Bufalin (Synonyms: 蟾毒靈)

目錄號(hào): HY-N0877 純度: 99.86%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南

摩爾計(jì)算器

Bufalin 是蟾酥中的有效活性成分，為有效的 Na⁺/K⁺-ATPase 抑制劑，可與其基 α1, α2 和 α3 結(jié)合，K_d 值分別為 42.5，45 和 40 nM。具有抗腫瘤活性。

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)

Bufalin Chemical Structure

CAS No. : 465-21-4

1. 客戶無需承擔(dān)相應(yīng)的運(yùn)輸費(fèi)用。

2. 同一機(jī)構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機(jī)構(gòu)（單位）一年內(nèi)

可免費(fèi)申領(lǐng)三個(gè)不同產(chǎn)品的試用裝。

3. 試用裝只面向終端客戶。

規(guī)格	價(jià)格	是否有貨
10 mM * 1 mL in DMSO	￥1078	In-stock
5 mg	￥980	In-stock
10 mg	￥1700	In-stock
50 mg		詢價(jià)
100 mg		詢價(jià)

or 大包裝詢價(jià)

* Please select Quantity before adding items.

Customer Review

Other Forms of Bufalin:

Bufalin (Standard) 詢價(jià)

MCE 顧客使用本產(chǎn)品發(fā)表的 6 篇科研文獻(xiàn)

•Pharmacol Res. 2021 Nov 2;105927. [Abstract]
•Apoptosis. 2023 May 30. [Abstract]
•Int J Mol Sci. 2022 Nov 1;23(21):13354. [Abstract]
•Int J Mol Med. 2020 Dec;46(6):2137-2149. [Abstract]
•Cancers. 2020 Aug 4;12(8):2169. [Abstract]
•Chem Res Toxicol. 2019 Dec 16;32(12):2479-2487. [Abstract]

Cell Viability Assay

: Bufalin purchased from MCE. Usage Cited in: Apoptosis. 2023 May 30. [Abstract]; Bufalin (12.5, 25, 50, 100, 200 nM; 24, 48, 72 h) significantly reduces the viability of MKN-45 and HGC-27 GC cells in a dose- and time-dependent manner.

Bufalin 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:

生物活性
純度 & 產(chǎn)品資料
參考文獻(xiàn)

生物活性

Bufalin is an active component isolated from Chan Su, acts as a potent Na⁺/K⁺-ATPase inhibitor, binds to the subunit α1, α2 and α3, with K_d of 42.5, 45 and 40 nM, respectively^[1]^[2]. Anti-cancer activity^[2].

IC₅₀ & Target

Kd: 42.5 nM (Na,K-ATPase α1), 45 nM (Na,K-ATPase α2), 40 nM (Na,K-ATPase α3)^[1]

