Lithocholic acid (Synonyms: 石胆酸)

目录号: HY-B0172 纯度: 99.99%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Lithocholic acid 是有毒的次级胆汁酸，能促使肝内胆汁淤积，能促进肿瘤发生。Lithocholic acid 也是一种 FXR 拮抗剂和 PXR/SXR 激动剂。

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Lithocholic acid Chemical Structure

CAS No. : 434-13-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥500	In-stock
50 mg	￥106	In-stock
500 mg	￥400	In-stock
1 g	￥600	In-stock
5 g	￥960	In-stock
10 g		询价
50 g		询价

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Customer Review

Other Forms of Lithocholic acid:

MCE 顾客使用本产品发表的 12 篇科研文献

Lithocholic acid 相关产品

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生物活性
纯度 & 产品资料
参考文献

生物活性

Lithocholic acid is a toxic secondary bile acid that can promote intrahepatic cholestasis and promote tumorigenesis. Lithocholic acid is also a FXR antagonist and a PXR/SXR agonist^[1]^[2]^[3]^[4]^[5].

IC₅₀ & Target

Microbial Metabolite

Human Endogenous Metabolite

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	> 200 μM Compound: LCA	Anticancer activity against human A549 cells assessed as inhibition of cell proliferation by MTT assay Anticancer activity against human A549 cells assessed as inhibition of cell proliferation by MTT assay	[PMID: 36439975]
Caco-2	IC₅₀	56 μM Compound: LCA	Cytotoxicity against human Caco2 cells assessed as cell viability after 24 hrs by MTT assay Cytotoxicity against human Caco2 cells assessed as cell viability after 24 hrs by MTT assay	[PMID: 24332653]
CHO	EC₅₀	0.58 μM Compound: 6, LCA	Agonist activity at human TGR5 expressed in CHO cells by luciferase assay Agonist activity at human TGR5 expressed in CHO cells by luciferase assay	[PMID: 18307294]
CHO	EC₅₀	5.6 μM Compound: LCA	Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay	[PMID: 19911773]
COS-1	EC₅₀	20 μM Compound: 6, LCA	Agonist activity at human FXR expressed in COS1 cells by luciferase assay Agonist activity at human FXR expressed in COS1 cells by luciferase assay	[PMID: 18307294]
COS-1	EC₅₀	6.7 μM Compound: LCA	Agonist activity at human FXR expressed in COS1 cells by luciferase reporter gene assay Agonist activity at human FXR expressed in COS1 cells by luciferase reporter gene assay	[PMID: 19911773]
DLD-1	IC₅₀	173.1 μM Compound: LCA	Cytotoxicity against human DLD1 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human DLD1 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 25685308]
Erythrocyte	IC₅₀	0.009 mg/mL Compound: L	Hemolytic activity in human erythrocytes assessed as release of hemoglobin after 60 mins Hemolytic activity in human erythrocytes assessed as release of hemoglobin after 60 mins	[PMID: 24461290]
HCT-116	IC₅₀	> 200 μM Compound: LCA	Anticancer activity against human HCT-116 cells assessed as inhibition of cell proliferation by MTT assay Anticancer activity against human HCT-116 cells assessed as inhibition of cell proliferation by MTT assay	[PMID: 36439975]
HCT-116	IC₅₀	81.1 μM Compound: LCA	Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 25685308]
HCT-8	IC₅₀	97.4 μM Compound: LCA	Cytotoxicity against human HCT8 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human HCT8 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 25685308]
HEK293	EC₅₀	0.68 μM Compound: 1, LCA	Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay Agonist activity at human GPBAR1 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 30 mins by cAMP-Glo assay	[PMID: 25735208]
HEK-293T	EC₅₀	2.14 μM Compound: LCA	Agonist activity at VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay Agonist activity at VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay	[PMID: 26774929]
HEK-293T	IC₅₀	46.7 μM Compound: LCA	Antagonist activity against VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as inhibition of 1,25-dihydroxyvitamin D3-induced SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay Antagonist activity against VP16 tagged-VDR-LBD (unknown origin) expressed in HEK293T cells assessed as inhibition of 1,25-dihydroxyvitamin D3-induced SRC1 coactivator peptide recruitment after 16 hrs by luciferase reporter gene based two hybrid assay	[PMID: 26774929]
HepG2	EC₅₀	50 μM Compound: LCA	Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 4 hrs by CellTiter-Glo assay Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 4 hrs by CellTiter-Glo assay	[PMID: 27652492]
HepG2	EC₅₀	50 μM Compound: LCA	Cytotoxicity in human HepG2 cells assessed as induction of cell necrosis incubated for 4 hrs by LDH release assay Cytotoxicity in human HepG2 cells assessed as induction of cell necrosis incubated for 4 hrs by LDH release assay	[PMID: 27652492]
HET-1A	CC₅₀	25 μM Compound: 35, LCA	Cytotoxicity against human HET-1A cells assessed as cell viability after 24 hrs by MTT assay Cytotoxicity against human HET-1A cells assessed as cell viability after 24 hrs by MTT assay	[PMID: 20713311]
HT-1080	IC₅₀	23 μM Compound: LCA	Cytotoxicity against human HT1080 cells assessed as cell viability after 24 hrs by MTT assay Cytotoxicity against human HT1080 cells assessed as cell viability after 24 hrs by MTT assay	[PMID: 24332653]
HT-29	IC₅₀	> 200 μM Compound: LCA	Anticancer activity against human HT-29 cells assessed as inhibition of cell proliferation by MTT assay Anticancer activity against human HT-29 cells assessed as inhibition of cell proliferation by MTT assay	[PMID: 36439975]
Huh-7	IC₅₀	> 200 μM Compound: LCA	Anticancer activity against human Huh-7 cells assessed as inhibition of cell proliferation by MTT assay Anticancer activity against human Huh-7 cells assessed as inhibition of cell proliferation by MTT assay	[PMID: 36439975]
LoVo	IC₅₀	> 200 μM Compound: LCA	Anticancer activity against human LoVo cells assessed as inhibition of cell proliferation by MTT assay Anticancer activity against human LoVo cells assessed as inhibition of cell proliferation by MTT assay	[PMID: 36439975]
MGC-803	IC₅₀	> 200 μM Compound: LCA	Anticancer activity against human MGC-803 cells assessed as inhibition of cell proliferation by MTT assay Anticancer activity against human MGC-803 cells assessed as inhibition of cell proliferation by MTT assay	[PMID: 36439975]
NCI-H716	EC₅₀	5 μM Compound: LCA	Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis Agonist activity at TGR5 expressed in NCI-H716 cells assessed as cAMP level after 60 mins by FRET analysis	[PMID: 24900463]
PC-3	IC₅₀	50 μM Compound: 1, LCA	Antagonist activity at EphA2 in human PC3 cells assessed as inhibition of ephrin-A1-Fc-stimulated EphA2 phosphorylation pretreated for 20 mins by sandwich ELISA Antagonist activity at EphA2 in human PC3 cells assessed as inhibition of ephrin-A1-Fc-stimulated EphA2 phosphorylation pretreated for 20 mins by sandwich ELISA	[PMID: 23489211]
RKO	IC₅₀	> 200 μM Compound: LCA	Anticancer activity against human RKO cells assessed as inhibition of cell proliferation by MTT assay Anticancer activity against human RKO cells assessed as inhibition of cell proliferation by MTT assay	[PMID: 36439975]
SK-HEP1	IC₅₀	> 200 μM Compound: LCA	Anticancer activity against human SK-HEP1 cells assessed as inhibition of cell proliferation by MTT assay Anticancer activity against human SK-HEP1 cells assessed as inhibition of cell proliferation by MTT assay	[PMID: 36439975]
SW480	IC₅₀	> 200 μM Compound: LCA	Anticancer activity against human SW480 cells assessed as inhibition of cell proliferation by MTT assay Anticancer activity against human SW480 cells assessed as inhibition of cell proliferation by MTT assay	[PMID: 36439975]

