| 规格 | 价格 | 库存 | 数量 |
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| 10 mM * 1 mL in DMSO |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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| 靶点 |
FXR (EC50: 99 nM)
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| 体外研究 (In Vitro) |
在大鼠肝细胞中，奥贝胆酸 (INT-747) 会提高 FXR 调节基因的表达[1]。奥贝胆酸 (INT-747) 可降低肝脏 JNK-1 和 JNK-2 表达[2]。在每个检查的菌株中，256 μg/mL 的奥贝胆酸 (INT-747) 完全抑制细菌生长。将INT-747添加到暴露于IFN-γ的Caco-2细胞的肠上皮中后，肠通透性没有改变[3]。
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| 体内研究 (In Vivo) |
奥贝胆酸 (INT-747)（10 毫克/公斤/天）完全逆转了 E217α 引起的胆汁淤积。通过提高 β-MCA、TCDCA 和 TDCA 的相对丰度，奥贝胆酸 (INT-747) 的给药可部分逆转 E217α 引起的总胆汁酸分泌受损[1]。在小鼠中，奥贝胆酸 (INT-747)7 (10 mg/kg) 和 HS 会加剧肺充血。在接受 HS 治疗的动物中，INT-747 不会改善肾脏病理学[2]。在 BDL 大鼠中，奥贝胆酸 (INT-747) (5 mg/kg) 显着提高了存活率。用奥贝胆酸 (INT-747) 治疗的 BDL 大鼠显示，仅在回肠中，闭孔claudin-1 的表达显着增加。使用 INT-747 治疗的 BDL 大鼠的回肠中 ZO-1 显着上调[3]。
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| 细胞实验 |
大鼠肝细胞暴露于1μM 6-ECDCA引起小异二聚体伴侣（Shp）和胆盐输出泵（bsep）mRNA的3-5倍诱导，胆固醇7α羟化酶（cyp7a1）、氧化甾醇12β羟化酶（cyp8b1）和Na（+）/牛磺胆酸盐共转运肽（ntcp）减少70-80%[2]。
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| 动物实验 |
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| 参考文献 |
[1]. Pellicciari R, et al. 6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity. J Med Chem. 2002 Aug 15;45(17):3569-72.
[2]. Fiorucci S, et al. Protective effects of 6-ethyl chenodeoxycholic acid, a farnesoid X receptor ligand, in estrogen-induced cholestasis. J Pharmacol Exp Ther. 2005 May;313(2):604-12. [3]. Ghebremariam YT, et al. FXR agonist INT-747 upregulates DDAH expression and enhances sensitivity in high-salt fed Dahl rats. PLoS One. 2013 Apr 4;8(4):e60653. [4]. Verbeke L, et al. The FXR Agonist Obeticholic Acid Prevents Gut Barrier Dysfunction and Bacterial Translocation in Cholestatic Rats. Am J Pathol. 2015 Feb;185(2):409-19 |
| 分子式 |
C26H44O4
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|---|---|---|
| 分子量 |
420.63
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| 精确质量 |
420.323959
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| 元素分析 |
C, 74.24; H, 10.54; O, 15.21
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| CAS号 |
459789-99-2
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| 相关CAS号 |
Obeticholic acid-d5;1992000-80-2;Obeticholic Acid-d4
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| 外观&性状 |
White to off-white solid powder
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| LogP |
5.7
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| tPSA |
77.8A^2
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| SMILES |
C[C@@H]([ C@H]1CC[C@@]2([H])[C@]3([H])[ C@H](O)[ C@H](CC)[C@]4([H])C[ C@H](O)CC[C@]4(C)[C@@]3([H])CC[C@]12C)CCC(O)=O
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| InChi Key |
ZXERDUOLZKYMJM-ZWECCWDJSA-N
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| InChi Code |
InChI=1S/C26H44O4/c1-5-17-21-14-16(27)10-12-26(21,4)20-11-13-25(3)18(15(2)6-9-22(28)29)7-8-19(25)23(20)24(17)30/h15-21,23-24,27,30H,5-14H2,1-4H3,(H,28,29)/t15-,16-,17-,18-,19+,20+,21+,23+,24-,25-,26-/m1/s1
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| 化学名 |
(4R)-4-[(3R,5S,6R,7R,8S,9S,10S,13R,14S,17R)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoic acid
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| 别名 |
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| HS Tariff Code |
2934.99.9001
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 溶解度 (体外) |
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| 溶解度 (体内) |
Solubility in Formulation 1: ≥ 5 mg/mL (11.89 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (11.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 4.76 mg/mL (11.32 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.5 mg/mL (5.94 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (5.94 mM) (saturation unknown) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 6: ≥ 2.5 mg/mL (5.94 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 7: ≥ 2.5 mg/mL (5.94 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 8: 5 mg/mL (11.89 mM) in 1% Methylcellulose(MC) (add these co-solvents sequentially from left to right, and one by one), Suspension solution; with ultrasonication. 1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL； 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果，工作液请现配现用！ 6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3774 mL | 11.8869 mL | 23.7739 mL | |
| 5 mM | 0.4755 mL | 2.3774 mL | 4.7548 mL | |
| 10 mM | 0.2377 mL | 1.1887 mL | 2.3774 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
计算结果:
工作液浓度： mg/mL；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
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Glyco-obeticholic acid-d5 (obeticholic acid impurity 8-d5)
ZLY28
FXRagonist 4
Tauro-β-muricholic acid-d4 sodium
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