SAR247799|1315311-14-8|(S1P1 agonist 3)-陌孚医药/Medlife

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SAR247799 (Synonyms: S1P1 agonist 3)

目录号: PL06760 纯度: ≥97%

CAS No. :1315311-14-8

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PL06760-50mg	50mg	询价	询价
PL06760-100mg	100mg	询价	询价

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中文名称	SAR247799
中文别名	SAR247799
英文名称	SAR247799
英文别名	Acetic acid, 2-[4-[5-(3-chlorophenoxy)oxazolo[5,4-d]pyrimidin-2-yl]-2,6-dimethylphenoxy]-;S1P1 agonist 3
Cas No.	1315311-14-8
分子式	C₂₁H₁₆ClN₃O₅
分子量	425.82
包装储存	4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

产品详情

SAR247799 (S1P1 agonist 3) 是一种具有口服活性的，选择性 G 蛋白偏向的鞘氨醇-1 磷酸受体-1 (S1P1) 激动剂，在 S1P1 过表达细胞和 HUVEC 中的 EC₅₀ 为 12.6-493 nM。SAR247799 可用于内皮保护的研究，包括 2 型糖尿病、代谢综合征。

生物活性

SAR247799 (S1P1 agonist 3) is an oral activity, selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist, with EC 50 s rang from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 can be used for the research of endothelial protection, including type-2 diabetes, metabolic syndrome.

性状

Solid

IC50 & Target[1][2]

S1PR1 12.6-493 nM (EC50)

体外研究(In Vitro)

SAR247799 (0, 0.003, 0.01, 0.03, 0.1, 0.3, 1, 3, 10 μM; 10 min) induces a concentration-dependent phosphorylation of extracellular-regulated kinase-1/2 (Erk1/2) and protein kinase B (Akt) in HUVECs.
SAR247799 (0-10 μM, 8 min) induces impedance change in HUVECs in a dose-dependent manner.
SAR247799 (1 μM, 1st) does not cause desensitization demonstrated by Ca flux assay in S1P1-Chinese hamster ovary (CHO) cells. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

SAR247799 (1 and 3 mg/kg; p.o.; 1 h before renal occlusion) dose dependently reduces the severity of ischemia/reperfusion (I/R)–induced acute kidney injury.
SAR247799 (0.3, 1, 3 mg/kg; i.v.) dose dependently increases the coronary conductance ratio in pig model of coronary endothelial dysfunction.
SAR247799 (30-min intravenous administration; 8- to 10-week-old farm pig) exposure (C max and AUC) increases with dose in pigs. Pharmacokinetic parameters :
Dose (mg/kg)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

ClinicalTrial

参考文献

[1]. Poirier B, et al. A G protein-biased S1P1 agonist, SAR247799, protects endothelial cells without affecting lymphocyte numbers. Sci Signal. 2020 Jun 2;13(634):eaax8050.
[2]. Evaristi MF, et al. A G-protein-biased S1P1 agonist, SAR247799, improved LVH and diastolic function in a rat model of metabolic syndrome. PLoS One. 2022 Jan 14;17(1):e0257929.

溶解度数据	In Vitro: DMSO : 33.33 mg/mL (78.27 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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