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SAR247799

CAS No. : 1315311-14-8

MCE 站：SAR247799

产品活性：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。

研究领域：GPCR/G Protein

作用靶点：LPL Receptor

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 Ca²⁺ flux assay in S1P1-Chinese hamster ovary (CHO) cells.

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)	N	Cmax (g/mL)	Tmax (h)	Tlast (h)	AUC0-last (g.h/mL)	Cl (L/h/kg)	Vss (L/kg)	T1/2z (h)
1	4	2.08 (8)	0.5 [0.5]	[8-48]	11.8 (46)	0.113 (75)	0.516 (11)	5.62 (57)
3	7	8.10 (12)	0.5 [0.5]	[24-72]	42.2 (23)	0.0754 (30)	0.446 (16)	6.21 (28)
10	3	36.7 (5)	0.5 [0.5-0.75]	72	294 (13)	0.0343 (13)	0.338 (7)	7.73 (8)
30	6	112 (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 T_max, which is expressed as median value with [range] ａnd Tlast as [range]. C_max, maximum concentration. T_max, time at which maximum concentration achieved. T_last, last time point sampled. AUC_0-last, area under curve from 0 to last time point. Cl, clearance. Vss, volume at steady state or volume of distribution. T_1/2z, elimination half-life. N, number of animals.

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