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  1. Metabolic Enzyme/Protease
  2. Stearoyl-CoA Desaturase (SCD)
  3. SCD1 inhibitor-1

SCD1 inhibitor-1 (化合物 48) 是一種口服有效的和肝選擇性的硬脂酰-CoA 去飽和酶 1 (SCD1) 抑制劑,對(duì)重組人 SCD1 酶的 IC50 為 8.8 nM。SCD1 inhibitor-1 可用于糖尿病、肝脂肪變性和肥胖等疾病的研究。

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SCD1 inhibitor-1 Chemical Structure

SCD1 inhibitor-1 Chemical Structure

CAS No. : 1069094-65-0

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10 mg ¥5600
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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

SCD1 inhibitor-1 (Compound 48) is an orally active and liver-selective inhibitor of stearoyl-CoA desaturase 1 (SCD1) with an IC50 of 8.8 nM for recombinant human SCD1 enzyme. SCD1 inhibitor-1 can be used in the study of diseases such as diabetes, hepatic steatosis and obesity[1].

IC50 & Target

IC50: 8.8 nM (Recombinant human SCD1 enzyme)[1]

體內(nèi)研究
(In Vivo)

SCD1 inhibitor-1 (3-10 mg/kg;口服;43 天) 在高脂小鼠模型中具有改善作用[1]。
SCD1 inhibitor-1 (1-10 mg/kg;口服;單劑量) 在高糖大鼠模型中具有改善作用[1]。
在大小鼠中的藥代動(dòng)力學(xué)分析[1]

Species Route Dose (mg/kg) Cmax (μM) tmax (h) t1/2 (h) AUC0-inf (μM·h) BA (%) Cltot (L/h/kg)
Rat p.o. 10 8.0 0.5 4.7 16.5 16 /
Mouse p.o. 10 1.7 1.0 5.2 10.2 28 /
Rat i.v. 1 / / / / / 0.21
Mouse i.v. 1 / / / / / 0.61

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

Animal Model: C57BL/6J mice with high fat diet[1]
Dosage: 3 and 10 mg/kg
Administration: Oral administration (p.o.); 43 days
Result: Improved glucose tolerance in a dose-dependent manner and had a significant effect at a dose of 10 mg/kg.
Decreased body weight in a mild dose-dependent manner.
Animal Model: Sprague Dawley rats with high sucrose diet[1]
Dosage: 1 and 10 mg/kg
Administration: Oral administration (p.o.); Single dose
Result: Inhibited SCD1 inhibitory activity in a dose-dependent manner in epididymal adipose tissue and the liver 6 h after oral administration and to a lesser extent in the eyelid.
Had a selective tissue distribution of liver/eyelid.
分子量

451.54

Formula

C21H22N3NaO3S2

CAS 號(hào)
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

4°C, sealed storage, away from moisture

*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)用現(xiàn)配,即刻使用。

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

DMSO 中的溶解度 : 8.33 mg/mL (18.45 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開(kāi)封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.2146 mL 11.0732 mL 22.1464 mL
5 mM 0.4429 mL 2.2146 mL 4.4293 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液;該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)用現(xiàn)配,即刻使用。

  • 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(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)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: 99.78%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液;該產(chǎn)品在溶液狀態(tài)不穩(wěn)定,建議您現(xiàn)用現(xiàn)配,即刻使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2146 mL 11.0732 mL 22.1464 mL 55.3661 mL
5 mM 0.4429 mL 2.2146 mL 4.4293 mL 11.0732 mL
10 mM 0.2215 mL 1.1073 mL 2.2146 mL 5.5366 mL
15 mM 0.1476 mL 0.7382 mL 1.4764 mL 3.6911 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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產(chǎn)品名稱:
SCD1 inhibitor-1
目錄號(hào):
HY-112812
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