Art. -Nr.: HY-135281

CYP11B2-IN-1

Name: CYP11B2-IN-1
Brand: MedChemExpress
SKU: HY-135281
Price: 120.00 USD
Availability: InStock
Rating: 5 (1 reviews)

Kundenbewertung

Based on 1 Customer Validation

CYP11B2-IN-1 is a CYP11B2 inhibitor with an IC₅₀ of 2.3 nM. CYP11B2-IN-1 inhibits CYP11B1 with an IC₅₀ of 142 nM.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.83%
CAS. Nr.: 1356479-78-1
Formel: C₁₈H₁₈FN₃O
Molecular Weight:311.35

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CYP11B2-IN-1 Chemical Structure

CAS. Nr.: 1356479-78-1

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

CYP11B2-IN-1 is a CYP11B2 inhibitor with an IC₅₀ of 2.3 nM. CYP11B2-IN-1 inhibits CYP11B1 with an IC₅₀ of 142 nM^[1].

IC₅₀ & Target

^[1]

CYP11B2

2.3 nM (IC₅₀)

CYP11B1

142 nM (IC₅₀)

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
COS-7	IC₅₀	>10000 nM Compound: 32	Inhibition of human CYP21 expressed in COS7 cells incubated for 1 hr before 17-hydroxypregnenolone substrate addition by HTRF-based assay Inhibition of human CYP21 expressed in COS7 cells incubated for 1 hr before 17-hydroxypregnenolone substrate addition by HTRF-based assay	[PMID: 26005536]
COS-7	IC₅₀	>10000 nM Compound: 32	Inhibition of human CYP17 expressed in COS7 cells incubated for 1 hr before 17-hydroxypregnenolone substrate addition by EIA method Inhibition of human CYP17 expressed in COS7 cells incubated for 1 hr before 17-hydroxypregnenolone substrate addition by EIA method	[PMID: 26005536]
V79	IC₅₀	0.3 nM Compound: 32	Inhibition of rhesus monkey CYP11B2 expressed in V79 cells incubated for 1 hr before 11-deoxycorticosterone substrate addition by HTRF-based assay Inhibition of rhesus monkey CYP11B2 expressed in V79 cells incubated for 1 hr before 11-deoxycorticosterone substrate addition by HTRF-based assay	[PMID: 26005536]
V79	IC₅₀	142 nM Compound: 32	Inhibition of human CYP11B1 expressed in V79 cells incubated for 1 hr before 11-deoxycortisol substrate addition by HTRF-based assay Inhibition of human CYP11B1 expressed in V79 cells incubated for 1 hr before 11-deoxycortisol substrate addition by HTRF-based assay	[PMID: 26005536]
V79	IC₅₀	2.3 nM Compound: 32	Inhibition of human CYP11B2 expressed in V79 cells incubated for 1 hr before 11-deoxycorticosterone substrate addition by HTRF-based assay Inhibition of human CYP11B2 expressed in V79 cells incubated for 1 hr before 11-deoxycorticosterone substrate addition by HTRF-based assay	[PMID: 26005536]
V79	IC₅₀	1.4 nM Compound: 1	Inhibition of human CYP11B2-CLE9 expressed in Chinese hamster V79 cells using 11-deoxycorticosterone as substrate preincubated for 1 hr followed by substrate addition measured after 3 hrs by HTRF assay Inhibition of human CYP11B2-CLE9 expressed in Chinese hamster V79 cells using 11-deoxycorticosterone as substrate preincubated for 1 hr followed by substrate addition measured after 3 hrs by HTRF assay	[PMID: 27979595]
V79	IC₅₀	100 nM Compound: 1	Inhibition of human CYP11B1-8C7 expressed in Chinese hamster V79 cells using 11-deoxycortisol as substrate preincubated for 1 hr followed by substrate addition measured after 3 hrs by HTRF assay Inhibition of human CYP11B1-8C7 expressed in Chinese hamster V79 cells using 11-deoxycortisol as substrate preincubated for 1 hr followed by substrate addition measured after 3 hrs by HTRF assay	[PMID: 27979595]

In Vitro

CYP11B2-IN-1 (Compound 32) also inhibits CYP19 with an IC₅₀ of 1021 nM^{[1] .}

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

In Vivo

In a rhesus pharmacodynamic model, CYP11B2-IN-1 (Compound 32) produces dose-dependent aldosterone lowering efficacy, with no apparent effect on cortisol levels^[1].
CYP11B2-IN-1also displays a good rhesus pharmacokinetics profile, with low plasma clearance and acceptable oral exposure.When dosed i.v. at 0.01 and 0.3 mg/kg, CYP11B2-IN-1 produces reductions in aldosterone AUC of 62% and 95%, respectively, compared to baseline^[1].

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

Chemical Information

CAS. Nr. 1356479-78-1
Appearance Solid
Molecular Weight 311.35
Formel C₁₈H₁₈FN₃O
Color Off-white to light yellow
SMILES

OC(C)(C)C1=CC(C2=NC3=CC=C(F)C=C3N2C4CC4)=CN=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (321.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.2118 mL

16.0591 mL

32.1182 mL

5 mM

0.6424 mL

3.2118 mL

6.4236 mL

10 mM

0.3212 mL

1.6059 mL

3.2118 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (8.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.03 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Hoyt SB, et al. Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.ACS Med Chem Lett. 2015 Apr 7;6(5):573-8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.2118 mL	16.0591 mL	32.1182 mL	80.2955 mL
	5 mM	0.6424 mL	3.2118 mL	6.4236 mL	16.0591 mL
	10 mM	0.3212 mL	1.6059 mL	3.2118 mL	8.0295 mL
	15 mM	0.2141 mL	1.0706 mL	2.1412 mL	5.3530 mL
	20 mM	0.1606 mL	0.8030 mL	1.6059 mL	4.0148 mL
	25 mM	0.1285 mL	0.6424 mL	1.2847 mL	3.2118 mL
	30 mM	0.1071 mL	0.5353 mL	1.0706 mL	2.6765 mL
	40 mM	0.0803 mL	0.4015 mL	0.8030 mL	2.0074 mL
	50 mM	0.0642 mL	0.3212 mL	0.6424 mL	1.6059 mL
	60 mM	0.0535 mL	0.2677 mL	0.5353 mL	1.3383 mL
	80 mM	0.0401 mL	0.2007 mL	0.4015 mL	1.0037 mL
	100 mM	0.0321 mL	0.1606 mL	0.3212 mL	0.8030 mL

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

CYP11B2-IN-1

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen