鹽酸利莫那班作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetRimonabant HydrochlorideCat. No.: HY-14137CAS No.: 158681-13-1分式: CHClNO分量: 500.25作靶點(diǎn): Cannabinoid Receptor; Bacterial作通路: GPCR/G Protein; Neuronal Signaling; Anti-infection儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 33.33 mg/mL (66.63 mM;

2、 Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)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(qǐng)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(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)

3、請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都?qǐng)先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的式助溶1. 請(qǐng)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 ultrasonic此案可獲

4、得 2.5 mg/mL (5.00 mM) 的均勻懸濁液，懸濁液可于服和腹腔注射。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.00 mM); Clear solution此案可獲得 2.5 mg/mL (5.00 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。Page 1

5、of 2 www.MedChemE以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL 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(dòng)劑， Ki 值為1.8 nM。Rimonabant hHydrochloride (SR 141716A Hydrochloride) 也能夠抑制分枝桿 膜蛋3 (MMPL3)。IC & Target CB11.8 nM (Ki)體外研究 Rimo

6、nabant could inhibit the growth of Mtb with an MIC of 54 M. MmpL3, an anti-TB target, is the direct target ofrimonabant2.Rimonabant itself (10-12-10-3 M, 12 concentrations) inhibits the basal binding of 35SGTPgS to human corticalmembranes in a concentration dependent manner, with a -log IC50 of 4.70

7、.2 (IC50 = 20 M) and a maximalinhibition 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 impaired glucosetolerance model and for 10 weeks to 6-month-old male obese Zucker rats as a model of the metabolic syndrome.RANTES and MCP-1 serum lev

8、els are increased in obese vs lean Zucker rats and significantly reduced by long-termtreatment with Rimonabant, which slowes weight gain in rats with the metabolic syndrome. Neutrophils andmonocytes are significantly increased in young and old obese vs lean Zucker rats and lowered by Rimonabant.Plat

9、elet-bound fibrinogen is significantly enhanced in obese vs lean Zucker rats of both age, and is reduced byRimonabant 1.Rimonabant (20 mg daily) exhibits a significant reduction in many cardiometabolic risk factors4.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 19. pii: S0

10、306-4522(19)30117-4.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Seely KA, et al. AM-251 and rimonabant act as direct antagonists at mu-opioid receptors: Implications for opioid/cannabinoid interaction studies.Neuropharmacology. 2012 Oct;63(5):905-15.2. Zhang B, e

11、t 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 frompostmortem human brain Biochem

12、ical 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 frompostmortem human brain Biochemical Pharmacology (2012), 83(2), 260-268.McePdfHeightPage 2 of 3 www.MedChemECaution: Product has not been