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

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
1020 nM
Compound: 1
Agonist activity at human MC1R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
Agonist activity at human MC1R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
[PMID: 20207541]
CHO EC50
1020 nM
Compound: 1r, MK-0489
Agonist activity at human MC1bR expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
Agonist activity at human MC1bR expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
[PMID: 20598882]
CHO EC50
2 nM
Compound: 1
Agonist activity at rat MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
Agonist activity at rat MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
[PMID: 20207541]
CHO EC50
22 nM
Compound: 1
Agonist activity at mouse MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
Agonist activity at mouse MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
[PMID: 20207541]
CHO EC50
351 nM
Compound: 1
Agonist activity at human MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
Agonist activity at human MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
[PMID: 20207541]
CHO EC50
4.6 nM
Compound: 1r, MK-0489
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins
[PMID: 20598882]
CHO EC50
4.9 nM
Compound: 1
Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
[PMID: 20207541]
CHO EC50
997 nM
Compound: 1
Agonist activity at rat MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
Agonist activity at rat MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation
[PMID: 20207541]
CHO IC50
13 nM
Compound: 1
Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells
Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells
[PMID: 20207541]
CHO IC50
13 nM
Compound: 1r, MK-0489
Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting
Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting
[PMID: 20598882]
CHO IC50
1938 nM
Compound: 1
Displacement of [125I]NDP-alpha-MSH from human MC1R expressed in CHO cells
Displacement of [125I]NDP-alpha-MSH from human MC1R expressed in CHO cells
[PMID: 20207541]
CHO IC50
83.9 nM
Compound: 1
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells
[PMID: 20207541]
CHO IC50
890 nM
Compound: 1
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells
[PMID: 20207541]
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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