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RP101988 Sale

目录号 : GC65324

RP101442 是 Ozanimod 的主要的活性代谢物,是一种选择性强的 S1PR1 激动剂,对 S1PR1 和 S1P5R 的 EC50 分别为 0.19 nM 和 32.8 nM。

RP101988 Chemical Structure

规格 价格 库存 购买数量
5mg
¥3,600.00
现货
10mg
¥6,120.00
现货
25mg
¥12,150.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

S1PR1

0.19nM(EC50)

S1PR5

32.8nM(EC50)

产品描述

RP101988, the major active metabolite of Ozanimod, is a selective, potent S1PR1 (sphingosine-1-phosphate receptor 1) agonist, with EC50s of 0.19 nM and 32.8 nM for S1PR1 and S1PR5, respectivlely[1].

RP101988 is a substrate of P-gp and breast cancer resistance protein (BCRP) drug transporters[2].

[1]. Tran JQ, et al. Cardiac Safety of Ozanimod, a Novel Sphingosine-1-Phosphate Receptor Modulator: Results of a Thorough QT/QTc Study. Clin Pharmacol Drug Dev. 2018;7(3):263-276.
[2]. Gilardi D, et al. PK, PD, and interactions: the new scenario with JAK inhibitors and S1P receptor modulators, two classes of small molecule drugs, in IBD [published online ahead of print, 2020 Jul 1]. Expert Rev Gastroenterol Hepatol. 2020;1-10.

Chemical Properties

Cas No. SDF Download SDF
分子式 C23H22N4O4 分子量 418.45
溶解度 DMSO : 125 mg/mL (298.72 mM; Need ultrasonic) 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.3898 mL 11.9489 mL 23.8977 mL
5 mM 0.478 mL 2.3898 mL 4.7795 mL
10 mM 0.239 mL 1.1949 mL 2.3898 mL
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Research Update

Effects of High- and Low-Fat Meals on the Pharmacokinetics of Ozanimod, a Novel Sphingosine-1-Phosphate Receptor Modulator

Clin Pharmacol Drug Dev 2018 Aug;7(6):634-640.PMID:29125718DOI:PMC6099448

Ozanimod (RPC1063) is an oral selective modulator of the sphingosine-1-phosphate 1 and 5 receptors under development for the treatment of relapsing multiple sclerosis and inflammatory bowel disease. The effects of high-fat and low-fat meals on the pharmacokinetics (PK) of a single oral dose of ozanimod were evaluated in 24 healthy volunteers in a randomized, open-label crossover trial. Each subject received a 1-mg dose of ozanimod hydrochloride under 3 meal conditions (fasted, high-fat, and low-fat), each separated by 7 days. Mean plasma concentration-time profiles for ozanimod and its active metabolites (RP101988 [major], RP101075 [minor]) were similar under all 3 conditions. Moreover, all PK parameters for ozanimod, RP101988, and RP101075 were similar under the 3 meal conditions. The 90% confidence intervals (CIs) for the ratios of geometric least-squares mean (fed/fasted) were within the equivalence limits of 0.80 to 1.25 for area under the concentration-time curve from time 0 to infinity (AUC0-∞ ) and maximum plasma concentration (Cmax ) for ozanimod, RP101988, and RP101075, except for the high-fat effect on RP101075 Cmax (90%CI, 0.76-0.88). Given this lack of a food effect on the exposure of ozanimod and its active metabolites, ozanimod can be taken without regard to meals.