Obeticholic Acid

目录号:S7660 别名: INT-747, 6-ECDCA

Obeticholic Acid Chemical Structure

Molecular Weight(MW): 420.63

Obeticholic Acid是一种有效的选择性farnesoid X receptor (FXR)兴奋剂,EC50为99 nM。Phase 3。

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客户使用Selleck该产品发表文献4篇:

客户使用该产品的3个实验数据:

  • HuCCT1 cells were treated with OCA (1 μM) and control solvent in the presence and absence of IL-6 (20 ng/mL). EMT-related proteins were examined by western blotting. β-actin was used as a control.

    Cell Physiol Biochem, 2018, 48(1):158-172. Obeticholic Acid purchased from Selleck.

    (D) Expression of hepatic FXR target genes, n = 3. Data are expressed as mean ± SD, ###P < 0.001 versus group 1, *P < 0.05, **P < 0.01, and ***P b 0.001 versus group 2, sP < 0.05, ssP < 0.01, and sssP < 0.001 versus group 3

    Toxicol Appl Pharmacol, 2017, 315:23-34. Obeticholic Acid purchased from Selleck.

  • (c) Functional bile canaliculi or lack thereof in PHHs within MPTCs (12 d of drug treatment) as visualized by transport of fluorescent (green) dye into the canaliculi between PHHs. DMSO-treated MPCC control image is shown to the far right. (d) Neutral lipid (Nile red, green) staining of PHHs within MPTCs (12 d of drug treatment). DMSO-treated MPCC control image is shown to the far right. (e) NR1I2 (PXR) gene expression in drug-treated MPTCs relative to DMSOtreated MPTC controls (12 d of treatment). (f) ABCC2 (MRP2) gene expression in drug-treated MPTCs relative to DMSO-treated MPTC controls (12 d of treatment). (g) IL-6 levels in drug-treated MPTC supernatants (6 d of treatment). In all panels, statistical significance is displayed relative to DMSO-treated MPTCs. *p r 0.05, **p r 0.01, ***p r 0.001, and ****p r 0.0001. Scale bars on images represent 80 mm.

    Integr Biol (Camb), 2017, 9(8):662-677. Obeticholic Acid purchased from Selleck.

质量管理及产品安全说明书

FXR抑制剂选择性比较

生物活性

产品描述 Obeticholic Acid是一种有效的选择性farnesoid X receptor (FXR)兴奋剂,EC50为99 nM。Phase 3。
靶点
FXR [1]
99 nM(EC50)
体外研究

在HuH7细胞中,Obeticholic Acid是一种有效的FXR激动剂,EC50 为85 nM。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
COS1 cells NUXkNXU{TnWwY4Tpc44h[XO|YYm= NH6wTXdC\2:waYP0JIFkfGm4aYT5JIF1KE[[UjDlfJBz\XO|ZXSgbY4hS0:VMTDj[YxteyCkeTDj[YxtNWKjc3XkJIJqd2y3bXnu[ZNk\W6lZTDhd5NigSxiRVO1NF06QSCwTR?= NFLRXYkzODBzNEi3NC=>
HeLa cells MV\GeY5kfGmxbjDhd5NigQ>? M4fJfFI1KGh? NGm2ZVVC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJIZ2dGxibHXu[5RpKE[[UjDlfJBz\XO|ZXSgbY4hUGWOYTDj[YxteyClb4TyZY5{\mWldHXkJJdqfGhicGPHOU1pfW2jbjDSXHIh[W[2ZYKgNlQhcHK|IHL5JGR2[WxvR3zvJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVO1NF0xNjF4IN88US=> NXy2fndkOjV7M{SyNlc>
CHO cells NGDhWZZHfW6ldHnvckBie3OjeR?= M1PwSFUhcA>? NIewNplC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJHRIWjViZYjwdoV{e2WmIHnuJGNJVyClZXzsd{Bi\nSncjC1JIhzeyCkeTDDVmUu\HKrdnXuJIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVO1NF0xNjd3NTFOwG0> MYexO|Y5PTZyMx?=
NCI-H716 cells M3L3dWZ2dmO2aX;uJIF{e2G7 M3T0dWFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6gWGdTPSC{ZXPldJRweiCneIDy[ZN{\WRiaX6gUmNKNUh5MU[gZ4VtdHNiYYPz[ZN{\WRiYYOgbY51emGlZXzseYxieiClQV3QJIxmfmWuIHL5JHRTNU[URWSgZZN{[XluIFXDOVA:OjBizszN M1LmcFIyPDV7NUiw
mouse GLUTag cells MYjGeY5kfGmxbjDhd5NigQ>? Ml[wRYdwdmm|dDDhZ5Rqfmm2eTDheEBIWC2EQWKxJIlvKG2xdYPlJGdNXVSjZzDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBqdnS{YXPlcIx2dGG{IHPBUXAhdGW4ZXy= M{jaO|I1Ozh5M{K1
human HepG2 cells NVe5R|JMTnWwY4Tpc44h[XO|YYm= NUL0XYFmOTBizszN M1PJclE5KGh? M1:wXmFod26rc4SgZYN1cX[rdImgZZQhTliUIHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KHWycnXneYxifGmxbjDv[kBUUFBibWLORUBmgHC{ZYPzbY9vKGG2IEGwJJVOKGGodHXyJFE5KGi{czDifUBTXC2SQ2KgZY5idHm|aYO= MkL4NlQ{QDd|MkW=
mouse primary hepatocytes MULGeY5kfGmxbjDhd5NigQ>? NEjoUYpC\2:waYP0JIFkfGm4aYT5JIF1KE[[UjDpckBud3W|ZTDwdolu[XK7IHjldIF1d2O7dHXzJIF{e2W|c3XkJIF{KHWycnXneYxifGmxbjDv[kBDTVOSIH3SUmEh\XiycnXzd4lwdg>? MUiyOFM5PzN{NR?=

... Click to View More Cell Line Experimental Data

体内研究 在大鼠胆汁郁积模型中,Obeticholic Acid促进胆汁流动,并保护肝细胞免受LCA引起的急性坏死。[1] 在WD喂养的DBA 小鼠体内,Obeticholic Acid (p.o.)改善蛋白尿和肾脏结构的改变,并调节肾脏炎症和氧化应激。[2]在硫代乙酰胺(TAA)中毒的和胆小管结扎的(BDL)大鼠体内,Obeticholic Acid (30 mg/kg p.o.) 通过降低总IHVR,恢复FXR下游信号通路,并降低门静脉压力,而不产生有害的全身性低血压。[3]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

动物实验:[1]
+ 展开
  • Animal Models: 大鼠胆汁郁积模型
  • Formulation: 7 μmol/kg/min
  • Dosages: 生理盐水
  • Administration: 使用 PE-50 聚乙烯管在右颈动脉进行注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 84 mg/mL (199.7 mM)
Ethanol 84 mg/mL warmed (199.7 mM)
Water Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 420.63
化学式

C26H44O4

CAS号 459789-99-2
稳定性 powder
in solvent
别名 INT-747, 6-ECDCA

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03836937 Recruiting Non-Alcoholic Fatty Liver Disease Sir Salimullah Medical College Mitford Hospital March 2019 Not Applicable
NCT03836937 Recruiting Non-Alcoholic Fatty Liver Disease Sir Salimullah Medical College Mitford Hospital March 2019 Not Applicable
NCT03633227 Recruiting Liver Cirrhosis Biliary Intercept Pharmaceuticals June 22 2018 Phase 4
NCT03633227 Recruiting Liver Cirrhosis Biliary Intercept Pharmaceuticals June 22 2018 Phase 4
NCT03439254 Recruiting Compensated Cirrhosis|Nonalcoholic Steatohepatitis Intercept Pharmaceuticals August 30 2017 Phase 3
NCT03439254 Recruiting Compensated Cirrhosis|Nonalcoholic Steatohepatitis Intercept Pharmaceuticals August 30 2017 Phase 3

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    What formulation can we use to dissolve Obeticholic Acid (Catalog No.S7660) for mice in vivo study?

  • 回答:

    You can use the vehicle of: 1% wt/vol methyl-cellulose as indicated in this paper, http://www.sciencedirect.com/science/article/pii/S0925443911000883 "daily oral gavage with 5 mg/kg/day INT-747 (6-ethyl-chenodeoxycholic acid, Obeticholic acid, Intercept Pharmaceuticals Inc, New York, NY) or vehicle (1% wt/vol methyl-cellulose) from 3 days prior to induction of colitis"

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID