PSB-12379 disodium

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PSB-12379 disodium 

PSB-12379 disodium 是一种核苷类似物，是一种有效的 Ecto-5′-Nucleotidase (CD73) 抑制剂，Kis 值为 9.03 nM (鼠) 和 2.21 nM (人)。

PSB-12379 disodium

PSB-12379 disodium Chemical Structure

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PSB-12379 disodium 的其他形式现货产品:

PSB-12379

生物活性

PSB-12379 disodium, a nucleotide analogue, is a potent Ecto-5′-Nucleotidase (CD73) inhibitor with Kis of 9.03 nM (rat) and 2.21 nM (human)[1][2].

IC50 & Target

Ki: 9.03 nM (rat), 2.21 nM (human) (Ecto-5’-Nucleotidase)[1].
体内研究
(In Vivo)

Metabolism: Only a small percentage (<23%) of PSB-12379 (10g) is metabolized under the applied conditions, while >77% of the compounds are recovered unchanged after a long incubation for 8 h. PSB-12379 (10g) is somewhat less stable, and 56% are metabolized within 8 h. Hydrolytic cleavage of the glycosidic bond, which is a typical phase I reaction of nucleosides and nucleotides, was observed as the main reaction[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

559.31

Formula

C18H21N5Na2O9P2
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]. Bhattarai S, et al. α,β-Methylene-ADP (AOPCP) Derivatives and Analogues: Development of Potent and Selective ecto-5′-Nucleotidase (CD73) Inhibitors. J Med Chem. 2015 Aug 13;58(15):6248-63.

    [2]. X-Ray Co-Crystal Structure Guides the Way to Subnanomolar Competitive Ecto-5 -Nucleotidase (CD73) Inhibitors for Cancer Immunotherapy Sanjay Bhattarai. Adv. Therap. 2019, 2, 1900075.

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