2. Metabolic Enzyme/Protease
  3. Cytochrome P450
  4. CYP11B1-IN-1

CYP11B1-IN-1 (Compound 25) is a selective, orally active hCYP11B1 inhibitor, with an IC50 of 2 nM against hCYP11B1 and an IC50 of 1.8 μM against rat CYP11B1. CYP11B1-IN-1 can be used for the research of Cushing's disease.

For research use only. We do not sell to patients.

CYP11B1-IN-1

CYP11B1-IN-1 Chemical Structure

CAS No. : 2101952-78-5

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CYP11B1-IN-1 Related Antibodies

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

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Description

CYP11B1-IN-1 (Compound 25) is a selective, orally active hCYP11B1 inhibitor, with an IC50 of 2 nM against hCYP11B1 and an IC50 of 1.8 μM against rat CYP11B1. CYP11B1-IN-1 can be used for the research of Cushing's disease[1].

IC50 & Target[1]

CYP11B1

1.8 nM (IC50)

CYP11B2

27 nM (IC50)

In Vitro

CYP11B1-IN-1 potently inhibits hCYP11B1 (IC50 = 2 nM), and exhibits 14-fold higher selectivity for hCYP11B1 over hCYP11B2 in V79MZ hamster fibroblasts expressing recombinant enzymes[1].
CYP11B1-IN-1 inhibits rat CYP11B1, with an IC50 of 1.8 μM in V79MZ hamster fibroblasts expressing this recombinant enzyme[1].
CYP11B1-IN-1 (1 μM; 0-60 min) exhibits superior metabolic stability in rat liver S9 fractions, with a half-life of 23 min, which is better than that of Ref 7 and metyrapone[1].
CYP11B1-IN-1 (6.25-100 μM; 66 h) shows no cytotoxicity in HEK293 cells, with an IC20 value of up to 42 μM[1].
CYP11B1-IN-1 (up to 100 μM) shows no mutagenic potential in *Salmonella typhimurium* strains TA98 and TAMix, with or without metabolic activation by rat liver S9 fraction[1].
CYP11B1-IN-1 (3.16 μM; 48 h) does not activate the aryl hydrocarbon receptor in HepG2 cells[1].

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

CYP11B1-IN-1 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: HEK293 cells
Concentration: 6.25-100 μM
Incubation Time: 66 h
Result: Showed no effect on cellular viability up to 42 μM (IC20 value).
Parmacokinetics
Species Dose Route Cmax Tmax T1/2 AUC0-∞ F Vdss CL
Rat[1] 5 mg/kg i.v. 27.8 μM / 4.8 h 3677 ng·h/mL / 3.1 L/kg 22.6 mL/min/kg
Rat[1] 28 mg/kg p.o. 6.4 μM 2.5 h 3.3 h 10220 ng·h/mL 50 % / /
Molecular Weight

266.30

Formula

C16H14N2O2
CAS No.
SMILES

N=1C=C(OC)C=C(C1)CC=2ON=C(C2)C=3C=CC=CC3
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-1 Related Classifications

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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-12101952-78-5Cytochrome P450CYPshuman liver S9 fractionV79MZ hamster fibroblastsCYP11B2CYP19A1Salmonella typhimuriumCYP17A1cushing’s diseaseCYP11B1rat liver S9 fractionHEK293 cellsInhibitorinhibitorinhibit

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