HPG1860
Based on 1 Customer Validation
HPG1860 is an orally active, highly selective and potent FXR agonist, with an EC50 of 18 nM (FXR-luciferase reporter assay). HPG1860 has EC50 values >30.0 μM for TGR5 and 13 other related nuclear receptors (cAMP biological assay). HPG1860 can be used for the research of non-alcoholic steatohepatitis (NASH).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.48%
- CAS 番号: 2226133-29-3
- 分子式: C27H26Cl2N4O4S
- 分子量:573.49
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
HPG1860 (Compound 23) shows EC50 values of 5 nM and 18 nM for FXR by time-resolved fluorescence energy transfer (TR-FRET) and luciferase reporter assays, respectively[1].
HPG1860 shows good stability in liver microsomes of human, rat, dog and monkey with t1/2 of 447.18, 115.79, 237.17 and 154.38 min, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
HPG1860 (1-10 mg/kg, p.o., once a day, 27 days) shows potent antifibrosis and anti-NASH activities in a mouse model of NASH induced by a high-fat diet and Carbon tetrachloride (HY-Y0298)[1].
HPG1860 shows favorable pharmacokinetics profile[1].
Pharmacokinetic parameters of HPG1860 in mice, rats, and dogs
| mouse | mouse | rat | rat | dog | dog | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| parameters | 1 mg/kg (i.v.) | 5 mg/kg (p.o.) | 3 mg/kg (i.v.) | 9 mg/kg (p.o.) | 1 mg/kg (i.v.) | 3 mg/kg (p.o.) | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Cmax (ng/mL) | NA | 3610 | NA | 1947 | NA | 1709 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Tmax (h) | NA | 0.25 | NA | 0.5 | NA | 1 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| AUC(0-t) (h × ng/mL) | 1006 | 3883 | 2611 | 4121 | 4591 | 8270 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| T1/2 (h) | 1.6 | 1.52 | 1.44 | 2.10 | 4.07 | 9.90 | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| CL (mL/min/kg) | 16.5 | NA | 18 | NA | 3.63 | NA | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Vss (L/kg) | 0.53 | NA | 29.3 | NA | 0.823 | NA | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| F (%) | NA | 77.2 | NA | 52.1 | NA | 59.4 |
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2226133-29-3
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性状 Solid
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分子量 573.49
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分子式 C27H26Cl2N4O4S
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Color White to off-white
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SMILES
ClC(C=CC=C1Cl)=C1C2=NOC(C3CC3)=C2CN4C[C@H](N(C5=NC6=C(OC)C=C(C(O)=O)C=C6S5)CC4)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 71.43 mg/mL (124.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (277 KB)
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SDS (251 KB)
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- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7437 mL | 8.7185 mL | 17.4371 mL | 43.5927 mL |
| 5 mM | 0.3487 mL | 1.7437 mL | 3.4874 mL | 8.7185 mL | |
| 10 mM | 0.1744 mL | 0.8719 mL | 1.7437 mL | 4.3593 mL | |
| 15 mM | 0.1162 mL | 0.5812 mL | 1.1625 mL | 2.9062 mL | |
| 20 mM | 0.0872 mL | 0.4359 mL | 0.8719 mL | 2.1796 mL | |
| 25 mM | 0.0697 mL | 0.3487 mL | 0.6975 mL | 1.7437 mL | |
| 30 mM | 0.0581 mL | 0.2906 mL | 0.5812 mL | 1.4531 mL | |
| 40 mM | 0.0436 mL | 0.2180 mL | 0.4359 mL | 1.0898 mL | |
| 50 mM | 0.0349 mL | 0.1744 mL | 0.3487 mL | 0.8719 mL | |
| 60 mM | 0.0291 mL | 0.1453 mL | 0.2906 mL | 0.7265 mL | |
| 80 mM | 0.0218 mL | 0.1090 mL | 0.2180 mL | 0.5449 mL | |
| 100 mM | 0.0174 mL | 0.0872 mL | 0.1744 mL | 0.4359 mL |
HPG1860 関連分類
HY-169792 関連分類
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