1. GPCR/G Protein Neuronal Signaling
  2. Cannabinoid Receptor
  3. Taranabant

Taranabant  (Synonyms: MK-0364)

目录号: HY-10013 纯度: 99.06%
Data Sheet SDS COA 产品使用指南 技术支持

Taranabant 是一种有效的选择性的 cannabinoid 1 (CB1) 受体反向激动剂,抑制结合和多种激动剂的功能活性,作用于人 CB1R,Ki 为 0.13 nM。

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Taranabant Chemical Structure

Taranabant Chemical Structure

CAS No. : 701977-09-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2247
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2 mg ¥990
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5 mg ¥1980
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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding Ki of 0.13 nM for the human CB1R in vitro.

IC50 & Target

IC50: 0.3 nM (hCB1R), 0.4 nM (rCB1R)[1]
Ki: 0.13 nM (hCB1R), 0.27 nM (rCB1R)[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
0.3 nM
Compound: 63
Inhibition of radiolabeled CP5549 binding to human Cannabinoid receptor 1 expressed in CHO cells by competition assay
Inhibition of radiolabeled CP5549 binding to human Cannabinoid receptor 1 expressed in CHO cells by competition assay
[PMID: 31497963]
CHO-K1 IC50
1170 nM
Compound: 3, MK-0364
Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry
Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry
[PMID: 18954042]
体外研究
(In Vitro)

Taranabant (MK-0364) 与人或大鼠 CB1R 结合,IC50 分别为 0.3 和 0.4 nM,对应的 Ki 值为 0.13 和 0.27 nM。Taranabant 与人或大鼠 CB2R 结合,IC50 值分别为 290 和 470 nM,对应的 Ki 值分别为 170 和 310 nM。CB1R对CB2R的选择性比约为1000倍[1]
Taranabant (MK-0364) 是一种新型无环大麻素-1 受体反向激动剂,用于处理肥胖症。Taranabant 对 CB1R 和 CB2R 的取代酰胺作用的 IC50 分别为 0.3±0.1 nM 和 290±60 nM。Taranabant 是一种 CB1R 反向激动剂,具有最小的共价蛋白结合潜力。Taranabant 是一种非常有效和选择性 (比 CB2 高 900 倍) 的 CB1R 反向激动剂,其亲和力比原始先导药物高 500 倍以上。在 cyclic-AMP 生成的功能测定中,Taranabant 被确定为反向激动剂 (EC50=2.4±1.4 nM)[2]

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

体内研究
(In Vivo)

Taranabant (MK-0364) 以剂量依赖性方式抑制C57BL/6N小鼠2小时和过夜的食物摄入以及过夜体重增加。在1 mg/kg和3 mg/kg剂量(口服)下,Taranabant显著抑制2小时食物摄入(分别减少36%和69%;P<0.05和P<0.00001)和过夜食物摄入(分别减少13%和40%;P<0.05和P<0.00001)以及过夜体重增加(分别减少48%和165%;P<0.01和P<0.00001)。Taranabant以剂量依赖性方式抑制食物摄入和体重增加,在饮食诱导肥胖(DIO)大鼠中的急性最小有效剂量为1 mg/kg[1]
Taranabant (MK-0364) 在三种动物模型中(大鼠:1 mg/kg 静脉注射,2 mg/kg 口服,生物利用度F=74%,半衰期t1/2=2.7小时;狗:0.2 mg/kg 静脉注射,0.4 mg/kg 口服,生物利用度F=31%,半衰期t1/2=14小时;恒河猴:0.2 mg/kg 静脉注射,0.4 mg/kg 口服,生物利用度F=31%,半衰期t1/2=3.6小时)具有良好的药代动力学特性,并且具有良好的脑部暴露(1 mg/kg 静脉注射后1小时脑和血浆浓度分别为0.11 μM和0.18 μM)[2]

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

Clinical Trial
NCT NumberSponsorConditionStart DatePhase
NCT00430742Merck Sharp & Dohme LLC
Obesity Type 2 Diabetes Mellitus|Type 2 Diabetes Mellitus
November 2006Phase 3
NCT00131391Merck Sharp & Dohme LLC
Obesity
July 2005Phase 3
NCT00109135Merck Sharp & Dohme LLC
Smoking
January 2005Phase 2
分子量

515.95

Formula

C27H25ClF3N3O2

CAS 号
性状

固体

颜色

White to off-white

中文名称

泰伦那班

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 42 mg/mL (81.40 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9382 mL 9.6909 mL 19.3817 mL
5 mM 0.3876 mL 1.9382 mL 3.8763 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 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

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.85 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.85 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

扫码获得
动物溶解方案

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

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO PEG300/PEG400Tween 80,均可在 MCE 网站选购。
纯度 & 产品资料
参考文献
Kinase Assay
[1]

The binding assay is performed by incubating various concentrations of Taranabant (MK-0364) with 0.5 nM [3H]CP 55,940, 1.5 μg of recombinant human CB1R-CHO membranes (or 0.1 μg of human CB2R-CHO membranes) in 50 mM Tris-HCl, pH 7.4, 5 mM MgCl2, 2.5 mM EDTA, 0.5 mg/mL fatty acid-free bovine serum albumin (BSA), 1× proteinase inhibitor mix, and 1% DMSO. After 1-h incubation at 37°C, the reaction is stopped by filtration, and bound radioligand is separated from free radioligand by washing the filter plate. Total specifically bound radiolabel is approximately 10% of the total added radiolabel. Inhibitory IC50 values are calculated through nonlinear curve fitting, from which Ki values are then calculated. The CB1R density (Bmax=5 pmol/mg based on [3H]CP 55,940 binding) in the recombinant human CB1R-CHO membranes is close to that from rat brain membranes (3-5 pmol/mg)[1].

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

Animal Administration
[1]

Mice[1]
Male C57BL/6N wild-type mice are used. MK-0364 is dissolved or dispersed (with sonication) as a fine homogeneous suspension in 0.225% methylcellulose/10% Tween 80 in water for subsequent oral dosing of mice. All mice are weighed, and vehicle (0.225% methylcellulose/10% Tween 80 in water) or Taranabant (1 or 3 mg/kg) is administered by oral gavage to male mice approximately 30 min before the onset of the dark phase of the light cycle (n=12 per group, age 23 weeks, mean body weight 34.14±0.53 g). Mice are fed ad libitum in the dark phase after dosing. A preweighed aliquot of a highly palatable medium-high fat diet (25% kcal from sucrose, 32% kcal from fat, 4.41 kcal/g) is provided in the food hopper of the cage 5 min before the onset of the dark phase of the light cycle and weighed 2 and 18 h after the onset of the dark phase of the light cycle. In addition, all mice are weighed 18 h after the onset of the dark phase of the light cycle. The study is of crossover design, i.e., vehicle and 1-mk/kg groups are dosed first. After a 4-day washout, the previous vehicle group is dosed with 3 mg/kg Taranabant, and the previous 1-mg/kg group is dosed with vehicle.
Rats[1]
For acute experiments, male Sprague-Dawley DIO rats are randomized into groups (n=6 rats/group) for compound and vehicle dosing. Rats are weighed 17 h after dosing to determine effects on overnight body weight gain. Taranabant is administered orally to DIO rats 1 h before the start of the dark cycle (3:00 PM) at 0.3, 1, and 3 mg/kg p.o. Vehicle is 10% Tween 80 in water, and dosing volume is 2 mL/kg. Powdered food is provided in food cups that are weighed continuously at 5-min intervals over 18 h, and the data are recorded using a computerized system.

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

参考文献

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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9382 mL 9.6909 mL 19.3817 mL 48.4543 mL
5 mM 0.3876 mL 1.9382 mL 3.8763 mL 9.6909 mL
10 mM 0.1938 mL 0.9691 mL 1.9382 mL 4.8454 mL
15 mM 0.1292 mL 0.6461 mL 1.2921 mL 3.2303 mL
20 mM 0.0969 mL 0.4845 mL 0.9691 mL 2.4227 mL
25 mM 0.0775 mL 0.3876 mL 0.7753 mL 1.9382 mL
30 mM 0.0646 mL 0.3230 mL 0.6461 mL 1.6151 mL
40 mM 0.0485 mL 0.2423 mL 0.4845 mL 1.2114 mL
50 mM 0.0388 mL 0.1938 mL 0.3876 mL 0.9691 mL
60 mM 0.0323 mL 0.1615 mL 0.3230 mL 0.8076 mL
80 mM 0.0242 mL 0.1211 mL 0.2423 mL 0.6057 mL

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目录号:
HY-10013
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