Tafluprost acid-d4

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Tafluprost acid-d4 

Tafluprost acid-d4 是 Tafluprost acid 的氘代物。Tafluprost acid (AFP-172) 是 Tafluprost 的一种活性代谢形式,是一种选择性前列腺素 FP 受体 (prostanoid FP receptor) 激动剂。Tafluprost acid 对人前列腺素 FP 受体具有高亲和力,其 KiEC50 值分别为 0.4 nM 和0.53 nM。Tafluprost acid 对前列腺素 EP3 受体 ( prostanoid EP3 receptor IC50=67 nM) 的结合亲和性比前列腺素 FP 受体弱 126 倍。Tafluprost acid 可用于青光眼的研究。

Tafluprost acid-d4

Tafluprost acid-d4 Chemical Structure

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生物活性

Tafluprost acid-d4 is the deuterium labeled Tafluprost acid. Tafluprost acid (AFP-172), an active metabolic form of Tafluprost, is a selective prostanoid FP receptor agonist. Tafluprost acid shows a high affinity for human prostanoid FP receptor with Ki and EC50 values of 0.4 nM and 0.53 nM, respectively. Tafluprost acid has 126 times weaker binding affinity for prostanoid EP3 receptor (IC50=67 nM) than for the prostanoid FP receptor. Tafluprost acid can be used in the research of glaucoma[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

414.48

Formula

C22H24D4F2O5

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]. Takagi Y, et al. Pharmacological characteristics of AFP-168 (tafluprost), a new prostanoid FP receptor agonist, as an ocular hypotensive drug. Exp Eye Res. 2004 Apr;78(4):767-76.

    [3]. Taketani Y, et al. Activation of the prostanoid FP receptor inhibits adipogenesis leading to deepening of the upper eyelid sulcus in prostaglandin-associated periorbitopathy. Invest Ophthalmol Vis Sci. 2014 Mar 4;55(3):1269-76.

    [4]. Fuwa M, et al. Advantages of Efficacy and Safety of Fixed-Dose Tafluprost/Timolol Combination Over Fixed-Dose Latanoprost/Timolol Combination. PLoS One. 2016 Jul 6;11(7):e0158797.

    [5]. Roh YJ, et al. Effects of AFP-172 on COX-2-induced angiogenic activities on human umbilical vein endothelial cells. Graefes Arch Clin Exp Ophthalmol. 2012 Dec;250(12):1765-75.

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