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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RMB 809.97 现货
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RMB 8001.23 现货
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客户使用该产品的2个实验数据:

  • (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 MWDGeY5kfGmxbjDhd5NigQ>? MnHYRYdwdmm|dDDhZ5Rqfmm2eTDheEBHYFJiZYjwdoV{e2WmIHnuJGNQWzFiY3XscJMh[nliY3XscE1j[XOnZDDibY9tfW2rbnXzZ4Vv[2ViYYPzZZktKEWFNUC9PVkhdk1? MoGxNlAxOTR6N{C=
HeLa cells MmixSpVv[3Srb36gZZN{[Xl? MYeyOEBp M4D1VWFod26rc4SgZYN1cX[rdImgZZQhcHWvYX6g[pVtdCCuZX7neIghTliUIHX4dJJme3OnZDDpckBJ\UyjIHPlcIx{KGOxdILhcpNn\WO2ZXSge4l1cCCyU1e1MYh2dWGwIGLYVkBi\nSncjCyOEBpenNiYomgSJVidC2JbH:gcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6NCCHQ{WwQVAvOTZizszN NV\OSIFVOjV7M{SyNlc>
CHO cells MXXGeY5kfGmxbjDhd5NigQ>? NGToVGE2KGh? NWHjXWQ{SWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBVT1J3IHX4dJJme3OnZDDpckBEUE9iY3XscJMh[W[2ZYKgOUBpenNiYomgR3JGNWS{aY\lckBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OC55NUWg{txO MYexO|Y5PTZyMx?=
NCI-H716 cells M3;aNGZ2dmO2aX;uJIF{e2G7 MUPB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIGTHVlUhemWlZYD0c5Ih\XiycnXzd4VlKGmwIF7DTU1JPzF4IHPlcIx{KGG|c3Xzd4VlKGG|IHnueJJi[2WubIXsZZIh[0GPUDDs[ZZmdCCkeTDUVk1HWkWWIHHzd4F6NCCHQ{WwQVIxKM7:TR?= NVnaT5ZkOjF2NUm1PFA>
mouse GLUTag cells NXLrc|RITnWwY4Tpc44h[XO|YYm= NYjBPWI6SWexbnnzeEBi[3Srdnn0fUBifCCJUD3CRXIyKGmwIH3veZNmKEeOVWTh[{Bk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiCrboTyZYNmdGy3bHHyJINCVVBibHX2[Yw> NW\pUmRIOjR|OEezNlU>
human HepG2 cells NEixWI9HfW6ldHnvckBie3OjeR?= NVPjSXRoOTBizszN MVSxPEBp MVzB[49vcXO2IHHjeIl3cXS7IHH0JGZZWiCrbjDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{B2eHKnZ4XsZZRqd25ib3[gV2hRKG2UTlGg[ZhxemW|c3nvckBifCBzMDD1UUBi\nSncjCxPEBpenNiYomgVnQuWEOUIHHuZYx6e2m| NWjiZ3NkOjR|OEezNlU>
mouse primary hepatocytes NVHifGVbTnWwY4Tpc44h[XO|YYm= M2TDSmFod26rc4SgZYN1cX[rdImgZZQhTliUIHnuJI1wfXOnIIDybY1ienliaHXwZZRw[3m2ZYOgZZN{\XO|ZXSgZZMhfXC{ZXf1cIF1cW:wIH;mJGJGW1BibWLORUBmgHC{ZYPzbY9v NIPhUmYzPDN6N{OyOS=>

... 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
NCT02177136 Completed Primary Sclerosing Cholangitis (PSC) Intercept Pharmaceuticals February 9 2015 Phase 2
NCT02633956 Completed Nonalcoholic Steatohepatitis Intercept Pharmaceuticals December 4 2015 Phase 2
NCT03439254 Recruiting Compensated Cirrhosis|Nonalcoholic Steatohepatitis Intercept Pharmaceuticals August 30 2017 Phase 3
NCT02430077 Recruiting Familial Partial Lipodystrophy University of Texas Southwestern Medical Center June 2016 Phase 2
NCT02548351 Recruiting Non Alcoholic Steatohepatitis (NASH) Intercept Pharmaceuticals September 2015 Phase 3
NCT02532335 Recruiting Obesity Sahlgrenska University Hospital Sweden August 2015 Phase 1

技术支持

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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