1. Metabolic Enzyme/Protease Autophagy
  2. FXR Endogenous Metabolite Autophagy
  3. Chenodeoxycholic Acid

Chenodeoxycholic Acid  (Synonyms: 鹅去氧胆酸; CDCA)

目录号: HY-76847 纯度: 99.90%
COA 产品使用指南

Chenodeoxycholic Acid 是一种疏水初级胆汁酸,能够活化核受体 FXR,该受体与胆固醇代谢有关。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Chenodeoxycholic Acid Chemical Structure

Chenodeoxycholic Acid Chemical Structure

CAS No. : 474-25-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550
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100 mg ¥500
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500 mg ¥700
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1 g ¥900
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5 g ¥1300
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Customer Review

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.

IC50 & Target

Human Endogenous Metabolite

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 200 μM
Compound: CDCA
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
106 μM
Compound: CDCA
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
15.6 μM
Compound: CDCA
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
Agonist activity at recombinant human TGR5 expressed in CHO cells assessed as increase in cAMP accumulation after 30 mins by TR-FRET assay
[PMID: 31268316]
CHO EC50
6.71 μM
Compound: 4, CDCA
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
6.71 μM
Compound: 2, CDCA
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
Agonist activity at human TGR5 expressed in CHO cells after 5 hrs by CRE-driven luciferase reporter gene assay
[PMID: 17685603]
COS-1 EC50
13 μM
Compound: 4, CDCA
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
13 μM
Compound: 2, CDCA
Agonist activity at human FXR expressed in COS1 cells after 5 hrs by CRE-driven luciferase reporter gene assay
Agonist activity at human FXR expressed in COS1 cells after 5 hrs by CRE-driven luciferase reporter gene assay
[PMID: 17685603]
COS-1 EC50
13 μM
Compound: 3, CDCA
Agonist activity at FXR expressed in COS1 cells by cell-based bioluminescence assay
Agonist activity at FXR expressed in COS1 cells by cell-based bioluminescence assay
[PMID: 20014870]
GBM IC50
> 50 μM
Compound: 1c, CDCA, chenodeoxycholic acid
Cytotoxicity against human GBM cells after 24 hrs by neutral red uptake assay
Cytotoxicity against human GBM cells after 24 hrs by neutral red uptake assay
[PMID: 20381215]
HCT-116 IC50
> 200 μM
Compound: CDCA
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
> 50 μM
Compound: 1c, CDCA, chenodeoxycholic acid
Cytotoxicity against human HCT116 cells after 24 hrs by neutral red uptake assay
Cytotoxicity against human HCT116 cells after 24 hrs by neutral red uptake assay
[PMID: 20381215]
HEK293 EC50
11.7 μM
Compound: 3, CDCA
Agonist activity at human recombinant FXR by transactivation of TK-MH100x4-LUC reporter gene in HEK293 cells
Agonist activity at human recombinant FXR by transactivation of TK-MH100x4-LUC reporter gene in HEK293 cells
[PMID: 16617018]
HEK293 EC50
16.8 μM
Compound: CDCA
Agonist activity at full length mouse FXR/RXRalpha expressed in human HEK293 cells assessed as induction of transcriptional activity after 18 hrs by dual luciferase reporter gene assay
Agonist activity at full length mouse FXR/RXRalpha expressed in human HEK293 cells assessed as induction of transcriptional activity after 18 hrs by dual luciferase reporter gene assay
[PMID: 22014750]
HEK293 EC50
16.8 μM
Compound: 2, CDCA
Agonist activity at mouse FXR expressed in HEK293 cells co-expressing mouse RXRalpha and ECRE-luc by luciferase reporter gene assay
Agonist activity at mouse FXR expressed in HEK293 cells co-expressing mouse RXRalpha and ECRE-luc by luciferase reporter gene assay
[PMID: 22018919]
HEK293 EC50
27 μM
Compound: 5, CDCA
Agonist activity at human recombinant FXR expressed in HEK293 cells coexpressing CMX-GAL4N by luciferase reporter gene assay
Agonist activity at human recombinant FXR expressed in HEK293 cells coexpressing CMX-GAL4N by luciferase reporter gene assay
[PMID: 22583617]
HEK293 EC50
27 μM
Compound: CDCA
Agonistic activity at FXR in HEK293 cells by GAL4 transactivation activity
Agonistic activity at FXR in HEK293 cells by GAL4 transactivation activity
[PMID: 17292610]
HEK293 EC50
6.1 μM
Compound: 2, CDCA
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
> 150 μM
Compound: CDCA
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
> 50 μM
Compound: CDCA
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]
HeLa EC50
18 μM
Compound: 1, CDCA
Agonist activity at human full length FXR expressed in HeLa cells cotransfected with pSG5-human RXR after 24 hrs by Dual-Glo luciferase reporter gene assay
Agonist activity at human full length FXR expressed in HeLa cells cotransfected with pSG5-human RXR after 24 hrs by Dual-Glo luciferase reporter gene assay
[PMID: 25934227]
HeLa EC50
18 μM
Compound: 1, CDCA
Agonist activity at human FXR expressed in human HeLa cells assessed as receptor activation by BSEP promoter-driven firefly luciferase reporter gene assay
Agonist activity at human FXR expressed in human HeLa cells assessed as receptor activation by BSEP promoter-driven firefly luciferase reporter gene assay
[PMID: 25255039]
HepG2 EC50
20 μM
Compound: 1; CDCA
Transactivation of human FXR (unknown origin) expressed in HepG2 cells co-expressing pSG5RXR/pGL4.70 after 24 hrs post transfection by luciferase reporter gene assay
Transactivation of human FXR (unknown origin) expressed in HepG2 cells co-expressing pSG5RXR/pGL4.70 after 24 hrs post transfection by luciferase reporter gene assay
[PMID: 30996771]
HET-1A CC50
216 μM
Compound: 1, CDCA
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
130.1 μM
Compound: CDCA
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: CDCA
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]
HT-29 IC50
> 80 μM
Compound: CDCA
Antiproliferative activity against human HT-29 cells after 48 hrs by SRB assay
Antiproliferative activity against human HT-29 cells after 48 hrs by SRB assay
[PMID: 27448915]
Huh-7 IC50
> 200 μM
Compound: CDCA
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]
KMS-11 IC50
> 50 μM
Compound: 1c, CDCA, chenodeoxycholic acid
Cytotoxicity against human KMS11 cells after 24 hrs by neutral red uptake assay
Cytotoxicity against human KMS11 cells after 24 hrs by neutral red uptake assay
[PMID: 20381215]
LoVo IC50
> 200 μM
Compound: CDCA
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: CDCA
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
30 μM
Compound: 1, CDCA
Agonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assay
Agonist activity at human TGR5 receptor expressed in NCI-H716 cells assessed as intracellular cAMP level by TR-FRET assay
[PMID: 21459580]
NCI-H716 EC50
33 μM
Compound: CDCA
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 60 mins by HTR-FRET assay
Agonist activity at TGR5 in human NCI-H716 cells assessed as increase in cAMP accumulation after 60 mins by HTR-FRET assay
[PMID: 31268316]
NCI-H716 EC50
6.7 μM
Compound: 2, CDCA
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-3M IC50
> 80 μM
Compound: CDCA
Antiproliferative activity against human PC3M cells after 48 hrs by SRB assay
Antiproliferative activity against human PC3M cells after 48 hrs by SRB assay
[PMID: 27448915]
RKO IC50
> 200 μM
Compound: CDCA
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: CDCA
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: CDCA
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)

