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

CYP11B1-IN-1 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 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)

Cellular Effect
Cell Line Type Value Description References
HEK293 IC20
42 μM
Compound: 25
Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 66 hrs by MTT assay
Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 66 hrs by MTT assay
[PMID: 28570067]
In Vitro

CYP11B1-IN-1 (Compound 25) 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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