|3-(4-氯苯基)-N-((4-氯苯基)磺酰基)-N'-甲基-4-苯基-4,5-二氢-1H-吡唑-1-酰胺|CsnPharm

CAS No.: 362519-49-1

(±)-Ibipinabant Catalog No. CSN21999

Synonyms: (±)-SLV319;(±)-BMS-646256;SLV319

(±)-SLV319 is a selective antagonist of cannabinoid-1 (CB1) receptor with Ki value of 7.8 nM and it has a weaker activation effect on CB2.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The endocannabinoid system, comprised of the cannabinoid receptors (CB1 and CB2) and their endogenous ligands (primarily anandamide and 2-AG), plays a prominent role in the control of food intake and energy metabolism. Stimulation of this system triggers metabolic processes leading to weight gain, lipogenesis, insulin resistance, dyslipidemias and impaired glucose homeostasis. (±)-SLV319, the racemate of SLV319, is a potent and selective CB-1 receptor antagonist with an IC₅₀ value of 22 nM^[1]. (±)-SLV319 exhibits a high affinity to CB1 (K_i = 7.8 ± 1.4 nM). In vivo, vehicle-treated Zucker diabetic fatty (ZDF) rats were severely hyperglycaemic and showed signs of β-cell decline, including dramatic reductions in unfasted insulin levels. (±)-SLV319 (10 mg/kg) reduced the following relative to vehicle controls: fasting glucose (-61%), glucose excursion area under the curve (AUC) in an oral glucose tolerance test (OGTT, -44%) and HbA1c (-50%). Furthermore, non-fasting insulin, islet area and islet insulin content were all increased (71, 40 and 76%, respectively) relative to vehicle controls^[2].
参考文献

[1] Chorvat RJ, Berbaum J, Seriacki K, McElroy JF. JD-5006 and JD-5037: peripherally restricted (PR) cannabinoid-1 receptor blockers related to SLV-319 (Ibipinabant) as metabolic disorder therapeutics devoid of CNS liabilities. Bioorg Med Chem Lett. 2012;22(19):6173‐6180
[2] Rohrbach K, Thomas MA, Glick S, et al. Ibipinabant attenuates β-cell loss in male Zucker diabetic fatty rats independently of its effects on body weight. Diabetes Obes Metab. 2012;14(6):555‐564

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0517 mL
- 10.2585 mL
- 20.5170 mL
- 5 mM
- 0.4103 mL
- 2.0517 mL
- 4.1034 mL
- 10 mM
- 0.2052 mL
- 1.0258 mL
- 2.0517 mL

技术信息

CAS号

362519-49-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H20Cl2N4O2S

运输

蓝冰

分子量

487.40

别名

(±)-SLV319;(±)-BMS-646256;SLV319;JD-5001

溶解度

DMSO	440.0 mg/mL (902.7 mM)
Water	insoluble

动物实验配方

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