Cheonodeoxycholic acid (CDCA) 和 Deoxycholic acid (DCA) 均抑制 11 beta HSD2,IC50 值分别为 22 mM 和 38 mM,并引起皮质醇依赖性核转位并增加盐皮质激素受体 (MR) 的转录活性)[1]。Cheonodeoxycholic acid 能够通过激活膜 G 蛋白偶联受体 (TGR5) 依赖性通路诱导细胞周期蛋白 D1 蛋白和 mRNA 表达显著增加,从而刺激 Ishikawa 细胞生长[2]。在培养的人肝母细胞瘤细胞系 Hep G2[3]中,Chenodeoxycholic Acid (CDCA) 可将 LDL 受体 mRNA 水平提高约 4 倍,将 HMG-CoA 还原酶和 HMG-CoA 合酶的 mRNA 水平提高两倍。布美他尼、BaCl2 和囊性纤维化跨膜电导调节剂 (CFTR) 抑制剂 CFTRinh-172 可抑制鹅脱氧胆酸诱导的 Isc (≥67%)。Chenodeoxycholic Acid 刺激的 Isc 被腺苷酸环化酶抑制剂 MDL12330A 降低了 43%,而 Chenodeoxycholic Acid 增加了细胞内 cAMP 浓度[4]。Chenodeoxycholic Acid 处理可激活 C/EBPβ,如其在 HepG2 细胞中的磷酸化、核积累和表达增加所示。Cheonodeoxycholic acid 增强荧光素酶基因从含有-1.65-kb GSTA2 启动子的构建体转录,该启动子含有 C/EBP 反应元件 (pGL-1651)。Chenodeoxycholic Acid 处理可激活 AMP 活化蛋白激酶 (AMPK),从而导致细胞外信号调节激酶 1/2 (ERK1/2) 激活,使用 AMPKα 显性失活突变体和化学抑制剂的实验结果证明了这一点[5]

