Silodosin-d4(Synonyms: 西洛多辛 d4)

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Silodosin-d4 (Synonyms: 西洛多辛 d4)

Silodosin-d4 (KAD 3213-d4) 是 Silodosin 的氘代物。Silodosin (KAD 3213; KMD 3213) 是一个强效的、有选择性的、口服活性的 α1A-adrenergic receptor (α1A-AR) 阻滞剂。Silodosin 对 α1A-AR 表现出高度的亲和力 (Ki=0.036 nM)，是 α1B-AR 和 α1D-AR 亲和力的 162 和 50 倍，Ki 值分别为 21 nM 和 2.0 nM。Silodosin 是一种有效且耐受性良好的试剂，可用于 LUTS/BPH 的研究。

Silodosin-d4(Synonyms: 西洛多辛 d4)

Silodosin-d4 Chemical Structure

CAS No. : 1426173-86-5

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生物活性

Silodosin-d4 (KAD 3213-d4) is the deuterium labeled Silodosin. Silodosin (KAD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH[1][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

499.56

Formula

C25H28D4F3N3O4
CAS 号

1426173-86-5
中文名称

西洛多辛 d4
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]. Maxime Rossi , Silodosin in the treatment of benign prostatic hyperplasia. Drug Des Devel Ther. 2010; 4: 291–297.

    [3]. Villa L, et al. Effects by silodosin on the partially obstructed rat ureter in vivo and on human and rat isolated ureters.Br J Pharmacol. 2013 May;169(1):230-8.

    [4]. Osman NI, et al.Silodosin : a new subtype selective alpha-1 antagonist for the treatment of lower urinary tract symptoms in patients with benign prostatic hyperplasia.Expert Opin Pharmacother. 2012 Oct;13(14):2085-96.

    [5]. Kawahara T, et al. Silodosin inhibits the growth of bladder cancer cells and enhances the cytotoxic activity of cisplatin via ELK1 inactivation.Am J Cancer Res. 2015 Sep 15;5(10):2959-68. eCollection 2015.

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