細(xì)胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
786-0	EC₅₀	7.5 nM Compound: 4	Cytotoxicity against human 786-O cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human 786-O cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
A549	IC₅₀	0.6 μM Compound: 7	Cytotoxicity against human A549 cells after 24 hrs by MTT assay Cytotoxicity against human A549 cells after 24 hrs by MTT assay	[PMID: 24050254]
Bel-7402	IC₅₀	7 nM Compound: 1	Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay	[PMID: 15844967]
BGC-823	IC₅₀	4.5 x 10^-2 μM Compound: 1	Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay	[PMID: 15844967]
BXPC-3	EC₅₀	11 nM Compound: 4	Cytotoxicity against human BxPC3 cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human BxPC3 cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
CCRF S-180	EC₅₀	> 20000 nM Compound: 4	Cytotoxicity against mouse S180 cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against mouse S180 cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
CCRF S-180	IC₅₀	> 50 μM Compound: 1	Cytotoxicity against mouse S180 cells expressing mutated alpha-1 Na+/K+-ATPase assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against mouse S180 cells expressing mutated alpha-1 Na+/K+-ATPase assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 23799775]
CNE	IC₅₀	0.279 μM Compound: 1	Cytotoxicity against human CNE1 cells assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against human CNE1 cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 23799775]
CNE2Z	IC₅₀	0.46 μM Compound: 1	Cytotoxicity against human CNE2Z cells assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against human CNE2Z cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 23799775]
H22	IC₅₀	> 50 μM Compound: 1	Cytotoxicity against mouse H22 cells expressing mutated alpha-1 Na+/K+-ATPase assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against mouse H22 cells expressing mutated alpha-1 Na+/K+-ATPase assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 23799775]
HCT-116	EC₅₀	11 nM Compound: 4	Cytotoxicity against human HCT116 cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human HCT116 cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
HeLa	IC₅₀	2.8 x 10^-2 μM Compound: 1	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	[PMID: 15844967]
HeLa	IC₅₀	279.9 nM Compound: Bufalin	Cytotoxicity activity against human HeLa cells after 48 hrs by MTT assay Cytotoxicity activity against human HeLa cells after 48 hrs by MTT assay	[PMID: 30245398]
HeLa	IC₅₀	594.2 nM Compound: Bufalin	Cytotoxicity activity against human HeLa cells after 24 hrs by MTT assay Cytotoxicity activity against human HeLa cells after 24 hrs by MTT assay	[PMID: 30245398]
HepG2	IC₅₀	0.345 μM Compound: 1	Cytotoxicity against adriamycin-resistant human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against adriamycin-resistant human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 23799775]
HepG2	IC₅₀	0.589 μM Compound: 1	Cytotoxicity against human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 23799775]
HepG2	IC₅₀	0.6 μM Compound: 7	Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay	[PMID: 24050254]
HepG2	EC₅₀	35 nM Compound: 4	Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
HL-60	IC₅₀	< 0.01 μg/mL Compound: 16	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	[PMID: 11575946]
HUVEC	EC₅₀	12 nM Compound: 4	Cytotoxicity against human HUVEC cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human HUVEC cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
KB	IC₅₀	0.67 μg/mL Compound: 16	Cytotoxicity against human KB cells after 72 hrs by MTT assay Cytotoxicity against human KB cells after 72 hrs by MTT assay	[PMID: 11575946]
MCF7	EC₅₀	42 nM Compound: 4	Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
MES-SA	EC₅₀	28 nM Compound: 4	Cytotoxicity against human MESSA cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human MESSA cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
MES-SA/Dx5	EC₅₀	18 nM Compound: 4	Cytotoxicity against human MES-SA/Dx5 cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human MES-SA/Dx5 cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
MH60	IC₅₀	> 25 μg/mL Compound: 16	Cytotoxicity against mouse MH60 cells after 72 hrs by MTT assay Cytotoxicity against mouse MH60 cells after 72 hrs by MTT assay	[PMID: 11575946]
MH60	IC₅₀	> 64.8 μM Compound: 3	Growth inhibition of IL-6-independent mouse MH60 cells after 72 hrs by MTT assay Growth inhibition of IL-6-independent mouse MH60 cells after 72 hrs by MTT assay	[PMID: 15620253]
MH60	IC₅₀	31.9 μM Compound: 3	Growth inhibition of IL6-dependent mouse MH60 cells after 72 hrs by MTT assay in presence of human recombinant IL6 Growth inhibition of IL6-dependent mouse MH60 cells after 72 hrs by MTT assay in presence of human recombinant IL6	[PMID: 15620253]
NCI-H1975	EC₅₀	13 nM Compound: 4	Cytotoxicity against human NCI-H1975 cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human NCI-H1975 cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
SK-OV-3	EC₅₀	10 nM Compound: 4	Cytotoxicity against human SKOV3 cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human SKOV3 cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
U-87MG ATCC	EC₅₀	14 nM Compound: 4	Cytotoxicity against human U87MG cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human U87MG cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]

體外研究
(In Vitro)

Bufalin (0、1、2、4 μM，持續(xù) 48 小時(shí)) 降低 NCI-H460 細(xì)胞的細(xì)胞活力^[2]。
Bufalin (2 μM) 增加 caspae-3、Endo G 和 GADD153 mRNA 表達(dá)，但降低 GRP78 mRNA 表達(dá)^[2]。

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

Cell Viability Assay^[2]

Cell Line:	NCI-H460 cells
Concentration:	0, 1, 2, 4 μM
Incubation Time:	48 hours
Result:	Decreased viability of NCI-H460 cells in a dose-dependent manner.

