2. Metabolic Enzyme/Protease
  3. Cytochrome P450
  4. 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.

CYP11B1-IN-2 Chemical Structure

CYP11B1-IN-2 Chemical Structure

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CYP11B1-IN-2 Related Antibodies

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP3A4 CYP17A1

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Description

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[1].

IC50 & Target

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)

In Vitro

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 Related Antibodies
In Vivo

CYP11B1-IN-2 (compound 7aa) (25 mg/kg, Orally, once) reduces plasma cortisol concentrations in rats[1].
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.

Animal Model: Adult Sprague-Dawley rats (male, 250-300 g)[1]
Dosage: 25 mg/kg
Administration: Orally, once
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.
Animal Model: Adult Sprague-Dawley rats (male, 250-300 g)[1]
Dosage: 5 mg/kg (IV) or 25 mg/kg (Orally)
Administration: IV or Orally, once
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
Molecular Weight

373.41

Formula

C21H19N5O2
SMILES

[H][C@@]12C(C3=CC=CN=C3)=NO[C@@]1([C@@H]4C[C@H]2CC4)C(NC5=CC6=C(C=C5)NN=C6)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CYP11B1-IN-2 Related Classifications

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The molarity calculator equation

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

CYP11B1-IN-2Cytochrome P450CYPsCortisolCYP11B1orally activeplasmaInhibitorinhibitorinhibit

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