2. GPCR/G Protein Neuronal Signaling
  3. Melanocortin Receptor
  4. MK-0489

MK-0489 是一种口服有效的、高效且具有选择性的 MC4R 激动剂。MK-0489 对人 MC4R 具有很强的结合亲和力 (IC50 = 13 nM) 和功能性激动剂活性 (EC50 = 4.6 nM)。MK-0489对小鼠 MC4R 显示出 22 nM (EC50) 的功能活性，对小鼠 MC3R 显示出 1.7 μM (EC50) 的功能活性。MK-0489 可用于肥胖症的研究。

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MK-0489

MK-0489 Chemical Structure

CAS No. : 778625-65-3

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MK-0489 相关抗体

Top Publications Citing Use of Products

查看 Melanocortin Receptor 亚型特异性产品:

查看所有亚型
MC1R MC3R MC2R MC4R MC5R

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MK-0489 is an orally active, highly effective, and selective MC4R agonist. MK-0489 exhibits a strong binding affinity (IC50 = 13 nM) and functional agonist activity (EC50 = 4.6 nM) at human MC4R. MK-0489 shows functional activity of 22 nM (EC50) on mouse MC4R and 1.7 μM (EC50) on mouse MC3R. MK-0489 can be used for the study of obesity[1].

IC50 & Target[1]

MC4R

 

体内研究
(In Vivo)

MK-0489 (Compound 1r) (2-20 mg/kg，口服，单次给药或每日两次，持续 14 天) 通过 MC4R 介导的减少特异性地降低小鼠的食物摄入量和体重，并且以剂量依赖的方式降低饮食诱导肥胖大鼠模型的体重[1]。

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

Animal Model: Wild type (WT) and MC4R/3R knockout (KO) mouse[1].
Dosage: 10 mg/kg
Administration: P.o., once
Result: Significant reducted in food intake and body weight was observed in wild-type mice; however, no significant effect was observed in MC4R/3R knockout mice.
Animal Model: Diet-induced obese rat model[1].
Dosage: 2 mg/kg, 6 mg/kg, 20 mg/kg
Administration: P.o., twice a day for 14 days
Result: Exhibited dose-dependent weight loss effect.
分子量

600.18

Formula

C34H44ClF2N3O2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MK-0489 相关分类

  • 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 *
= × ×

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.

Keywords:

MK-0489778625-65-3MK0489MK 0489Melanocortin ReceptorMC ReceptorMC4RAgonistObesityInhibitorinhibitorinhibit

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目录号：
HY-11073
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