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

Clinical Trial
分子量

392.57

Formula

C24H40O4

CAS 号
性状

固体

颜色

White to off-white

中文名称

鹅去氧胆酸

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

RT, protect from light

In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : ≥ 50 mg/mL (127.37 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

0.1 M NaOH 中的溶解度 : 50 mg/mL (127.37 mM; ultrasonic and adjust pH to 8 with NaOH)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5473 mL 12.7366 mL 25.4732 mL
5 mM 0.5095 mL 2.5473 mL 5.0946 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用,-20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (6.37 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 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 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.37 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 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。

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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: 20% HP-β-CD in Saline

    Solubility: ≥ 20 mg/mL (50.95 mM); 澄清溶液

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

g

每只动物的给药体积

μL

动物数量

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: 99.90%

参考文献
Kinase Assay
[1]

Briefly, transfected HEK-293 cells, incubated in charcoal-treated Dulbecco's modified Eagle's medium for 24 h, are washed once with Hanks' solution and resuspended in a buffer containing 100 mM NaCl, 1 mM MgCl2, 1 mM EDTA, 1 mM EGTA, 250 mMsucrose, 20 mM Tris-HCl, pH 7.4. Cells are lysed by freezing in liquid nitrogen. Dehydrogenase activity is measured in a final volume of 20 μL containing the appropriate concentration of bile acid, 30 nCi of [3H]cortisol, and unlabeled cortisol to a final concentrations of 50 nM. The reaction is started by mixing cell lysate with the reaction mixture. Alternatively, endoplasmic reticulum microsomes are prepared from transfected HEK-293 cells and incubated with reaction mixture containing various concentrations of cortisol and CDCA. Incubation proceeded for 20 min, and the conversion of cortisol to cortisone is determined by thin layer chromatography (TLC). Because of the inaccuracy of the TLC method at low conversion rates and the end-product inhibition of 11βHSD2 at conversion rates higher than 60-70%, only conversion rates between 10 and 60% are considered for calculation. The inhibitory constant IC50 is evaluated using the curve-fitting program. Results are expressed as means±S.E. and consist of at least four independent measurements.

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

Cell Assay
[1]

The cell viability is analyzed by incubating transfected HEK-293 cells and CHO cells for 1 h with the corresponding concentration of bile acid and staining with trypan blue. The toxicity of bile acids is analyzed using the tetrazolium salt MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) according to the cell proliferation kit I. No significant differences between control and bile acid-treated cells are obtained in both tests.

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

参考文献

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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用,-20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / 0.1 M NaOH 1 mM 2.5473 mL 12.7366 mL 25.4732 mL 63.6829 mL
5 mM 0.5095 mL 2.5473 mL 5.0946 mL 12.7366 mL
10 mM 0.2547 mL 1.2737 mL 2.5473 mL 6.3683 mL
15 mM 0.1698 mL 0.8491 mL 1.6982 mL 4.2455 mL
20 mM 0.1274 mL 0.6368 mL 1.2737 mL 3.1841 mL
25 mM 0.1019 mL 0.5095 mL 1.0189 mL 2.5473 mL
30 mM 0.0849 mL 0.4246 mL 0.8491 mL 2.1228 mL
40 mM 0.0637 mL 0.3184 mL 0.6368 mL 1.5921 mL
50 mM 0.0509 mL 0.2547 mL 0.5095 mL 1.2737 mL
60 mM 0.0425 mL 0.2123 mL 0.4246 mL 1.0614 mL
80 mM 0.0318 mL 0.1592 mL 0.3184 mL 0.7960 mL
100 mM 0.0255 mL 0.1274 mL 0.2547 mL 0.6368 mL
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  • 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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产品名称:
Chenodeoxycholic Acid
目录号:
HY-76847
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