Naftopidil (Synonyms: 萘哌地爾; KT-611; BM-15275)

目錄號(hào): HY-B0391 純度: 98.47%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南技術(shù)支持

Naftopidil (KT-611) 是一種選擇性的 alpha1-腎上腺素受體 (α1-adrenoceptor) 拮抗劑，對(duì)克隆的人類(lèi) α_1a、α_1b 和 α_1d 亞型腎上腺素受體的親和力 K_i 值分別為 3.7 nM、20 nM 、1.2 nM，具有抗增殖作用。Naftopidil 可用于前列腺增生的研究。

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

Naftopidil Chemical Structure

CAS No. : 57149-07-2

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規(guī)格	價(jià)格	是否有貨
10 mM * 1 mL in DMSO	￥500	In-stock
500 mg	￥400	In-stock
1 g	￥640	In-stock
5 g	￥900	In-stock
10 g	￥1500	In-stock
50 g		詢價(jià)

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Customer Review

Other Forms of Naftopidil:

Naftopidil-d₅ 詢價(jià)
Naftopidil dihydrochloride 詢價(jià)
Naftopidil hydrochloride 詢價(jià)
Naftopidil (Standard) 詢價(jià)

Naftopidil 相關(guān)產(chǎn)品

•相關(guān)化合物庫(kù):

•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)蛋白產(chǎn)品:

查看 Adrenergic Receptor 亞型特異性產(chǎn)品:

查看所有亞型

α adrenergic receptor β adrenergic receptor

生物活性
純度 & 產(chǎn)品資料
參考文獻(xiàn)

生物活性

Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with K_is of 3.7 nM, 20 nM and 1.2 nM for the cloned human α_1a-, α_1b- and α_1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia^[1]^[2].

IC₅₀ & Target^[1]

Alpha-1A adrenergic receptor

3.7 nM (Ki)

Alpha-1B adrenergic receptor

20 nM (Ki)

Alpha-1D adrenergic receptor

1.2 nM (Ki)

細(xì)胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
786-0	IC₅₀	13.3 μM Compound: 1	Antiproliferative activity against human 786-O cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human 786-O cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31759851]
DU-145	IC₅₀	> 50 μM Compound: 1	Cytotoxicity against human DU145 cells after 48 hrs by WST-8 assay Cytotoxicity against human DU145 cells after 48 hrs by WST-8 assay	[PMID: 25874333]
DU-145	IC₅₀	21.1 μM Compound: 1	Antiproliferative activity against human DU145 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human DU145 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31759851]
DU-145	IC₅₀	34.58 μM Compound: Naftopidil	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	34.58 μM Compound: Naftopidil	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	34.58 μM Compound: Naftopidil	Cytotoxicity against human DU145 cells assessed as inhibition of cell viability after 24 hrs by CCK-8 assay Cytotoxicity against human DU145 cells assessed as inhibition of cell viability after 24 hrs by CCK-8 assay	[PMID: 25488843]
HEK293	IC₅₀	47.3 μM Compound: 1	Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31759851]
KK-47 cell line	IC₅₀	19 μM Compound: 1	Antiproliferative activity against human KK47 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human KK47 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31759851]
LNCaP	IC₅₀	> 50 μM Compound: 1	Cytotoxicity against human LNCAP cells after 48 hrs by WST-8 assay Cytotoxicity against human LNCAP cells after 48 hrs by WST-8 assay	[PMID: 25874333]
LNCaP	IC₅₀	22.36 μM Compound: Naftopidil	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	22.36 μM Compound: Naftopidil	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	22.36 μM Compound: Naftopidil	Cytotoxicity against human LNCAP cells assessed as inhibition of cell viability after 24 hrs by CCK-8 assay Cytotoxicity against human LNCAP cells assessed as inhibition of cell viability after 24 hrs by CCK-8 assay	[PMID: 25488843]
PC-3	IC₅₀	> 50 μM Compound: 1	Cytotoxicity against human PC3 cells after 48 hrs by WST-8 assay Cytotoxicity against human PC3 cells after 48 hrs by WST-8 assay	[PMID: 25874333]
PC-3	IC₅₀	31.2 μM Compound: 1	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31759851]
PC-3	IC₅₀	42.1 μM Compound: Naftopidil	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	42.1 μM Compound: Naftopidil	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]
PC-3	IC₅₀	42.1 μM Compound: Naftopidil	Cytotoxicity against human PC3 cells assessed as inhibition of cell viability after 24 hrs by CCK-8 assay Cytotoxicity against human PC3 cells assessed as inhibition of cell viability after 24 hrs by CCK-8 assay	[PMID: 25488843]
PNT1A	IC₅₀	27 μM Compound: 1	Cytotoxicity against human PNT1A cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human PNT1A cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31759851]
RWPE-1	IC₅₀	> 50 μM Compound: Naftopidil	Antiproliferative activity against human RWPE1 cells after 24 hrs by CCK-8 assay Antiproliferative activity against human RWPE1 cells after 24 hrs by CCK-8 assay	[PMID: 30482547]
RWPE-1	IC₅₀	> 50 μM Compound: Naftopidil	Cytotoxicity against human RWPE1 cells assessed as inhibition of cell viability after 24 hrs by CCK-8 assay Cytotoxicity against human RWPE1 cells assessed as inhibition of cell viability after 24 hrs by CCK-8 assay	[PMID: 25488843]
T-24	IC₅₀	18.5 μM Compound: 1	Antiproliferative activity against human T24 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human T24 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 31759851]

