2. GPCR/G Protein
  3. Kisspeptin Receptor
  4. GPR54 antagonist-1

GPR54 antagonist‑1 是一种 GPR54 拮抗剂，对人和大鼠 GPR54 的 IC50 值分别为 3.6 nM 和 15 nM。GPR54 antagonist‑1 具有血脑屏障穿透能力。GPR54 antagonist‑1 可阻断人和大鼠 GPR54 受体的功能。GPR54 antagonist‑1 可降低去势雄性大鼠的血浆黄体生成素水平。GPR54 antagonist‑1 可用于前列腺癌和子宫内膜异位症的研究。

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GPR54 antagonist-1

GPR54 antagonist-1 Chemical Structure

CAS No. : 925924-27-2

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GPR54 antagonist-1 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

GPR54 antagonist‑1 is a GPR54 antagonist with IC50 values of 3.6 nM and 15 nM against human and rat GPR54, respectively. GPR54 antagonist‑1 shows blood‑brain barrier penetration. GPR54 antagonist‑1 blocks the function of human and rat GPR54 receptors. GPR54 antagonist‑1 suppresses plasma luteinizing hormone levels in castrated male rats. GPR54 antagonist‑1 can be used for the study of prostate cancer and endometriosis[1].

体外研究
(In Vitro)

GPR54 antagonist-1 (孵育 60 分钟) 可强效抑制 125I-metastin (40-54) 与表达人源或大鼠源 GPR54 的细胞膜结合，其 IC50 值分别为 3.6 nM 和 15 nM[1]。
GPR54 antagonist-1 可在表达人 GPR54 的 CHO 细胞中完全抑制 metastin (40-54) 诱导的 Ca2+ 动员，其 IC50 为 0.93 μM[1]。
GPR54 antagonist-1 (10 μM; 2 h) 在 Caco-2 单层细胞中表现出低水平的 P-糖蛋白介导外排[1]。

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

GPR54 antagonist-1 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Plasma Concentration Brain Concentration
Rat[1] 0.2 mg/kg i.v. 14.0 ng/mL 13.2 ng/g
体内研究
(In Vivo)

GPR54 antagonist-1 (1.1 mg/kg；静脉注射；每 10 分钟 1 次，共 5 次) 降低去势雄性大鼠的血浆 LH 水平[1]。
GPR54 antagonist-1 (0.2 mg/kg；静脉注射；单次给药) 在给药后 30 分钟时，在雄性大鼠体内的脑/血浆浓度比值达 0.94[1]。

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

Animal Model: Wister (male, 11 weeks old, castrated 7 days prior to testing)[1]
Dosage: 0.22 mg/kg (repeated 5 times, total 1.1 mg/kg)
Administration: i.v.; 5 times at 10-minute intervals
Result: Reduced plasma LH levels by 32% compared to vehicle control at 60 minutes post-administration.
Reduced plasma LH levels significantly at 180 minutes post-administration.
分子量

519.95

Formula

C27H23ClFN5O3
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

GPR54 antagonist-1 相关分类

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  • 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:

GPR54 antagonist-1925924-27-2Kisspeptin ReceptorKiss1RGPR54Caco-2 monolayersrat GPR54prostate cancerendometriosisCa2+ mobilizationCHO cell membranesluteinizing hormonecastrated male ratshuman GPR54Inhibitorinhibitorinhibit

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