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  1. Metabolic Enzyme/Protease
  2. 5 alpha Reductase
  3. Finasteride

Finasteride  (Synonyms: 非那雄胺; MK-906)

目錄號: HY-13635 純度: 99.97%
COA 產(chǎn)品使用指南 技術(shù)支持

Finasteride (MK-906) 是一種具有口服活性的競爭性 5α-還原酶 (5α-reductase) 抑制劑,對 II 型 5α-還原酶的 IC50 值為 4.2 nM。Finasteride 對 II 型 5α-還原酶的親和力比對 I 型酶高約 100 倍。Finasteride 可用于研究前列腺增生 (BPH) 和雄激素性脫發(fā)。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報,我們不為任何個人用途提供產(chǎn)品和服務(wù)

Finasteride Chemical Structure

Finasteride Chemical Structure

CAS No. : 98319-26-7

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥563
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100 mg ¥512
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200 mg ¥880
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500 mg   詢價  
1 g   詢價  

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Other Forms of Finasteride:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Finasteride (MK-906) is an orally active and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia[1][2][3].

IC50 & Target

IC50: 4.2 nM (type II 5α-reductase)[1]

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
DU-145 IC50
13.53 μM
Compound: Finasteride
Cytotoxicity against human DU145 cells assessed as growth inhibition after 24 hrs by CCK8 assay
Cytotoxicity against human DU145 cells assessed as growth inhibition after 24 hrs by CCK8 assay
[PMID: 29615343]
DU-145 IC50
14.53 μM
Compound: Finasteride
Antiproliferative activity against human DU145 cells after 24 hrs by CCK-8 assay
Antiproliferative activity against human DU145 cells after 24 hrs by CCK-8 assay
[PMID: 30482547]
DU-145 IC50
3.9 μM
Compound: Finasteride
Cytotoxicity against Homo sapiens (human) DU145 cells after 48 hr by MTT assay
Cytotoxicity against Homo sapiens (human) DU145 cells after 48 hr by MTT assay
10.1007/s00044-010-9393-3
DU-145 IC50
3.9 μM
Compound: Finasteride
Antiproliferative activity against human DU145 cells assessed as growth inhibition after 48 hrs by MTT assay
Antiproliferative activity against human DU145 cells assessed as growth inhibition after 48 hrs by MTT assay
[PMID: 20171759]
DU-145 IC50
548 μM
Compound: Finasteride
Cytotoxicity against human DU145 cells by rapid colorimetric assay
Cytotoxicity against human DU145 cells by rapid colorimetric assay
[PMID: 26780831]
HEK293 IC50
> 50 μM
Compound: 1
Cytotoxicity against HEK293 cells after 24 hrs by MTT assay
Cytotoxicity against HEK293 cells after 24 hrs by MTT assay
[PMID: 28693914]
HEK293 IC50
218 nM
Compound: 2a
In vitro inhibition of human Steroid 5-alpha-reductase type I in transfected 293 cells using [3H]- delta4-Androstenedione as substrate
In vitro inhibition of human Steroid 5-alpha-reductase type I in transfected 293 cells using [3H]- delta4-Androstenedione as substrate
[PMID: 7739004]
HEK293 IC50
30.3 nM
Compound: 3
Inhibition of human type-2 5-alpha reductase expressed in HEK293 cells using [3H]-androstenedione as substrate after 30 mins by HPLC analysis
Inhibition of human type-2 5-alpha reductase expressed in HEK293 cells using [3H]-androstenedione as substrate after 30 mins by HPLC analysis
[PMID: 22776417]
HEK293 IC50
40 nM
Compound: Finasteride
Inhibition of human 5alpha-2 reductase expressed in HEK293 cells assessed as suppression of conversion of [3]androstenedione incubated for 30 mins by radioactivity-based HPLC analysis
Inhibition of human 5alpha-2 reductase expressed in HEK293 cells assessed as suppression of conversion of [3]androstenedione incubated for 30 mins by radioactivity-based HPLC analysis
[PMID: 26780831]
HEK293 IC50
453 nM
Compound: 3
