Rimonabant-Hydrochloride-SR-141716A-Hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERimonabant HydrochlorideCat. No.: HY-14137CAS No.: 158681-13-1Synonyms: SR 141716A (Hydrochloride)分式: CHClNO分量: 500.25作靶點: Cannabinoid Receptor; Bacterial作通路: GPCR/G Protein; Neuronal Signaling; Anti-infection儲存式: Powder -20C 3

2、years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 33.33 mg/mL (66.63 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.9990 mL 9.9950 mL 19.9900 mL5 mM 0.3998 mL 1.9990 mL 3.9980 mL10 mM 0.1999 mL 0.9995 mL 1.9990 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限

3、。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.00 mM); Suspended solution; Need ultrasonic2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility:

4、2.5 mg/mL (5.00 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Rimonabant hHydrochloride (SR 141716A Hydrochloride)中素受體 1 (CB1) 效的、選擇性的反向激動劑， Ki 值為1.8 nM。Rimonabant hHydrochloride (SR 141716A Hydrochloride) 也能夠抑制分枝桿菌膜蛋3 (MMPL3)。IC50 & Target CB11.8 nM (Ki)

5、體外研究 Rimonabant could inhibit the growth of Mtb with an MIC of 54 M. MmpL3, an anti-TB target, is the directtarget of rimonabant 2.Rimonabant itself (10-12-10-3 M, 12 concentrations) inhibits the basal binding of 35SGTPgS to humancortical membranes in a concentration dependent manner, with a -log IC

6、50 of 4.70.2 (IC50 = 20 M) and amaximal inhibition of 482% 3.體內(nèi)研究 Rimonabant (10 mg/kg by gavage) is fed for 2 weeks to 3-month-old male obese Zucker rats as an impairedglucose tolerance model and for 10 weeks to 6-month-old male obese Zucker rats as a model of themetabolic syndrome. RANTES and MCP-

7、1 serum levels are increased in obese vs lean Zucker rats andsignificantly reduced by long-term treatment with Rimonabant, which slowes weight gain in rats with themetabolic syndrome. Neutrophils and monocytes are significantly increased in young and old obese vs leanZucker rats and lowered by Rimon

8、abant. Platelet-bound fibrinogen is significantly enhanced in obese vs leanZucker rats of both age, and is reduced by Rimonabant 1.Rimonabant (20 mg daily) exhibits a significant reduction in many cardiometabolic risk factors 4.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cell. 2019 Jan 24;176(3):636-648.e13. Neuroscience. 2019 Feb

9、 19. pii: S0306-4522(19)30117-4.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Seely KA, et al. AM-251 and rimonabant act as direct antagonists at mu-opioid receptors: Implications for opioid/cannabinoid interactionstudies. Neuropharmacology. 2012 Oct;63(5):905-15.2. Zhang B,

10、et al. Crystal Structures of Membrane Transporter MmpL3, an Anti-TB Drug Target. Cell. 2019 Jan 24;176(3):636-648.e13.3. Erdozain, A. M. et al. The inverse agonist effect of rimonabant on G protein activation is not mediated by the cannabinoid CB1 receptor:Evidence from postmortem human brain Bioche

11、mical Pharmacology (2012), 83(2), 260-268.4. Erdozain, A. M. et al. The inverse agonist effect of rimonabant on G protein activation is not mediated by the cannabinoid CB1 receptor:Evidence from postmortem human brain Biochemical Pharmacology (2012), 83(2), 260-268.McePdfHeightCaution: Product has not be