2. GPCR/G Protein
  3. RXFP Receptor
  4. RXFP1 receptor agonist-9

RXFP1 receptor agonist-9 是一种强效的 RXFP1 激动剂，其 EC50 值为 2.5 μM，Ymax 值为 65%。RXFP1 receptor agonist-9 具有显著的微粒体稳定性，良好的药物代谢性质和药效学活性。RXFP1 receptor agonist-9 可用于研究心力衰竭。

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RXFP1 receptor agonist-9

RXFP1 receptor agonist-9 Chemical Structure

CAS No. : 2924765-23-9

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RXFP1 receptor agonist-9 相关抗体

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  • 生物活性

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生物活性

RXFP1 receptor agonist-9 is a potent RXFP1 agonist with an EC50 of 2.5 μM and Ymax of 65%. RXFP1 receptor agonist-9 exhibits good microsomal stability, reasonable PK and pharmacological activity. RXFP1 receptor agonist-9 can be used to the study of heart failure[1].

药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Rat 1 mg/kg i.v. T1/2 4.43 hr
Rat 10 mg/kg p.o. F 6 %
Rat 1 mg/kg i.v. AUC 9.6 μM·h
Rat 1 mg/kg i.v. Vss 0.09 L/kg
Rat 1 mg/kg i.v. CL 2.5 mL/min/kg
体内研究
(In Vivo)

RXFP1 receptor agonist-9 (Compound 39) (1.5-5 mg/min/kg, i.v., 每天1次，持续 21 天) 在异氟烷麻醉的未接种大鼠中诱导出剂量依赖性的心率增加 (与松弛素的血流动力学特征一致) [1]。
RXFP1 receptor agonist-9 (25 mg/kg, i.v., 分别在第 6 天和第 7 天注射) 可引起耻骨间韧带 (IPL) 显著扩张，这重现了松弛素在 C57BL/6 小鼠中的作用[1]。

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

Animal Model: Isoflurane-anesthetized male Sprague Dawley (SD) rat model
Dosage: 5 mg/min/kg
Administration: IV, 60 min
Result: Induced a 25% increase on heart rate.
Animal Model: Isoflurane-anesthetized male Sprague Dawley (SD) rat model
Dosage: 0.5 mg/min/kg, 1.5 mg/min/kg, 5 mg/min/kg,
Administration: Intravenous injection (i.v.), 60 min
Result: Observed a dose-dependent increase at 1.5 and 5 mg/min/kg while no major effect was observed at 0.5 mg/min/kg.
Animal Model: Baseline microCT scan acquired for the estrogen primed C57BL/6 female mice pubis (primed with estrogen on day 0)
Dosage: 25 mg/kg,
Administration: IV, respectively on day 6 and 7
Result: Showed 500% symphysis widening, and thus IPL expansion.
分子量

727.67

Formula

C37H34F5N3O7
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

RXFP1 receptor agonist-9 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

RXFP1 receptor agonist-92924765-23-9RXFP ReceptorRelaxin family peptideNorbornyl BisamidesRelaxinHuman relaxin-2Heart failureInhibitorinhibitorinhibit

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