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SAR247799
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SAR247799图片
CAS NO:1315311-14-8
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
S1P1 agonist 3
产品介绍
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-biasedsphingosine-1 phosphate receptor-1 (S1P1 )agonist, with EC50s 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[1][2][3][4].

IC50& Target[1]

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[1].
SAR247799 (0-10 μM, 8 min) induces impedance change in HUVECs in a dose-dependent manner[1].
SAR247799 (1 μM, 1st) does not cause desensitization demonstrated by Ca2+flux assay in S1P1-Chinese hamster ovary (CHO) cells[1].

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[1].
SAR247799 (0.3, 1, 3 mg/kg; i.v.) dose dependently increases the coronary conductance ratio in pig model of coronary endothelial dysfunction[1].
SAR247799 (30-min intravenous administration; 8- to 10-week-old farm pig) exposure (Cmaxand AUC) increases with dose in pigs. Pharmacokinetic parameters[1]:

Dose (mg/kg)NCmax(g/mL)Tmax(h)Tlast(h)AUC0-last(g.h/mL)Cl (L/h/kg)Vss (L/kg)T1/2z(h)
142.08 (8)0.5 [0.5][8-48]11.8 (46)0.113 (75)0.516 (11)5.62 (57)
378.10 (12)0.5 [0.5][24-72]42.2 (23)0.0754 (30)0.446 (16)6.21 (28)
10336.7 (5)0.5 [0.5-0.75]72294 (13)0.0343 (13)0.338 (7)7.73 (8)
306112 (27)0.5 [0.5- 1.0][48-72]908 (16)0.0338 (18)0.294 (11)7.35 (11)
Mean values with (CV%) except Tmax, which is expressed as median value with [range] and Tlast as [range]. Cmax, maximum concentration. Tmax, time at which maximum concentration achieved. Tlast, last time point sampled. AUC0-last, area under curve from 0 to last time point. Cl, clearance. Vss, volume at steady state or volume of distribution. T1/2z, elimination half-life. N, number of animals.

Animal Model:Acute kidney injury rats (12 to 15-week-old Fischer rats)[1]
Dosage:1 and 3 mg/kg
Administration:P.o.; administered 1 hour before renal occlusion.
Result:Inhibited the increase in serum creatinine (89 and 96% at 1 and 3 mg/kg) and urea (61 and 85% at 1 and 3 mg/kg).
Protected renal proximal tubules against necrosis and blunted the development of interstitial hemorrhage.
Animal Model:Acute kidney injury rats (8- to 12-week-old Fischer rats)[1]
Dosage:3 mg/kg
Administration:P.o.; twice a day for 7 days and twice a day for 7 day
Result:Showed a dosedependent trend for reducing macrophage.
Clinical Trial
分子量

425.82

性状

Solid

Formula

C21H16ClN3O5

CAS 号

1315311-14-8

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)

溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL(78.27 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.3484 mL11.7421 mL23.4841 mL
5 mM0.4697 mL2.3484 mL4.6968 mL
10 mM0.2348 mL1.1742 mL2.3484 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。