Inhibition of human type-1 5-alpha reductase expressed in HEK293 cells using [3H]-androstenedione as substrate after 30 mins by HPLC analysis
Inhibition of human type-1 5-alpha reductase expressed in HEK293 cells using [3H]-androstenedione as substrate after 30 mins by HPLC analysis
[PMID: 22776417]
HEK293 IC50
453 nM
Compound: Finasteride
Inhibition of human 5alpha-1 reductase expressed in HEK293 cells assessed as suppression of conversion of [3]androstenedione incubated for 30 mins by radioactivity-based HPLC analysis
Inhibition of human 5alpha-1 reductase expressed in HEK293 cells assessed as suppression of conversion of [3]androstenedione incubated for 30 mins by radioactivity-based HPLC analysis
[PMID: 26780831]
LNCaP IC50
0.76 μM
Compound: Finasteride
Inhibition of steroid 5-alpha-reductase in human LNCAP cells assessed as reduction in 5- dihydrotestosterone formation incubated for 60 mins by LC-MS analysis
Inhibition of steroid 5-alpha-reductase in human LNCAP cells assessed as reduction in 5- dihydrotestosterone formation incubated for 60 mins by LC-MS analysis
[PMID: 32040314]
LNCaP IC50
13.53 μM
Compound: Finasteride
Antiproliferative activity against human LNCAP cells after 24 hrs by CCK-8 assay
Antiproliferative activity against human LNCAP cells after 24 hrs by CCK-8 assay
[PMID: 30482547]
LNCaP IC50
14.53 μM
Compound: Finasteride
Cytotoxicity against human LNCAP cells assessed as growth inhibition after 24 hrs by CCK8 assay
Cytotoxicity against human LNCAP cells assessed as growth inhibition after 24 hrs by CCK8 assay
[PMID: 29615343]
LNCaP IC50
19.8 μg/mL
Compound: Finasteride
Inhibitory activity against 5-alpha-reductase type 1 in cell culture system using LNCaP cells (androgen-sensitive human prostatic cancer cell line)
Inhibitory activity against 5-alpha-reductase type 1 in cell culture system using LNCaP cells (androgen-sensitive human prostatic cancer cell line)
[PMID: 11527731]
LNCaP IC50
53 μM
Compound: Finasteride
Inhibitory activity against 5-alpha-reductase type 1 in cell culture system using LNCaP cells (androgen-sensitive human prostatic cancer cell line)
Inhibitory activity against 5-alpha-reductase type 1 in cell culture system using LNCaP cells (androgen-sensitive human prostatic cancer cell line)
[PMID: 11527731]
Macrophage IC50
28.2 μM
Compound: Finasteride
Cytotoxicity against Balb/C mouse macrophages assessed as cell viability after 24 hrs by MTT assay
Cytotoxicity against Balb/C mouse macrophages assessed as cell viability after 24 hrs by MTT assay
[PMID: 20171759]
MCF7 IC50
44.14 μM
Compound: 1
Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 24 hrs by MTT assay
[PMID: 28693914]
MDA-MB-231 IC50
> 50 μM
Compound: 1
Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay
[PMID: 28693914]
PC-3 IC50
> 80 μM
Compound: 1
Cytotoxicity against human PC3 cells after 48 hrs by MTT assay
Cytotoxicity against human PC3 cells after 48 hrs by MTT assay
[PMID: 28757062]
PC-3 IC50
17.8 μM
Compound: Finasteride
Antiproliferative activity against AR-deficient human PC3 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay
Antiproliferative activity against AR-deficient human PC3 cells assessed as reduction in cell viability after 24 hrs by CCK-8 assay
[PMID: 31493989]
PC-3 IC50
17.8 μM
Compound: Finasteride
Antiproliferative activity against human PC3 cells after 24 hrs by CCK-8 assay
Antiproliferative activity against human PC3 cells after 24 hrs by CCK-8 assay
[PMID: 30482547]
PC-3 IC50
17.83 μM
Compound: Finasteride
Cytotoxicity against human PC3 cells assessed as growth inhibition after 24 hrs by CCK8 assay
Cytotoxicity against human PC3 cells assessed as growth inhibition after 24 hrs by CCK8 assay
[PMID: 29615343]
體外研究
(In Vitro)

Finasteride (10 μM;6-24 小時) 誘導(dǎo) PC-3 細(xì)胞中 HO-1 和 Nrf2 蛋白的表達(dá)[2]。
Finasteride降低 P. crustosum 中的 [3 H]睪酮 (T) 到 [3H]二氫睪酮 (DHT)。[1]。

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

Western Blot Analysis[2]

Cell Line: PC-3, DU-145, and LNCaP cells
Concentration: 10 μM
Incubation Time: 6, 12, 24 h
Result: Increased the expression of HO-1 protein in a time-dependent manner in PC-3 cells.
Induced the expression of Nrf2 protein in DU-145 and PC-3 cells, but not in LNCaP cells.
體內(nèi)研究
(In Vivo)

Finasteride (0.1-0.5 mg/kg;每天口服一次,持續(xù) 16 周) 可減小 BPH 犬的前列腺大小,而不會對精液質(zhì)量或血清睪酮濃度產(chǎn)生不利影響[3]。

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

Animal Model: Male dogs with spontaneous BPH (2.7-11 years old; 10.3-49 kg)[3]
Dosage: 0.1-0.5 mg/kg
Administration: P.o. once daily for 16 weeks
Result: Decreased prostatic diameter (20%), prostatic volume (43%), and serum DHT concentration (58%).
Decreased semen volume but did not adversely effect on semen quality or serum testosterone concentration.
No adverse effects on dogs.
Clinical Trial
分子量

372.54

Formula

C23H36N2O2

CAS 號
性狀

固體

顏色

White to off-white

中文名稱

非那雄胺;非那斯特萊;非那司提;非那甾胺

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(xì)胞實驗: 

DMSO 中的溶解度 : 100 mg/mL (268.43 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 2.6843 mL 13.4214 mL 26.8428 mL
5 mM 0.5369 mL 2.6843 mL 5.3686 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, 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(dāng)?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(dāng)保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.71 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 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

    2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
  • 方案 二

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

    Solubility: ≥ 2.5 mg/mL (6.71 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。

以下溶解方案,請直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 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: 50% PEG300    50% Saline

    Solubility: 2 mg/mL (5.37 mM); 懸濁液; 超聲助溶

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(jǐn)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: 99.97%

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, 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 2.6843 mL 13.4214 mL 26.8428 mL 67.1069 mL
5 mM 0.5369 mL 2.6843 mL 5.3686 mL 13.4214 mL
10 mM 0.2684 mL 1.3421 mL 2.6843 mL 6.7107 mL
15 mM 0.1790 mL 0.8948 mL 1.7895 mL 4.4738 mL
20 mM 0.1342 mL 0.6711 mL 1.3421 mL 3.3553 mL
25 mM 0.1074 mL 0.5369 mL 1.0737 mL 2.6843 mL
30 mM 0.0895 mL 0.4474 mL 0.8948 mL 2.2369 mL
40 mM 0.0671 mL 0.3355 mL 0.6711 mL 1.6777 mL
50 mM 0.0537 mL 0.2684 mL 0.5369 mL 1.3421 mL
60 mM 0.0447 mL 0.2237 mL 0.4474 mL 1.1184 mL
80 mM 0.0336 mL 0.1678 mL 0.3355 mL 0.8388 mL
100 mM 0.0268 mL 0.1342 mL 0.2684 mL 0.6711 mL
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產(chǎn)品名稱:
Finasteride
目錄號:
HY-13635
需求量: