2. GPCR/G Protein
  3. LPL Receptor
  4. SAR247799

SAR247799  (Synonyms: S1P1 agonist 3)

目录号: HY-115831 纯度: 97.21%
COA 产品使用指南

摩尔计算器

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。

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SAR247799 Chemical Structure

SAR247799 Chemical Structure

CAS No. : 1315311-14-8

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规格 价格 是否有货 数量
1 mg ￥2181
In-stock
5 mg ￥4800
In-stock
10 mg ￥8000
In-stock
50 mg   询价  
100 mg   询价  

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Customer Review

SAR247799 相关抗体

Top Publications Citing Use of Products

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LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SAR247799 相关抗体:
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 (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)
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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

Formula

C21H16ClN3O5
CAS 号
性状

固体

颜色

Off-white to light yellow

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 中的溶解度 : 33.33 mg/mL (78.27 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

SAR247799 相关分类

完整储备液配制表

* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3484 mL 11.7421 mL 23.4841 mL 58.7103 mL
5 mM 0.4697 mL 2.3484 mL 4.6968 mL 11.7421 mL
10 mM 0.2348 mL 1.1742 mL 2.3484 mL 5.8710 mL
15 mM 0.1566 mL 0.7828 mL 1.5656 mL 3.9140 mL
20 mM 0.1174 mL 0.5871 mL 1.1742 mL 2.9355 mL
25 mM 0.0939 mL 0.4697 mL 0.9394 mL 2.3484 mL
30 mM 0.0783 mL 0.3914 mL 0.7828 mL 1.9570 mL
40 mM 0.0587 mL 0.2936 mL 0.5871 mL 1.4678 mL
50 mM 0.0470 mL 0.2348 mL 0.4697 mL 1.1742 mL
60 mM 0.0391 mL 0.1957 mL 0.3914 mL 0.9785 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SAR2477991315311-14-8S1P1 agonist 3SAR 247799SAR-247799LPL ReceptorLysophospholipid Receptortype-2 diabetesmetabolic syndromeendothelial protectionHUVECspigratInhibitorinhibitorinhibit

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目录号：
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