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).
For research use only. We do not sell to patients.
- Purity: 99.48%
- CAS No.: 2226133-29-3
- Formula: C27H26Cl2N4O4S
- Molecular Weight:573.49
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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 |
Chemical Information
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CAS No. 2226133-29-3
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Appearance Solid
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Molecular Weight 573.49
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 |
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| 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 Related Classifications
HY-169792 Related Classifications
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