体外研究
(In Vitro)

Lithocholic Acid 可抑制 CDCA 和 GW4064 诱导的 FXR 激活，IC₅₀分别为 0.7 和 1.4 μM^[5]。
Lithocholic Acid (10-30 μM，24 小时) 抑制 HepG2 细胞中 100 nM GW4064 诱导的 BSEP 表达^[5]。
Lithocholic Acid (0-500 μM) 剂量依赖性地抑制神经母细胞瘤细胞 (BE(2)-m17、SK-n-SH、SK-n-MCIXC 和 Lan-1) 的增殖^[3] .

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

体内研究
(In Vivo)

Lithocholic acid (LCA) 可用于诱导胆汁淤积模型_[6]_[7]。

诱导胆汁淤积_[6]_[7]

致病原理

LCA 对肝细胞有一定毒性，可通过其渗透作用改变胆汁分泌，并通过改变富含胆管膜的肝细胞细胞膜组分，引起胆汁淤积。

具体造模方法：

大鼠：Wistar • 雄性 • 250-300 g (处理：1 h)
给药方式：0.2 μmol/100 g • iv • 处理 1 h 后处死大鼠
小鼠：ICR • 雄性 • 5-7 周龄 (处理：3 天)
给药方式：150 mg/kg • 口服 • 每日 2 次，共 5 次

Note

(1) LCA (静脉注射) 溶于 7.5% 牛血清白蛋白和 0.45% 生理盐水中。
(2) LCA (灌胃) 在玉米油中溶解。第 5 次处理后 12 h 处死动物。可于第 1 剂给药后 0、12、24 和 36 h 时，采用尾部放血法采集 50μL 血样。

造模成功指标

组织学改变：LCA 注射后短时间内显著增加胆汁流量，之后胆汁流量显著减少。可观察到肝组织病理改变，包括肝坏死和弥漫性空泡。

相关产品： /

拮抗产品： /

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

Animal Model:	Male mice (C57BL/6)^[4].
Dosage:	0.6% LCA-supplement diet, with the AIN93G diet as a control
Administration:	in diet, for 6 days
Result:	Induced liver injury. Activated TGFβ-SMAD3 signaling. Increased serum ALP activities.

Animal Model:	Male mice (C57BL/6)^[2].
Dosage:	125 mg/kg, dissolved in corn oil
Administration:	i.p., twice a day for four days
Result:	Induced liver injury, generated necrosis and neutrophilic-granulocytic infiltrate (H&E staining). Increased AST, ALT and ALP level.

分子量

376.57

Formula

C₂₄H₄₀O₃

CAS 号

434-13-9

性状

固体

颜色

White to off-white

中文名称

石胆酸；3-羟基胆基酸；石胆甾酸；胆石酸

结构分类

Steroids

初始来源

微生物

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	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 250 mg/mL (663.89 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

Ethanol 中的溶解度 : 10 mg/mL (26.56 mM; 超声助溶 (<60°C))

H₂O 中的溶解度 : 0.99 mg/mL (2.63 mM; ultrasonic and warming and adjust pH to 11 with NaOH and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6555 mL	13.2777 mL	26.5555 mL
5 mM	0.5311 mL	2.6555 mL	5.3111 mL
10 mM	0.2656 mL	1.3278 mL	2.6555 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, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

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

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.52 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.52 mM); 澄清溶液

此方案可获得 ≥ 2.08 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。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
方案三

请依序添加每种溶剂： 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (2.66 mM); 澄清溶液

此方案可获得 ≥ 1 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 EtOH 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。
方案四

请依序添加每种溶剂： 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (2.66 mM); 澄清溶液

此方案可获得 ≥ 1 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 EtOH 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案五

请依序添加每种溶剂： 10% EtOH 90% Corn Oil
Solubility: ≥ 1 mg/mL (2.66 mM); 澄清溶液

此方案可获得 ≥ 1 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。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 EtOH 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

每只动物的给药体积

μL

动物数量

只

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: 99.99%

选择批次：

Data Sheet (655 KB) SDS (393 KB)

COA (285 KB) HNMR (260 KB) RP-HPLC (183 KB) MS (80 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Jenkins, D.J., et al., Effect on blood lipids of very high intakes of fiber in diets low in saturated fat and cholesterol. N Engl J Med, 1993. 329(1): p. 21-6. [Content Brief]

[2]. Yang R, et al. Metabolomic analysis of cholestatic liver damage in mice. Food Chem Toxicol. 2018 Jul 14;120:253-260. [Content Brief]

[3]. Goldberg, A.A., et al., Lithocholic bile acid selectively kills neuroblastoma cells, while sparing normal neuronal cells. Oncotarget, 2011. 2(10): p. 761-82. [Content Brief]

[4]. Matsubara, T., et al., TGF-beta-SMAD3 signaling mediates hepatic bile acid and phospholipid metabolism following lithocholic acid-induced liver injury. J Lipid Res, 2012. 53(12): p. 2698-707. [Content Brief]

[5]. Yu J, et al. Lithocholic acid decreases expression of bile salt export pump through farnesoid X receptor antagonist activity. J Biol Chem. 2002 Aug 30;277(35):31441-7. [Content Brief]

Lithocholic acid 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

H₂O / Ethanol / DMSO	1 mM	2.6555 mL	13.2777 mL	26.5555 mL	66.3887 mL
Ethanol / DMSO	5 mM	0.5311 mL	2.6555 mL	5.3111 mL	13.2777 mL
	10 mM	0.2656 mL	1.3278 mL	2.6555 mL	6.6389 mL
	15 mM	0.1770 mL	0.8852 mL	1.7704 mL	4.4259 mL
	20 mM	0.1328 mL	0.6639 mL	1.3278 mL	3.3194 mL
	25 mM	0.1062 mL	0.5311 mL	1.0622 mL	2.6555 mL
DMSO	30 mM	0.0885 mL	0.4426 mL	0.8852 mL	2.2130 mL
	40 mM	0.0664 mL	0.3319 mL	0.6639 mL	1.6597 mL
	50 mM	0.0531 mL	0.2656 mL	0.5311 mL	1.3278 mL
	60 mM	0.0443 mL	0.2213 mL	0.4426 mL	1.1065 mL
	80 mM	0.0332 mL	0.1660 mL	0.3319 mL	0.8299 mL
	100 mM	0.0266 mL	0.1328 mL	0.2656 mL	0.6639 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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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:

Lithocholic acid434-13-9石胆酸3-羟基胆基酸石胆甾酸胆石酸AutophagyEndogenous MetaboliteApoptosisFXRNR1H4bile acidneuroblastomaHepG2liverInhibitorinhibitorinhibit

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Lithocholic acid (Synonyms: 石胆酸)

Customer Review

Other Forms of Lithocholic acid:

MCE 顾客使用本产品发表的 12 篇科研文献

Lithocholic acid 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

生物活性

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

Lithocholic acid 相关分类

完整储备液配制表

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Lithocholic acid (Synonyms: 石胆酸)

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Other Forms of Lithocholic acid:

Lithocholic acid 相关抗体

MCE 顾客使用本产品发表的 12 篇科研文献

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Lithocholic acid 相关抗体:

摩尔计算器

稀释计算器

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