]. Maruyama K, et, al. MCI-9042: high affinity for serotonergic receptors as assessed by radioligand binding assay. J Pharmacobiodyn. 1991 Apr;14(4):177-81.

    [4]. Kataoka H, et, al. Inhibitory Effect of Serotonin Antagonist on Leukocyte-Endothelial Interactions In Vivo and In Vitro. PLoS One. 2016 Jan 29;11(1):e0147929.

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