2. GPCR/G Protein Neuronal Signaling
  3. MCHR1 (GPR24)
  4. RGH-706

RGH-706 是一种具有口服活性、可透过血脑屏障的选择性 MCH1 受体拮抗剂，对 hMCHR1 的 IC50 为 6.2 nM。RGH-706 对 hMCH2 受体无拮抗活性。RGH-706 可改善肥胖。RGH-706 可用于肥胖症、普拉德-威利综合征的相关研究。

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RGH-706

RGH-706 Chemical Structure

CAS No. : 2027497-52-3

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RGH-706 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

RGH-706 is an orally active, blood-brain barrier-permeable, selective MCH1 receptor antagonist with an IC50 of 6.2 nM against hMCHR1. RGH-706 shows no antagonistic activity against hMCH2 receptors. RGH-706 improves obesity. RGH-706 can be used in research related to obesity and Prader-Willi syndrome[1].

体外研究
(In Vitro)

RGH-706 (60 min) 是一种强效的 hMCHR1 拮抗剂，其 IC50 为 6.2 nM[1]。
RGH-706 (3 μM; 5.5 h) 在小鼠样本中于 3 μM 条件下具有高血浆蛋白结合率 (fu = 0.0235) 和高脑组织结合率 (fu = 0.009)[1]。

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

RGH-706 相关抗体:
体内研究
(In Vivo)

RGH-706 (0.3-3 mg/kg；口服；每日两次；14-28 天) 可在饮食诱导肥胖的 C57BL/6 小鼠中产生剂量依赖性的持续性体重下降[1]。

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

Animal Model: C57BL/6 (male, obese, ~45g average body weight, diet-induced obesity model)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 3 mg/kg
Administration: p.o.; twice daily; 14 days (for 0.3,1,3 mg/kg); twice daily; 28 days (for 3 mg/kg)
Result: Induced dose-dependent body weight loss after 14 days of treatment, with control-subtracted body weight loss of 13.1% at 3 mg/kg b.i.d.
Caused a sustained 10-30% decrease in daily food intake.
Determined an ED50 (dose for 5% weight loss) of 0.25 mg/kg p.o.
Sustained body weight loss with no habituation to treatment in a 28-day DIO study with 3 mg/kg b.i.d.
dosing.
Showed supraproportional increases in plasma and brain concentrations across the 0.3-3 mg/kg dose range: at 0.3 mg/kg, Cmax plasma was 0.175 μM and Cmax brain was 0.258 μM; at 1 mg/kg, Cmax plasma was 0.664 μM and Cmax brain was 1.010 μM; at 3 mg/kg, Cmax plasma was 2.51 μM and Cmax brain was 3.010 μM.
Achieved receptor occupancy of 24% at 0.3 mg/kg b.i.d.
and 99% at 3 mg/kg b.i.d., with corresponding Cu brain/IC50 potency ratios of 0.37 and 5.78, respectively.
分子量

462.97

Formula

C26H27ClN4O2
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

RGH-706 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

RGH-7062027497-52-3RGH706RGH 706MCHR1 (GPR24)Melanin concentrating hormone receptor 1obesitydiet-induced obese C57BL/6 micehERG channelmiceVB-Caco-2 cellsMCH1 receptorhMCH2 receptorsprader?willi syndromeliver microsomeshuman MCH1-expressing cellsInhibitorinhibitorinhibit

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