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

Drinabant  (Synonyms: AVE1625)

目录号: HY-14788 纯度: ≥99.0%
COA 产品使用指南

Drinabant (AVE1625) 是具有口服活性的 CB1 受体的拮抗剂。Drinabant (AVE1625) 抑制hCB1-R 和 rCB1-R 激动剂刺激的钙信号的 IC50 值分别为 25 nM 和 10 nM。对 hCB2-R 无活性。

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Drinabant Chemical Structure

Drinabant Chemical Structure

CAS No. : 358970-97-5

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1 mg ¥1503
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查看 Cannabinoid Receptor 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体内研究
(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].

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
分子量

497.38

Formula

C23H20Cl2F2N2O2S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

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

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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产品名称:
Drinabant
目录号:
HY-14788
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