體外研究
(In Vitro)

Naftopidil suppresses human prostate tumor growth by altering interactions between tumor cells and stroma^[2].
Naftopidil (10 μM for PCa cells, 0.1-10 μM for PrSC; 3 days) shows growth inhibitory effects on PCa cells and PrSC^[2].
Naftopidil (50 μM for E9 cells, 25 μM for PrSC; 48 hours) increases the level of cell-cycle regulatory protein p27 in E9 cells, but not PrSC^[2].

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

Cell Proliferation Assay^[2]

Cell Line:	PCa cells, PrSC
Concentration:	10 μM (PCa cells); 0.1 μM, 1 μM, 10 μM (PrSC)
Incubation Time:	3 days
Result:	Exhibited growth inhibitory effects on PCa cells and PrSC in dose-dependent manners.

Western Blot Analysis^[2]

Cell Line:	PCa cells, PrSC
Concentration:	50 μM (E9 cells), 25 μM (PrSC)
Incubation Time:	48 hours
Result:	Increased the level of cell-cycle regulatory protein p27 in E9 cells, but not PrSC.

體內(nèi)研究
(In Vivo)

Naftopidil (10 mg/kg; p.o; daily; for 28 days) decreases microvessel density (MVD) in E9+PrSC tumors mice model^[2].

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

Animal Model:	Male athymic mice (7-8 weeks), with E9+PrSC xenograft^[2]
Dosage:	10 mg/kg
Administration:	Oral administration, daily, for 28 days
Result:	Decreased tumor weights.

Clinical Trial

分子量

392.49

Formula

C₂₄H₂₈N₂O₃

CAS 號(hào)

57149-07-2

性狀

固體

顏色

White to off-white

中文名稱(chēng)

萘哌地爾

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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(shí)驗(yàn)：

DMSO 中的溶解度 : 33.33 mg/mL (84.92 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)

H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.5478 mL	12.7392 mL	25.4784 mL
5 mM	0.5096 mL	2.5478 mL	5.0957 mL
10 mM	0.2548 mL	1.2739 mL	2.5478 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；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)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(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

方案一

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.37 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。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)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(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.37 mM); 懸濁液; 超聲助溶

此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)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。
方案三

請(qǐng)依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.37 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(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

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

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

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

請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動(dòng)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(guò) 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購(gòu)。，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

儲(chǔ)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(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。

動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)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(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。

請(qǐng)確保第一步儲(chǔ)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: 98.47%

選擇批次：

Data Sheet (629 KB) SDS (393 KB)

COA (288 KB) LCMS (88 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[1]. R Takei, et al. Naftopidil, a novel alpha1-adrenoceptor antagonist, displays selective inhibition of canine prostatic pressure and high affinity binding to cloned human alpha1-adrenoceptors. Jpn J Pharmacol. 1999 Apr;79(4):447-54. [Content Brief]

[2]. Yasuhide Hori, et al. Naftopidil, a selective {alpha}1-adrenoceptor antagonist, suppresses human prostate tumor growth by altering interactions between tumor cells and stroma. Cancer Prev Res (Phila). 2011 Jan;4(1):87-96. [Content Brief]

Naftopidil 相關(guān)分類(lèi)

Endocrinology Cardiovascular Disease

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5478 mL	12.7392 mL	25.4784 mL	63.6959 mL
	5 mM	0.5096 mL	2.5478 mL	5.0957 mL	12.7392 mL
	10 mM	0.2548 mL	1.2739 mL	2.5478 mL	6.3696 mL
	15 mM	0.1699 mL	0.8493 mL	1.6986 mL	4.2464 mL
	20 mM	0.1274 mL	0.6370 mL	1.2739 mL	3.1848 mL
	25 mM	0.1019 mL	0.5096 mL	1.0191 mL	2.5478 mL
	30 mM	0.0849 mL	0.4246 mL	0.8493 mL	2.1232 mL
	40 mM	0.0637 mL	0.3185 mL	0.6370 mL	1.5924 mL
	50 mM	0.0510 mL	0.2548 mL	0.5096 mL	1.2739 mL
	60 mM	0.0425 mL	0.2123 mL	0.4246 mL	1.0616 mL
	80 mM	0.0318 mL	0.1592 mL	0.3185 mL	0.7962 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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滬(浦)應(yīng)急管危經(jīng)許[2021]201709(QFYS)

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Naftopidil (Synonyms: 萘哌地爾; KT-611; BM-15275)

Customer Review

Other Forms of Naftopidil: