Taranabant NEW
| Price | $99 |
| Package | 1mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: Taranabant | CAS No.: 701977-09-5 |
| Purity: 99.06% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | Taranabant |
| Description | Taranabant (MK-0364) is a selective and potent cannabinoid 1 (CB1) receptor inverse agonist used in the study of obesity and nicotine dependence. |
| In vitro | Taranabant (MK-0364) is a novel, acyclic cannabinoid-1 receptor inverse agonist designed for the treatment of obesity. It binds to human or rat CB1 receptors with an IC50 of 0.3 and 0.4 nM, respectively, corresponding to Ki values of 0.13 and 0.27 nM, respectively. Additionally, Taranabant binds to human or rat CB2 receptors with an IC50 value of 290 and 470 nM, respectively, corresponding to Ki values of 170 and 310 nM, respectively. The selectivity ratio of CB1 receptors over CB2 receptors is approximately 1000-fold[2].The IC50s of Taranabant for CB1 receptors and CB2 receptors by substituted amides are 0.3±0.1 nM and 290±60 nM, respectively. Taranabant is a CB1 receptor inverse agonist with minimal potential for covalent protein binding. It exhibits exceptional potency and selectivity (900-fold over CB2) as a CB1 receptor inverse agonist, showing over a 500-fold improvement in affinity compared to the original lead. In a functional assay of cyclic-AMP production, Taranabant is determined to be an inverse agonist (EC50=2.4±1.4 nM)[1]. |
| In vivo | In C57BL/6N mice, Taranabant (MK-0364) dose-dependently inhibits 2-hour and overnight food intake, as well as overnight gains in body weight. At the oral doses of 1 and 3 mg/kg, Taranabant significantly inhibits 2-hour food intake (36 and 69% reductions, respectively; P<0.05 and P<0.00001, respectively) and overnight food intake (13 and 40% reductions, respectively; P<0.05 and P<0.00001, respectively), along with overnight gains in body weight (48 and 165% reductions, respectively; P<0.01 and P<0.00001, respectively). Taranabant demonstrates dose-dependent inhibition of food intake and weight gain, with an acute minimum effective dose of 1 mg/kg in diet-induced obese (DIO) rats[1].Taranabant (MK-0364) exhibits a favorable pharmacokinetic profile in three species (rat, 1 mg/kg iv, 2 mg/kg po, F=74%, t1/2=2.7 h; dog, 0.2 mg/kg iv, 0.4 mg/kg po, F=31%; t1/2=14 h; rhesus monkey, 0.2 mg/kg iv, 0.4 mg/kg po, F=31%, t1/2=3.6 h) and good brain exposure (1 mg/kg iv, brain and plasma concentrations of 0.11 and 0.18 μM at 1 h, respectively)[2]. |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 40 mg/mL (77.52 mM) |
| Keywords | MK 0364 | Taranabant | MK0364 |
| Inhibitors Related | β-Caryophyllene | CB2 modulator 1 | Pregnenolone | Pregnenolone acetate | CB1 antagonist 2 | OMDM-5 | CB2 receptor agonist 2 | 2,3-Butanediol | Drinabant | AM281 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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