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

Drinabant  (Synonyms: AVE1625)

Cat. No.: HY-14788 Purity: ≥99.0%
COA Handling Instructions

Drinabant (AVE1625) is an orally active CB1 receptor antagonist. Drinabant (AVE1625) inhibits the agonist-stimulated calcium signal with IC50 values of 25 nM and 10 nM for the hCB1-R and rCB1-R, respectively, and is ineffective for the hCB2-R.

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

Drinabant Chemical Structure

Drinabant Chemical Structure

CAS No. : 358970-97-5

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Description

Drinabant (AVE1625) is an orally active CB1 receptor antagonist. Drinabant (AVE1625) inhibits the agonist-stimulated calcium signal with IC50 values of 25 nM and 10 nM for the hCB1-R and rCB1-R, respectively, and is ineffective for the hCB2-R[1].

IC50 & Target[1]

hCB1-R

25 nM (IC50)

rCB1-R

10 nM (IC50)

CB2

10000 nM (IC50)

In Vivo

AVE1625 (10 mg/kg orally once daily), combined with Olanzapine (HY-14541) attenuates body weight gain, diminishing the enhanced food intake while maintaining increased energy expenditure and decreased motility[2].
AVE1625 (1, 3, and 10 mg/kg ip), reverses abnormally persistent LI induced by MK-801 (HY-15084B) or neonatal nitric oxide synthase inhibition in rodents, and improves both working and episodic memory[3].

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

Animal Model: Rats[1].
Dosage: 30 mg/kg.
Administration: Oral gavage, single dose.
Result: Had free access to food during the preceding night (postprandial state) caused a pronounced reduction of food intake during the subsequent 10-12 h without differences in their locomotor activity relative to that of the control group.
Caused an increase in FFA and glycerol, indicating increased lipolysis from fat tissue.
Immediately resulted in a pronounced increase in VCO2 and VO2, indicating increased oxidation of energetic substrates and increased TEE.
Animal Model: Female Hanover Wistar rats weighing 225 ± 8.6 g[2].
Dosage: 10 mg/kg.
Administration: Orally once daily.
Result: Reduced their weight markedly within the first 3 days of treatment where upon animals maintained lower body weight, although they lost about 7.3 ± 1.3 g fat during the 12 days of treatment.
Clinical Trial
Molecular Weight

497.38

Formula

C23H20Cl2F2N2O2S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CS(=O)(N(C1CN(C(C2=CC=C(Cl)C=C2)C3=CC=C(Cl)C=C3)C1)C4=CC(F)=CC(F)=C4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 15 mg/mL (30.16 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0105 mL 10.0527 mL 20.1054 mL
5 mM 0.4021 mL 2.0105 mL 4.0211 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0105 mL 10.0527 mL 20.1054 mL 50.2634 mL
5 mM 0.4021 mL 2.0105 mL 4.0211 mL 10.0527 mL
10 mM 0.2011 mL 1.0053 mL 2.0105 mL 5.0263 mL
15 mM 0.1340 mL 0.6702 mL 1.3404 mL 3.3509 mL
20 mM 0.1005 mL 0.5026 mL 1.0053 mL 2.5132 mL
25 mM 0.0804 mL 0.4021 mL 0.8042 mL 2.0105 mL
30 mM 0.0670 mL 0.3351 mL 0.6702 mL 1.6754 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Drinabant
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