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

GW-803430 (GW-3430) 是一種有效的選擇性黑色素濃縮激素受體 1 (MCH R1) 拮抗劑,pIC50 為 9.3。GW-803430 在肥胖動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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10 mM * 1 mL in DMSO ¥1909
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5 mg ¥1800
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Customer Review

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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]

細(xì)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]
體外研究
(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.

體內(nèi)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 號
性狀

固體

顏色

Off-white to yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 12.5 mg/mL (25.93 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請?jiān)?個月內(nèi)使用,-20°C儲存時,請?jiān)?個月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計(jì)算器
請輸入動物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.10%

參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請?jiān)?個月內(nèi)使用,-20°C儲存時,請?jiān)?個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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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Inquiry Information

產(chǎn)品名稱:
GW-803430
目錄號:
HY-11083
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