1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. Clobetasol propionate

Clobetasol propionate  (Synonyms: 丙酸氯倍他索)

目录号: HY-13600 纯度: 99.85%
COA 产品使用指南

Clobetasol propionate 是一种有效的,选择性的 CYP3A5 抑制剂,IC50 为 0.206 μM。Clobetasol propionate 不会抑制 CYP3A4 或其他主要 CYP。Clobetasol propionate 是一种皮质类固醇,具有用于研究牛皮癣和其他皮肤病的潜力。

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Clobetasol propionate Chemical Structure

Clobetasol propionate Chemical Structure

CAS No. : 25122-46-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥715
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100 mg ¥650
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200 mg ¥980
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500 mg ¥1980
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5 g   询价  

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Customer Review

Other Forms of Clobetasol propionate:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Clobetasol propionate is a potent and selective CYP3A5 inhibitor with an IC50 of 0.206 μM. Clobetasol propionate has no inhibiting on CYP3A4 or other major CYPs. Clobetasol propionate is a corticosteroid and has the potential for psoriasis and other dermatoses research[1][2][3].

IC50 & Target[1]

CYP3A5

0.206 μM (IC50)

CYP3A4

15.6 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
ASPC1 IC50
0.021 μM
Compound: Clob
Inhibition of CYP3A5 in doxycycline-induced CYP3A5 overexpressing wild type human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate pretreated with doxycycline for 24 hrs followed by incubation with compound for
Inhibition of CYP3A5 in doxycycline-induced CYP3A5 overexpressing wild type human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate pretreated with doxycycline for 24 hrs followed by incubation with compound for
[PMID: 31965799]
ASPC1 IC50
0.044 μM
Compound: Clob
Inhibition of CYP3A5 in wild type human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate after 24 hrs by LC-MS/MS analysis
Inhibition of CYP3A5 in wild type human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate after 24 hrs by LC-MS/MS analysis
[PMID: 31965799]
ASPC1 IC50
0.078 μM
Compound: Clob
Inhibition of CYP3A5 in lentiviral pLVX-TRE3G-ZsGreen1-CYP3A5 transduced wild type human AsPC1 cells overexpressing CYP3A5 assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate after 24 hrs by LC-MS/MS analysis
Inhibition of CYP3A5 in lentiviral pLVX-TRE3G-ZsGreen1-CYP3A5 transduced wild type human AsPC1 cells overexpressing CYP3A5 assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate after 24 hrs by LC-MS/MS analysis
[PMID: 31965799]
ASPC1 IC50
0.103 μM
Compound: Clob
Inhibition of CYP3A5 in CRISPR/Cas9-mediated CYP3A5 knock-out and doxycycline-induced CYP3A5 overexpressing human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate pretreated with doxycycline for 24 hrs followed
Inhibition of CYP3A5 in CRISPR/Cas9-mediated CYP3A5 knock-out and doxycycline-induced CYP3A5 overexpressing human AsPC1 cells assessed as decrease in 1-hydroxymidazolam formation using midazolam as substrate pretreated with doxycycline for 24 hrs followed
[PMID: 31965799]
体外研究
(In Vitro)

Clobetasol propionate has an IC50 of 15.6 μM for CYP3A4[1].
Clobetasol propionate (1 μM; 24 hours) selectively inhibits CYP3A5 and does not increase the protein level of CYP3A4. Clobetasol propionate does not affect cell growth in any cell line (AsPC-1 wild-type (WT), AsPC-1CYP3A5–/– cells with CYP3A5 overexpression (“3A5–/– + 3A5OE” cells), and AsPC-1CYP3A5–/– cells with CYP3A4 overexpression (“3A5–/– + 3A4OE” cells))[1].

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

体内研究
(In Vivo)

Clobetasol propionate (applied topically; daily for 14 days) reduces the epidermal thickness of both normal and psoriatic skin in human psoriatic skin-SCID mouse transplant model topical application[3].

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

Clinical Trial
分子量

466.97

Formula

C25H32ClFO5

CAS 号
性状

固体

颜色

White to off-white

中文名称

丙酸氯倍他索

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 100 mg/mL (214.15 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1415 mL 10.7073 mL 21.4147 mL
5 mM 0.4283 mL 2.1415 mL 4.2829 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 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

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.35 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.35 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.85%

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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1415 mL 10.7073 mL 21.4147 mL 53.5366 mL
5 mM 0.4283 mL 2.1415 mL 4.2829 mL 10.7073 mL
10 mM 0.2141 mL 1.0707 mL 2.1415 mL 5.3537 mL
15 mM 0.1428 mL 0.7138 mL 1.4276 mL 3.5691 mL
20 mM 0.1071 mL 0.5354 mL 1.0707 mL 2.6768 mL
25 mM 0.0857 mL 0.4283 mL 0.8566 mL 2.1415 mL
30 mM 0.0714 mL 0.3569 mL 0.7138 mL 1.7846 mL
40 mM 0.0535 mL 0.2677 mL 0.5354 mL 1.3384 mL
50 mM 0.0428 mL 0.2141 mL 0.4283 mL 1.0707 mL
60 mM 0.0357 mL 0.1785 mL 0.3569 mL 0.8923 mL
80 mM 0.0268 mL 0.1338 mL 0.2677 mL 0.6692 mL
100 mM 0.0214 mL 0.1071 mL 0.2141 mL 0.5354 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:
Clobetasol propionate
目录号:
HY-13600
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