Pemetrexed-d5 disodium(Synonyms: LY231514-d5 disodium)

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Pemetrexed-d5 disodium (Synonyms: LY231514-d5 disodium)

Pemetrexed-d5 (LY231514-d5) disodium 是 Pemetrexed disodium 的氘代物。Pemetrexed disodium (LY231514 disodium) 是一种叶酸拮抗剂 (antifolate)。Pemetrexed disodium 抑制胸苷酸合成酶 (TS)，二氢叶酸还原酶 (DHFR) 和甘氨酰胺核苷酸甲酰转移酶 (GARFT) 的 Ki 分别为 1.3

Pemetrexed-d5 disodium(Synonyms: LY231514-d5 disodium)

Pemetrexed-d5 disodium Chemical Structure

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生物活性

Pemetrexed-d5 (LY231514-d5) disodium is the deuterium labeled Pemetrexed disodium. Pemetrexed disodium (LY231514 disodium) is an antifolate, the Kis of the pentaglutamate of Pemetrexed disodium are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively[1].

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

476.41

Formula

C20H14D5N5Na2O6
中文名称

培美曲塞二钠盐 d5 (双钠盐)
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]. Shih C, et al. LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes. Cancer Res. 1997 Mar 15;57(6):1116-23.

    [3]. Anraku M, et al. Synergistic antitumor effects of regulatory T cell blockade combined with pemetrexed in murine malignantmesothelioma. J Immunol. 2010 Jul 15;185(2):956-66.

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