2. GPCR/G Protein
  3. Orphan GPCR
  4. GPR61 Inverse agonist 2

GPR61 Inverse agonist 2 是一种选择性的 GPR61 反向激动剂，对人源的 IC50 为 6.2 nM，对小鼠源的 IC50 为 20 nM；对人源的 Ki 为 0.21 nM，对小鼠源的 Ki 为 0.72 nM。GPR61 Inverse agonist 2 可结合 GPR61 被诱导产生的细胞内变构口袋，破坏受体与 Gαs 的相互作用，并消除 GPR61 的组成型活性。GPR61 Inverse agonist 2 不会改变健康小鼠的食物摄入量或体重。GPR61 Inverse agonist 2 可用于恶病质/肌少症的相关研究。

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GPR61 Inverse agonist 2

GPR61 Inverse agonist 2 Chemical Structure

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GPR61 Inverse agonist 2 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

GPR61 Inverse agonist 2 is a selective GPR61 inverse agonist with human IC50 of 6.2 nM and mouse IC50 of 20 nM, human Ki of 0.21 nM, and mouse Ki of 0.72 nM. GPR61 Inverse agonist 2 binds to an induced intracellular allosteric pocket of GPR61, disrupts receptor-Gαs interactions, and abolishes GPR61 constitutive activity. GPR61 Inverse agonist 2 does not alter food intake or body weight in healthy mice. GPR61 Inverse agonist 2 can be used for the research of cachexia/sarcopenia[1].

体外研究
(In Vitro)

GPR61 Inverse agonist 2 (Compound 15) 可高效抑制过表达人源 GPR61 的 CHO 细胞中该受体的组成型活性，其 IC50 为 6.2 nM[1]。
GPR61 Inverse agonist 2 可抑制过表达细胞中小鼠 GPR61 的组成型活性，其 IC50 为 20 nM[1]。
GPR61 Inverse agonist 2 可特异性结合人源 GPR61，从而提高受体的细胞表面表达水平并抑制组成型活性，且对 MC4R 无活性[1]。
GPR61 Inverse agonist 2 可特异性结合过表达人源 GPR61 的 CHO 细胞，而与亲本 CHO 细胞无显著结合[1]。
GPR61 Inverse agonist 2 以高亲和力与过表达 CHO 细胞中的人源 GPR61 (Ki = 0.21 nM) 和鼠源 GPR61 (Ki = 0.72 nM) 结合[1]。

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

GPR61 Inverse agonist 2 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route CL Vdss T1/2 Brain-to-Plasma Ratio Bioavailability
Mice[1] 1 mg/kg i.v. 2 mL/min/kg 0.13 L/kg 0.97 h / /
Mice[1] 5 mg/kg p.o. / / / / 85 %
Mice[1] 10 mg/kg s.c. / / / 0.7 % /
体内研究
(In Vivo)

GPR61 Inverse agonist 2 (Compound 15) (10-30 mg/kg；口服；每日 2 次；连续 14 天) 不会改变健康小鼠的食物摄入量或体重[1]。

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

Animal Model: Mice (10-11 weeks old)[1]
Dosage: 10 mg/kg; 30 mg/kg
Administration: p.o.; twice daily; 14 days
Result: Showed no statistically significant changes in food intake over 14 days.
Showed no statistically significant changes in body weight over 14 days.
分子量

454.88

Formula

C18H17ClF2N6O2S
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

GPR61 Inverse agonist 2 相关分类

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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:

GPR61 Inverse agonist 2Orphan GPCRRrphan G protein-coupled receptorGPR61MC4RCHO cellsmousecryo-EMcachexia/sarcopeniahumanGαsInhibitorinhibitorinhibit

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