Obeticholic Acid
目录号：S7660 别名： INT-747, 6-ECDCA
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。
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 |
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 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 |
|
||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| 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
|
|---|
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
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
*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
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 )
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。.
分子量计算器
通过输入化合物的化学式来计算其分子量：
注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2
摩尔浓度计算器
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 |
技术支持
在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。
如果有其他问题，请给我们留言。
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"
