CYP11B1-IN-2
CYP11B1-IN-2 (compound 7aa) is an orally active, potent and selective CYP11B1 inhibitor, with IC50 values of 9 nM and 25 nM for human CYP11B1 and rat CYP11B1, respectively. CYP11B1-IN-2 can be used for the research of diseases caused by excessive cortisol.
For research use only. We do not sell to patients.
- CAS No.: 3031098-46-8
- Formula: C21H19N5O2
- Molecular Weight:373.41
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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CYP11B1 9 ± 2 nM (IC50, human CYP11B1) |
CYP11B1 25 nM (IC50, rat CYP11B1) |
CYP11B2 1121 ± 237 nM (IC50) |
CYP1A2 >10 μM (IC50) |
CYP2C9 >10 μM (IC50) |
CYP2C19 >10 μM (IC50) |
CYP2D6 >10 μM (IC50) |
CYP2E1 >10 μM (IC50) |
CYP3A4 >10 μM (IC50) |
CYP11B1-IN-2 (compound 7aa) exhibits good selectivity over a panel of hepatic CYP enzymes, such as CYP1A2, CYP2C9, CYP2C19, CYP3A4, CYP2D6, and CYP2E1 with IC50 values greater than 10 μM[1].
CYP11B1-IN-2 presents a cLog P of 3.12, indicating a good balance between lipophilicity and hydrophilicity, which was further manifested by an aqueous solubility of 196 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
CYP11B1-IN-2 (5 mg/kg (IV) or 25 mg/kg (Orally); once) has a maximum plasma concentration of 12 686 μg/L, with similar terminal half-lives of around 4.5 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult Sprague-Dawley rats (male, 250-300 g)[1]
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Dosage:25 mg/kg
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Administration:Orally, once
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Result:Strongly reduced the plasma concentrations of cortisol from 376 ± 22 to 28 ± 5 ng/L after a dose of 25 mg/kg body weight per oral in rats.
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Animal Model:Adult Sprague-Dawley rats (male, 250-300 g)[1]
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Dosage:5 mg/kg (IV) or 25 mg/kg (Orally)
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Administration:IV or Orally, once
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Result:Pharmacokinetic Parameters of CYP11B1-IN-2 in male Sprague-Dawley rats[1].
IV (5 mg/kg) PO (25 mg/kg) Tmax (h) 0 4.2 ± 0.2 Cmax (μg/L) 12 685.7 ± 421.3 7993.3 ± 478.7 AUC0-∞ (μg/L·h) 50 928.7 ± 982.6 54 539.2 ± 1633.9 T1/2 (h) 4.5 ± 0.4 4.6 ± 0.2 CL (mL/h/kg) 17.2 ± 1.2 F (%) 21.4