2. GPCR/G Protein Neuronal Signaling
  3. MCHR1 (GPR24)
  4. NGD-4715

NGD-4715 是一种口服有效的黑色素聚集激素受体 1 (MCHR1) 拮抗剂，IC50、Ki 值分别为 10.6 nM、5.9 nM。NGD-4715 可作为食物摄入抑制剂、体重调节剂及代谢调节剂，能够减少饮食诱导肥胖大鼠的食物摄入、体重增长、血糖水平。NGD-4715 可用于肥胖相关研究。

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NGD-4715

NGD-4715 Chemical Structure

CAS No. : 873318-96-8

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NGD-4715 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NGD-4715 is an orally effective melanin-concentrating hormone receptor 1 (MCHR1) antagonist with IC50 and Ki values of 10.6 nM and 5.9 nM, respectively. NGD-4715 acts as an inhibitor of food intake, a body weight regulator and a metabolic regulator, and reduces food intake, body weight gain and blood glucose levels in diet-induced obese rats. NGD-4715 is applicable to obesity-related research[1].

体外研究
(In Vitro)

NGD-4715 可强效抑制 MCHR，且对 hERG 通道的抑制作用极弱 (IC50 = 38.4 μM)[1]。

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

NGD-4715 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 CL Vss Tmax Cmax F AUC0-∞
Rat[1] 10 mg/kg p.o. 2.1 h 27.7 mL/min/kg 2.8 L/kg 0.5 h 212 ng/mL 40.0 % 765 ng·h/mL
体内研究
(In Vivo)

NGD-4715 (5-15 mg/kg；口服；每日 2 次；10-26 天) 可呈剂量依赖性地减少易肥胖的饮食诱导肥胖 Wistar 大鼠的摄食量与体重[1]。

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

Animal Model: Wistar rats (male, obesity-prone, diet-induced obesity model)[1]
Dosage: 5 mg/kg (10-day treatment); 5 mg/kg (26-day treatment); 15 mg/kg (26-day treatment)
Administration: p.o.; twice daily; 10 days; 26 days
Result: Caused a 3.1% reduction in body weight over 10 days.
Reduced weight gain relative to controls over 26 days at 5 mg/kg twice daily.
Induced body weight loss over 26 days at 15 mg/kg twice daily.
Dose-dependently reduced daily food intake.
Lowered blood glucose levels, improved glucose tolerance, and reduced diet-induced hyperinsulinemia and hyperleptinemia.
Prevented post-treatment hyperphagia, with body weight gain paralleling vehicle controls during recovery.
Showed no signs of malaise, altered locomotor activity, or anxiogenic effects.
分子量

477.52

Formula

C25H30F3N3O3
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

NGD-4715 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

NGD-4715873318-96-8NGD4715NGD 4715MCHR1 (GPR24)Melanin concentrating hormone receptor 1metabolic modulatormelanin-concentrating hormone receptor 1Wistar ratshyperinsulinemiadiet-induced obesity ratshyperleptinemiabody weight modulatorfood intake inhibitorMCHR1hERG channelInhibitorinhibitorinhibit

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