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

Clobetasol propionate  (Synonyms: 丙酸氯倍他索)

目錄號: HY-13600 純度: 99.85%
COA 產(chǎn)品使用指南

Clobetasol propionate 是一種有效的,選擇性的 CYP3A5 抑制劑,IC50 為 0.206 μM。Clobetasol propionate 不會抑制 CYP3A4 或其他主要 CYP。Clobetasol propionate 是一種皮質(zhì)類固醇,具有用于研究牛皮癬和其他皮膚病的潛力。

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Clobetasol propionate Chemical Structure

Clobetasol propionate Chemical Structure

CAS No. : 25122-46-7

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規(guī)格 價格 是否有貨 數(shù)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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1 g   詢價  
5 g   詢價  

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Customer Review

Other Forms of Clobetasol propionate:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

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)

細胞效力
(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]
體外研究
(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.

體內(nèi)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 號
性狀

固體

顏色

White to off-white

中文名稱

丙酸氯倍他索

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細胞實驗: 

DMSO 中的溶解度 : ≥ 100 mg/mL (214.15 mM; 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)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)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,避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

動物實驗:

請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用;
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑: 10% DMSO    90% Corn Oil

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

    此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液,此方案實驗周期在半個月以上的動物實驗酌情使用。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中,混合均勻。

動物溶解方案計算器
請輸入動物實驗的基本信息:

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

由于實驗過程有損耗,建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購。 ,Tween 80,均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度,以下方案僅供參考,如有需要,請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液,加入 μL  μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上,請謹慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.85%

參考文獻

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,避免反復凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(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 2.1415 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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產(chǎn)品名稱:
Clobetasol propionate
目錄號:
HY-13600
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