CYP8B1-IN-1
CYP8B1-IN-1 is an orally active CYP8B1 inhibitor (human IC50 = 0.4 nM; mouse IC50 = 0.5 nM). CYP8B1-IN-1 acts by inhibiting cytochrome P450 (Cytochrome P450) 8B1-mediated 12α-hydroxylation in Cholic acid (HY-N0324) synthesis and is selective over other CYP isoforms. CYP8B1-IN-1 can be used in research on non-alcoholic fatty liver disease, type 2 diabetes, and metabolic diseases.
For research use only. We do not sell to patients.
- CAS No.: 2188211-90-5
- Formula: C23H21ClF3N7O
- Molecular Weight:503.91
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
CYP8B1 0.4 nM (IC50, human) |
CYP8B1 0.5 nM (IC50, mouse) |
In Vitro
CYP8B1-IN-1 exhibits acceptable metabolic stability, with a mouse Clint of 261 mL/min/kg and a rhesus monkey Clint of 86 mL/min/kg[1].
CYP8B1-IN-1 is highly selective for the screened CYP subtypes, with over 3000-fold selectivity relative to CYP8B1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD1 (male, 12-15 weeks; Charles River Laboratories)[1]
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Dosage:0.3 mpk, 1 mpk, 3 mpk, and 10 mpk
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Administration:p.o.; single administration; 6 h
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Result:Showed dose-dependent reduction of 7,12-diHCO compared with vehicle.
Plasma exposures were 0.001 μM at 0.3 mpk, 0.003 μM at 1 mpk, 0.02 μM at 3 mpk, and 0.01 μM at 10 mpk.
Chemical Information
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CAS No. 2188211-90-5
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Molecular Weight 503.91
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Formula C23H21ClF3N7O
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SMILES
C[C@@H]1CN(C2=C(C#N)C=NC3=CC=C(Cl)C=C32)CC[C@@H]1C(N4CCN5C(C4)=NN=C5C(F)(F)F)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CYP8B1-IN-1 Related Classifications
HY-189878 Related Classifications
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