GW 803430|515141-51-2|(GW-3430)-陌孚医药/Medlife

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GW 803430 (Synonyms: GW-3430)

目录号: PC11377 纯度: ≥98%

CAS No. :515141-51-2

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中文名称

GW 803430

英文名称

GW 803430

英文别名

Thieno[3,2-d]pyrimidin-4(3H)-one,6-(4-chlorophenyl)-3-[3-methoxy-4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-;6-(4-chlorophenyl)-3-[3-methoxy-4-(2-pyrrolidin-1-ylethoxy)phenyl]thieno[3,2-d]pyrimidin-4-one;GW 803430;6-(4-chloro-phenyl)-3-[3-methoxy-4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-3H-thieno[3,2-d]pyrimidin-4-one;GW-3430;GW-803430A;GW-803430

Cas No.

515141-51-2

分子式

C₂₅H₂₄N₃O₃Scl

分子量

481.99

包装储存

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

GW-803430 (GW-3430) is a potent and selective melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pIC₅₀ of 9.3. GW-803430 is orally active in an animal model of obesity.

性状

Solid

IC50 & Target[1][2]

pIC50: 9.3 (MCH R1)

体外研究(In Vitro)

GW-803430 demonstrates a potent antagonist activity towards MCH induced MCHR1 receptor with an IC₅₀ value of ~13?nM.

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

体内研究(In Vivo)

GW-803430 (0.3, 3, and 15 mg/kg; oral administration; once daily) causes a sustained dose-dependent weight loss relative to vehicle controls.
GW-803430 is a suitable compound for its good pharmacokinetic properties (bioavailability=31%, t_1/2=11 h) and brain penetration (6:1 brain:plasma concentration) in mice.

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

Animal Model:	High fat diet-induced obese AKR/J mice
Dosage:	0.3, 3, and 15 mg/kg
Administration:	Orally, qd,12 days
Result:	Caused a sustained dose-dependent weight loss of -6.2%, -12.1%, and -13.1%, respectively, relative to vehicle controls.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Hertzog DL, et al. The discovery and optimization of pyrimidinone-containing MCH R1 antagonists. Bioorg Med Chem Lett. 2006 Sep 15;16(18):4723-7. [Information]

[2]. Velusami CC, et al. Effect of Nelumbo nucifera Petal Extracts on Lipase, Adipogenesis, Adipolysis, and Central Receptors of Obesity. Evid Based Complement Alternat Med. 2013;2013:145925. [Information]

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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