MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

SAR247799

CAS No. : 1315311-14-8

MCE 国际站：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.

相关产品：Fingolimod hydrochloride | PF-543 Citrate | Siponimod | Ozanimod | JTE-013 | BMS-986020 | Ki16425 | Sphingosine-1-phosphate | TY-52156 | AM095 | Etrasimod | Ponesimod | SEW2871 | 1-Oleoyl lysophosphatidic acid | AS2717638 | CYM-5541 | LPA2 antagonist 1 | Cenerimod | FTY720 (S)-Phosphate | AM966 | Ceranib-2 | CYM50308 | Amiselimod hydrochloride | CYM50260 | GSK2018682 | ONO⁻⁷300243 | TAK-615 | ASP6432

热门产品线：重组蛋白 | 化合物库 | 天然产物 | 染料试剂 | PROTAC | 同位素标记物

Trending products：Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Dye Reagents | PROTAC | Isotope-Labeled Compounds

品牌介绍:
• MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供最新最全的高品质小分子活性化合物；
• 10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
• 设有专业的实验中心和严格的质控、验证体系；
• 提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
• 产品的生物活性多经各国客户实验验证；
• Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
• 专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
• 与世界各大制药公司及知名科研机构建立了长期的合作。