體內(nèi)研究
(In Vivo)

Bufalin (0.1、0.2 或 0.4 mg/kg，腹腔注射，每天一次，持續(xù) 14 天) 在攜帶 NCI-H460 細(xì)胞的小鼠中顯示出顯著的抗腫瘤活性^[2]。

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

Animal Model:	Forty male athymic BALB/c nu/nu mice (6-8 weeks old)^[2]
Dosage:	0.1, 0.2, or 0.4 mg/kg
Administration:	I.P. every day until 14 days
Result:	Dose-dependently suppressed tumor growth.

分子量

386.52

Formula

C₂₄H₃₄O₄

CAS 號(hào)

465-21-4

性狀

固體

顏色

White to off-white

結(jié)構(gòu)分類

Steroids

初始來源

動(dòng)物

toad

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	6 months
	-20°C	1 month

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : 100 mg/mL (258.72 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	2.5872 mL	12.9359 mL	25.8719 mL
5 mM	0.5174 mL	2.5872 mL	5.1744 mL
10 mM	0.2587 mL	1.2936 mL	2.5872 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, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(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(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.47 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 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(qǐng)依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.47 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。
方案三

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.38 mM); 澄清溶液

此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 20.8 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。

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 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: 99.86%

選擇批次：

Data Sheet (634 KB) SDS (480 KB)

COA (268 KB) HNMR (167 KB) LCMS (112 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[1]. Katz A, et al. Selectivity of digitalis glycosides for isoforms of human Na,K-ATPase. J Biol Chem. 2010 Jun 18;285(25):19582-92. [Content Brief]

[2]. Wu SH, et al. Bufalin induces apoptosis in vitro and has Antitumor activity against human lung cancer xenografts in vivo. Environ Toxicol. 2017 Apr;32(4):1305-1317. [Content Brief]

Bufalin 相關(guān)分類

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	2.5872 mL	12.9359 mL	25.8719 mL	64.6797 mL
	5 mM	0.5174 mL	2.5872 mL	5.1744 mL	12.9359 mL
	10 mM	0.2587 mL	1.2936 mL	2.5872 mL	6.4680 mL
	15 mM	0.1725 mL	0.8624 mL	1.7248 mL	4.3120 mL
	20 mM	0.1294 mL	0.6468 mL	1.2936 mL	3.2340 mL
	25 mM	0.1035 mL	0.5174 mL	1.0349 mL	2.5872 mL
	30 mM	0.0862 mL	0.4312 mL	0.8624 mL	2.1560 mL
	40 mM	0.0647 mL	0.3234 mL	0.6468 mL	1.6170 mL
	50 mM	0.0517 mL	0.2587 mL	0.5174 mL	1.2936 mL
	60 mM	0.0431 mL	0.2156 mL	0.4312 mL	1.0780 mL
	80 mM	0.0323 mL	0.1617 mL	0.3234 mL	0.8085 mL
	100 mM	0.0259 mL	0.1294 mL	0.2587 mL	0.6468 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.

Keywords:

Bufalin465-21-4Na+/K+ ATPaseSodium potassium pumpInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只為有資質(zhì)的科研機(jī)構(gòu)、醫(yī)藥企業(yè)基于科學(xué)研究或藥證申報(bào)的用途提供醫(yī)藥研發(fā)服務(wù)，不為任何個(gè)人或者非科研性質(zhì)的、非用于藥證申報(bào)使用等其他用途提供服務(wù)。

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Bufalin (Synonyms: 蟾毒靈)

Customer Review

Other Forms of Bufalin:

MCE 顧客使用本產(chǎn)品發(fā)表的 6 篇科研文獻(xiàn)