2. GPCR/G Protein Neuronal Signaling
  3. Melanocortin Receptor
  4. MC4R Antagonist-1

MC4R Antagonist-1 (compound 1) 是一种 MC4R 选择性拮抗剂 (IC50<10 nM)。MC4R Antagonist-1 可用于恶病质、厌食症、神经性厌食症、非自愿体重减轻、生长发育迟缓、肌肉减少症、肌肉消耗、肌无力、虚弱、骨质疏松症的相关研究。

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MC4R Antagonist-1

MC4R Antagonist-1 Chemical Structure

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MC4R Antagonist-1 相关抗体

Top Publications Citing Use of Products

查看 Melanocortin Receptor 亚型特异性产品:

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MC1R MC3R MC2R MC4R MC5R

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MC4R Antagonist-1 (compound 1) is an MC4R-selective antagonist (IC50<10 nM). MC4R Antagonist-1 can be used for the research of cachexia, anorexia, anorexia nervosa, involuntary weight loss, failure to thrive, sarcopenia, muscle wasting, muscle weakness, frailty, osteoporosis[1].

IC50 & Target

MC4R

<10 nM (IC50)

体外研究
(In Vitro)

MC4R Antagonist-1 (compound 1) (0.1-1000 nM；8-16 h) 可恢复过表达 T162I-MC4R 的 HEK293 细胞中 α-MSH 诱导的 cAMP 信号，EC50＜50 nM 且 Emax＞150%[1]。
MC4R Antagonist-1 (10 μM；10-16 h) 显著提升转染 24 种 MC4R 功能缺失突变体的 HEK293 细胞的质膜 MC4R 水平并升高质膜 / 总 MC4R 比值[1]。
MC4R Antagonist-1 (在人肝微粒体体外体系中仅生成 4 种 GSH 加合物且总相对丰度为 3.6%，无肝微粒体时未产生 GSH 加合物[1]。

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

MC4R Antagonist-1 相关抗体:

Cell Viability Assay[1]

Cell Line: HEK293 cells transiently transfected with 24 loss-of-function MC4R variants
Concentration: 0.75 μM, 10 μM
Incubation Time: 10-16 h
Result: Significantly increased plasma membrane MC4R levels and the ratio of plasma membrane to total cellular MC4R for all tested MC4R loss-of-function variants.
体内研究
(In Vivo)

MC4R Antagonist-1 (compound 1) (30-60 mpk；皮下注射；每日两次；19 天) 在纯合子 MC4RR165Q/R165Q MC4R 缺陷肥胖小鼠模型中，可显著降低小鼠体重与累积摄食量[1]。

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

Animal Model: Homozygous MC4RR165Q/R165Q MC4R-deficient (MC4R-D) mice (8 weeks old, single-housed, preconditioned with 45% high-fat diet)[1]
Dosage: 10 mpk, 30 mpk, 60 mpk
Administration: subcutaneous injection, twice daily (BID) for 19 days
Result: At 30 mpk and 60 mpk BID, significantly decreased body weight and cumulative food intake compared with the vehicle-treated group, whereas 10 mpk BID did not produce significant effects on body weight or cumulative food intake.
分子量

477.53

Formula

C25H28FN7O2
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

MC4R Antagonist-1 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:

MC4R Antagonist-1Melanocortin ReceptorMC ReceptorMC4Rcachexiasarcopeniaanorexia nervosafrailtymuscle weaknessfailure to thriveanorexiamuscle wastinginvoluntary weight lossInhibitorinhibitorinhibit

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