2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel Metabolic Enzyme/Protease
  3. Orphan GPCR GABA Receptor Phosphodiesterase (PDE)
  4. GPR61 Inverse agonist 3

GPR61 Inverse agonist 3 是一种具有选择性且可透过血脑屏障的 GPR61 反向激动剂，对人源的 IC50 为 4.0 nM，对小鼠源的 IC50 为 8.8 nM，人源 Ki 为 0.34 nM，小鼠源 Ki 为 1.1 nM。GPR61 Inverse agonist 3 可破坏 GPR61-Gαs 蛋白相互作用，从而消除 GPR61 的组成型活性。GPR61 Inverse agonist 3 可中度抑制 GABAA 氯离子通道和 PDE3A1，对应的 IC50 值分别为 4.6 μM 和 8.9 μM。GPR61 Inverse agonist 3 与泛 CYP 抑制剂联合给药时，对成年小鼠的食物摄入无功能性影响。GPR61 Inverse agonist 3 可用于恶病质/肌肉减少症的相关研究。

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GPR61 Inverse agonist 3

GPR61 Inverse agonist 3 Chemical Structure

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GPR61 Inverse agonist 3 相关抗体

Top Publications Citing Use of Products

查看 Phosphodiesterase (PDE) 亚型特异性产品:

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GPR61 Inverse agonist 3 is a selective and brain-penetrant GPR61 inverse agonist with human IC50 of 4.0 nM, mouse IC50 of 8.8 nM, human Ki of 0.34 nM, mouse Ki of 1.1 nM. GPR61 Inverse agonist 3 disrupts GPR61-Gαs protein interactions to abolish GPR61 constitutive activity. GPR61 Inverse agonist 3 moderately inhibits GABAA chloride channel and PDE3A1 with IC50 values of 4.6 and 8.9 μM. GPR61 Inverse agonist 3 shows no functional effect on food intake in adult mice co-administered with a pan-CYP inhibitor. GPR61 Inverse agonist 3 can be used for the research of cachexia/sarcopenia[1].

IC50 & Target[1]

PDE3A

8.9 μM ()

体外研究
(In Vitro)

GPR61 Inverse agonist 3 (Compound 23) 可强效抑制 TREx 诱导过表达 CHO 细胞中人类 GPR61 的组成型活性，其 IC50 为 4.0 nM，且与人类 GPR61 结合的 Ki 为 0.34 nM[1]。
GPR61 Inverse agonist 3 可强效抑制过表达 CHO 细胞中小鼠 GPR61 的组成型活性，其 IC50 为 8.8 nM，且与小鼠 GPR61 的结合 Ki 为 1.1 nM[1]。
GPR61 Inverse agonist 3 具有中等 MDR1 外排性、低 BCRP 外排性、良好的被动渗透性，以及在人肝细胞中的高固有清除率，对应数值分别为 7.4、1.2、32 × 10-6 cm/s 和 152 μL/min/million cells[1]。
GPR61 Inverse agonist 3 对 GPR61 具有高度选择性，仅对 GABAA 氯离子通道 (IC50 = 4.6 μM) 和 PDE3A1 (IC50 = 8.9 μM) 表现出中等程度的脱靶活性，对其他 104 个靶点或受试离子通道均无显著活性[1]。

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

GPR61 Inverse agonist 3 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Brain-to-Plasma Ratio CL Vdss T1/2 F
Mice[1] 7.5 mg/kg s.c. 46 % / / / /
Rat[1] 1 mg/kg i.v. / 38 mL/min/kg 2.4 L/kg 3.4 h /
Rat[1] 5 mg/kg p.o. / / / / 7 %
体内研究
(In Vivo)

GPR61 Inverse agonist 3 (Compound 23) (300 mg/kg；口服；单次给药) 联合 ABT (HY-103389) 预处理不会使 10-11 周龄小鼠的 24 小时累计进食量产生统计学意义的升高[1]。

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

Animal Model: Mice (10-11 week-old)[1]
Dosage: 300 mg/kg
Administration: p.o.; single dose (administered 2 h after ABT pretreatment)
Result: Did not produce a statistically significant increase in 24-hour cumulative food intake compared to vehicle controls.
分子量

528.96

Formula

C21H23ClF2N6O4S
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 3 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 3Orphan GPCRGABA ReceptorPhosphodiesterase (PDE)Rrphan G protein-coupled receptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorCHO cellsadult micehuman hepatocytesMDR1GPR61cachexia/sarcopeniaphosphodiesterase 3A1γ-aminobutyric acid type A chloride channelspan-CYP inhibitorGαs proteinInhibitorinhibitorinhibit

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