1. GPCR/G Protein Neuronal Signaling
  2. MCHR1 (GPR24)
  3. GW-803430

GW-803430  (Synonyms: GW-3430)

目录号: HY-11083 纯度: 99.10%
COA 产品使用指南 技术支持

GW-803430 (GW-3430) 是一种有效的选择性黑色素浓缩激素受体 1 (MCH R1) 拮抗剂,pIC50 为 9.3。GW-803430 在肥胖动物模型中具有口服活性。

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GW-803430 Chemical Structure

GW-803430 Chemical Structure

CAS No. : 515141-51-2

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     可免费申领三个不同产品的试用装。

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Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1909
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1 mg ¥850
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5 mg ¥1800
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25 mg ¥5750
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target

pIC50: 9.3 (MCH R1)[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
16 nM
Compound: 43
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
Antagonist activity at human MCHR1 expressed in HEK293 cells assessed as inhibition of MCH-stimulated Ca2+ influx preincubated for 120 mins followed by MCH challenge by FLIPR assay
[PMID: 26022839]
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[2].

MCE 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[1].
GW-803430 is a suitable compound for its good pharmacokinetic properties (bioavailability=31%, t1/2=11 h) and brain penetration (6:1 brain:plasma concentration) in mice[1].

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

Animal Model: High fat diet-induced obese AKR/J mice[1]
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.
分子量

481.99

Formula

C25H24ClN3O3S

CAS 号
性状

固体

颜色

Off-white to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 12.5 mg/mL (25.93 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0747 mL 10.3737 mL 20.7473 mL
5 mM 0.4149 mL 2.0747 mL 4.1495 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.10%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0747 mL 10.3737 mL 20.7473 mL 51.8683 mL
5 mM 0.4149 mL 2.0747 mL 4.1495 mL 10.3737 mL
10 mM 0.2075 mL 1.0374 mL 2.0747 mL 5.1868 mL
15 mM 0.1383 mL 0.6916 mL 1.3832 mL 3.4579 mL
20 mM 0.1037 mL 0.5187 mL 1.0374 mL 2.5934 mL
25 mM 0.0830 mL 0.4149 mL 0.8299 mL 2.0747 mL
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.

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产品名称:
GW-803430
目录号:
HY-11083
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