1. GPCR/G Protein
  2. Cannabinoid Receptor

Otenabant (Synonyms: CP-945598)

Cat. No.: HY-10871 Purity: 99.65%
Handling Instructions

Otenabant is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.

For research use only. We do not sell to patients.

Otenabant Chemical Structure

Otenabant Chemical Structure

CAS No. : 686344-29-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 94 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
10 mg USD 119 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 396 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Other Forms of Otenabant:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Otenabant is a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, exhibits 10,000-fold greater selectivity against human CB2 receptor.

IC50 & Target

Ki: 0.7 nM (CB1)

In Vitro

Otenabant HCl has low affinity with Ki of 7.6 μM for human CB2 receptors[1]. Otenabant HCl inhibits CB1 receptor with moderate unbound microsomal clearance, low hERG affinity, and adequate CNS penetration[2].

In Vivo

Otenabant acutely stimulates energy expenditure in rats and decreases the respiratory quotient indicating a metabolic switch to increased fat oxidation. Otenabant (10 mg/kg, p.o.) promotes a 9%, vehicle adjusted weight loss in a 10 day weight loss study in diet-induced obese mice[1]. Otenabant HCl reverses four cannabinoid agonistmediated behaviors (locomotor activity, hypothermia, analgesia, and catalepsy) following administration of the synthetic CB1 receptor agonist CP-55940. Otenabant HCl exhibits dose-dependent anorectic activity in a model of acute food intake in rodents and increased energy expenditure and fat oxidation[2].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.9592 mL 9.7959 mL 19.5917 mL
5 mM 0.3918 mL 1.9592 mL 3.9183 mL
10 mM 0.1959 mL 0.9796 mL 1.9592 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[2]

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 (10-10 M 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Otenabant is suspended in 0.5% methyl cellulose.

Male, 14 week old C57/Bl6/6J mice which has been maintained on a high fat diet (45% kcal from fat) for 6 weeks are selected for the DIO weight loss study. The animals body weights range at least five standard deviations from age-matched chow-fed control animals mean body weight. Mice are singly housed. The mean starting weight of all animals is 38.9±0.5 g. On day 0, mice are randomLy assigned to treatment groups (n=10 per group). Mice are dosed daily with vehicle or 10 mg/kg (p.o.) CP-945,598 over 10 days, starting approximately at 30 min before the start of the 12 h dark cycle. BW and food intake are recorded daily. Analysis of variance and comparison of means are calculated for daily and cumulative FI and cumulative BW measurements. P < 0.05 is considered statistically significant. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

510.42

Formula

C₂₅H₂₅Cl₂N₇O

CAS No.

686344-29-6

SMILES

ClC1=CC=CC=C1C2=NC3=C(N4CCC(NCC)(C(N)=O)CC4)N=CN=C3N2C5=CC=C(Cl)C=C5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Otenabant
Cat. No.:
HY-10871
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