Obeticholic Acid
製品コードS7660 別名：INT-747, 6-ECDCA
分子量(MW)：420.63
Obeticholic Acid is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Phase 3.
カスタマーフィードバック(3)
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(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.
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.
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(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.
質量管理及び製品安全説明書
FXR阻害剤の選択性比較
生物活性
| 製品説明 | Obeticholic Acid is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. Phase 3. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 体外試験 |
In HuH7 cells, Obeticholic Acid acts as a potent FXR agonist with EC50 of 85 nM. [1] |
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| 細胞データ |
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| 体内試験 | In rat cholestasis model, Obeticholic Acid promotes bile flow, and protects hepatocytes against acute necrosis caused by LCA. [1] Obeticholic Acid (p.o.) improves proteinuria, ameliorates renal structural changes, and modulates renal inflammation and oxidative stress in WD-fed DBA mice. [2] In thioacetamide (TAA)-intoxicated and bile-duct-ligated (BDL) rats, Obeticholic Acid (30 mg/kg p.o.) reactivates the FXR downstream signaling pathway and decreases portal pressure by lowering total IHVR without deleterious systemic hypotension. [3] |
お薦めの試験操作（参考用のみ）
| 動物試験： |
+ 展開
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溶解度 (25°C)
| 体外 | DMSO | 84 mg/mL (199.7 mM) |
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| Ethanol | 84 mg/mL warmed (199.7 mM) | |
| Water | Insoluble |
* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。
化学情報
| 分子量 | 420.63 |
|---|---|
| 化学式 | C26H44O4 |
| CAS No. | 459789-99-2 |
| 保管 | 粉 |
| in solvent | |
| 別名 | INT-747, 6-ECDCA |
便利ツール
モル濃度計算器
求めたい質量、体積または濃度を計算してください。
質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)
モル濃度計算器方程式
*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA（製品ページで利用可能な）。
希釈計算器
貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます：
開始濃度 x 開始体積 = 最終濃度 x 最終体積
希釈の計算式
この方程式は、一般に略語を使われます：C1V1 = C2V2 ( 入力 出力 )
常に貯蔵液を準備するとき、小びんラベルとMSDS/COA（オンラインで利用できる）で見つかる製品のバッチに特有の分子量を使ってください。
分子量计算器
そのモル質量と元素組成を計算するために、合成物の化学式を入力してください：
チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2
モル濃度計算器
臨床試験
| 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 |
技術サポート
ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。
他に質問がある場合は、お気軽にお問い合わせください。
よくある質問（FAQ）
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質問1：
What formulation can we use to dissolve Obeticholic Acid (Catalog No.S7660) for mice in vivo study?
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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"
