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Rimonabant

利莫那班,SR141716

Rimonabant是一个大脑中心大麻素受体（CB1）特异性口服拮抗剂。在hCB1转染HEK293细胞中IC50浓度为13.6 nM，EC50浓度为17.3 nM。

目录号
EY1536
EY1536
EY1536
纯度
99.41%
99.41%
99.41%
规格
10 mg
50 mg
100 mg
原价
300
1200
2100
售价
300
1200
2100
库存
现货
现货
现货
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  • 生物活性

    Rimonabant is a selective antagonist of CB1 with IC50 of 13.6 nM and EC50 of 17.3 nM in hCB1 transfected HEK 293 membrane.

  • 体外研究

  • 体内研究

    30% PEG400+0.5% Tween80+5% propylene glycol

  • 激酶实验

  • 细胞实验

    0,1,4 μM

  • 动物实验

    20 ml/kg (小鼠) 和 5 ml/kg (大鼠)WIN55212-2静脉注射之前，Rimonabant 通过腹腔注射(30 分钟)或口服(1 小时)给药

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Chu CM, et al, Org Biomol Chem, 2008, 6(18), 3399-3407
    [2] Rinaldi-Carmona, M., Barth, F., Héaulme, M., et al. SR141716A, a potent and selective antagonist of the brain cannabinoid receptor. FEBS Lett 350 240-244 (1994).
    [3] Malfitano, A.M., Laezza, C., Pisanti, S., et al. Rimonabant (SR141716) exerts anti-proliferative and immunomodulatory effects in human peripheral blood mononuclear cells. Brit J Pharmacol 153 1003-1010 (2009).

    分子式
    C22H21Cl3N4O    		 分子量
    463.79    		 CAS号
    168273-06-1    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    25 mg/mL     		Water
    <1 mg/mL    		 Ethanol
    20 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT00263042 Cardiovascular Disease Drug: Rimonabant|Drug: Placebo (for Rimonabant) Sanofi Phase 3 2005-12-01 2016-04-21
    NCT00228176 Carotid Artery Plaque|Arteriosclerosis|Obesity|Metabolic Syndrome X Drug: Rimonabant|Drug: Placebo (for Rimonabant) Sanofi Phase 3 2005-08-01 2016-04-21
    NCT00576667 Fatty Liver Drug: Rimonabant|Drug: Placebo (for Rimonabant) Sanofi Phase 3 2008-01-01 2016-04-18
    NCT00577148 Fatty Liver Drug: Rimonabant|Drug: Placebo (for Rimonabant) Sanofi Phase 3 2008-02-01 2016-04-18
    NCT00584389 Obesity Drug: rimonabant|Behavioral: Dietary intervention University of Surrey|European Foundation for the Study of Diabetes|Royal Surrey County Hospital Phase 4 2007-07-01 2010-04-16
    NCT00325650 Prediabetic State Drug: Rimonabant|Drug: Placebo (for Rimonabant) Sanofi Phase 3 2006-05-01 2016-04-19
    NCT00299325 Metabolic Syndrome Drug: Rimonabant|Drug: Placebo (for Rimonabant)|Other: Mild hypocaloric diet Sanofi Phase 3 2006-02-01 2016-06-01
    NCT00547118 Schizophrenia|Schizoaffective Disorder|Obesity|Hypertension|Smoking Drug: Rimonabant|Drug: Placebo University of Maryland|National Institute on Drug Abuse (NIDA) Phase 2 2007-11-01 2015-02-24
    NCT00690456 Diabetes Mellitus, Type 2 Drug: Rimonabant|Drug: Placebo (for Rimonabant)|Drug: Metformin Sanofi Phase 3 2008-05-01 2016-04-18
    NCT00603109 Prader-willi Syndrome Drug: rimonabant|Drug: placebo Weill Medical College of Cornell University|National Institutes of Health (NIH)|PWSAUSA Phase 3 2007-08-01 2011-01-03
    NCT00478972 Obesity|Diabetes Mellitus Type 2 Drug: Rimonabant|Drug: placebo (for Rimonabant)|Other: Diet and exercise Sanofi Phase 3 2007-04-01 2016-06-06
    NCT00754689 Diabetes Mellitus, Type 2 Drug: Rimonabant|Drug: Metformin|Drug: placebo Sanofi Phase 3 2008-09-01 2016-05-13
    NCT00478595 Obesity|Diabetes Mellitus Type 2 Drug: Rimonabant|Drug: Placebo (for Rimonabant)|Drug: Anti-diabetic monotherapy Sanofi Phase 3 2007-04-01 2016-06-01
    NCT00449605 Diabetes Mellitus, Type 2 Drug: Rimonabant|Drug: Glimepiride|Drug: Metformin Sanofi Phase 3 2007-03-01 2016-04-13
    NCT00464256 Smoking Cessation Drug: rimonabant Sanofi Phase 3 2004-04-01 2010-12-09
    NCT00464165 Smoking Cessation Drug: rimonabant Sanofi Phase 3 2002-11-01 2010-12-09
    NCT00546325 Diabetes Mellitus, Type 2 Drug: Rimonabant|Drug: Placebo Sanofi Phase 3 2007-10-01 2010-12-09
    NCT00358228 Smoking Cessation Drug: Rimonabant Sanofi Phase 3 2002-09-01 2010-12-09
    NCT00525681 Renal Transplantation Drug: cyclosporine A|Drug: tacrolimus University of Oslo School of Pharmacy Phase 4 2007-09-01 2014-12-02
    NCT00405808 Obesity Drug: Rimonabant|Drug: Placebo Sanofi Phase 3 2006-12-01 2011-01-25
    NCT00458081 Obesity|Microalbuminuria|Diabetes Mellitus, Type 2|Dyslipidemia Drug: Rimonabant|Drug: Placebo Sanofi Phase 3 2007-03-01 2010-12-09
    NCT00412698 Obesity|Dyslipidemias Drug: rimonabant|Drug: Placebo Sanofi Phase 3 2006-12-01 2010-12-09
    NCT00459173 Maintenance of Smoking Cessation Drug: rimonabant (SR141716) Sanofi Phase 3 2002-11-01 2009-04-06
    NCT00075205 Healthy|Alcohol Drinking Drug: SR141716 (Rimonabant) National Institute on Alcohol Abuse and Alcoholism (NIAAA)|Sanofi-Synthelabo|National Institutes of Health Clinical Center (CC) Phase 2 2003-12-31 2017-01-24

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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