SAR247799
(Synonyms: S1P1 agonist 3) 目录号 : GC65910
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。
Cas No.:1315311-14-8
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
SAR247799 (S1P1 agonist 3) is an oral activity, selective G-protein-biased sphingosine-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].
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].
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 (Cmax and AUC) increases with dose in pigs. Pharmacokinetic parameters [1]:
| 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) |
| 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. |
| Cas No. | 1315311-14-8 | SDF | Download SDF |
| 别名 | S1P1 agonist 3 | ||
| 分子式 | C21H16ClN3O5 | 分子量 | 425.82 |
| 溶解度 | DMSO : 33.33 mg/mL (78.27 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 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°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。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3484 mL | 11.7421 mL | 23.4841 mL |
| 5 mM | 0.4697 mL | 2.3484 mL | 4.6968 mL |
| 10 mM | 0.2348 mL | 1.1742 mL | 2.3484 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet