Otenabant hydrochloride NEW
Price | $39 | $54 | $74 |
Package | 1mg | 2mg | 5mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-19 |
Product Details
Product Name: Otenabant hydrochloride | CAS No.: 686347-12-6 |
Purity: ≥95% | Supply Ability: 10g |
Release date: 2024/11/19 |
Product Introduction
Bioactivity
Name | Otenabant hydrochloride |
Description | Otenabant hydrochloride (Otenabant) (CP-945598) is a competitive, high affinity, selective antagonist of the CB1 receptor (Ki: 0.7 nM). |
Kinase Assay | Membranes are prepared from CHOK1 cells stably transfected with the human CB-1 receptor cDNA. GTPγ [35S] binding assays are performed in a 96-well FlashPlate format in duplicate using 100 pM GTPγ [35S] and 10μg membrane per well in assay buffer composed of 50 mM Tris HCl, pH 7.4, 3 mM MgCl2, pH 7.4, 10 mM MgCl2, 20 mM EGTA, 100 mM NaCl, 30 μM GDP, 0.1% bovine serum albumin, and the following protease inhibitors: 100 μg/mL bacitracin, 100 μg/mL benzamidine, 5 μg/mL aprotinin, 5 μg/mL leupeptin. The assay mix is then incubated with increasing concentrations of antagonist (10-10M to 10-5 M) for 10 min and challenged with the cannabinoid agonist CP-55,940 (10 μM). Assays are performed at 30°C for 1 h. The FlashPlates are then centrifuged at 2000 g for 10 min. Stimulation of GTPγ [35S] binding is then quantified using a Wallac Microbeta. EC50 calculations are done using Prism by GraphPad. Inverse agonism is measured in the absence of agonist. |
In vitro | In a diet-induced obesity model in mice, CP-945598 (10 mg/kg) facilitated a 9% reduction in body weight over a 10-day weight loss study. CP-945598 significantly enhanced energy expenditure in rats and reduced the respiratory quotient, indicating a metabolic shift towards increased fat oxidation. Additionally, CP-945598 HCl reversed behaviors mediated by four cannabinoid agonists (hypothermia, spontaneous activity, catalepsy, and analgesia). In acute food intake models in rodent species, CP-945598 HCl suppressed appetite, further promoting fat oxidation and energy consumption. |
In vivo | CP-945598 HCl exhibits lower affinity towards human CB2 receptors (Ki: 7.6 μM) and demonstrates inhibitory effects on the CB1 receptor. Additionally, it possesses moderate microsomal clearance, low affinity for hERG, and sufficient penetration of the central nervous system (CNS). |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : Slightly soluble |
Keywords | Cannabinoid Receptor | CP945598 | inhibit | CP945598 Hydrochloride | Otenabant hydrochloride | Inhibitor | CP-945598 Hydrochloride | CP 945598 | CP-945598 | Otenabant Hydrochloride |
Inhibitors Related | β-Caryophyllene | CB2 modulator 1 | Pregnenolone | Pregnenolone acetate | CB1 antagonist 2 | OMDM-5 | CB2 receptor agonist 2 | 2,3-Butanediol | Drinabant | AM281 |
Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
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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