2. Metabolic Enzyme/Protease
  3. FXR Aminotransferases (Transaminases)
  4. HPG1860

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.

HPG1860

HPG1860 Chemical Structure

CAS No. : 2226133-29-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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HPG1860 Related Antibodies

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Description

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)[1].

In Vitro

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 Related Antibodies
In Vivo

HPG1860 (3 mg/kg, p.o.) significantly promotes the expression of FXR target genes (SHP, BSEP and FGF15) in liver and ileum[1].
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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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
Animal Model: Male C57BL/6 mice (7 weeks of age) maintained with a high-fat diet (for 11 weeks) and intraperitoneally injected with 25% CCl4 (twice a week for the final 4 weeks)[1]
Dosage: 1, 3, and 10 mg/kg
Administration: Intraperitoneal injection (i.p.), once a day, 27 days
Result: Decreased markers of liver injury ALT and AST at all tested doses with AST level comparable to that of the CCl4-untreated mice.
Resulted in statistically significant NAFLD activity score (NAS) improvement.
Alleviated steatosis in a dose-dependent manner, with complete clearance of steatosis at 10 mg/kg.
Alleviated live inflammation while Obeticholic acid (HY-12222) barely affected liver inflammation.
Exhibited modest amelioration of fibrosis.
Clinical Trial
Molecular Weight

573.49

Formula

C27H26Cl2N4O4S
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7437 mL 8.7185 mL 17.4371 mL
5 mM 0.3487 mL 1.7437 mL 3.4874 mL
View the 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.

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
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
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
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HPG1860 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HPG18602226133-29-3HPG 1860HPG-1860FXRAminotransferases (Transaminases)NR1H4NASHAntifibrosisCaco-2InflammationOCAHFDSteatosisInhibitorinhibitorinhibit

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