CYP11B2-IN-1
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.
For research use only. We do not sell to patients.
- Purity: 99.83%
- CAS No.: 1356479-78-1
- Formula: C18H18FN3O
- Molecular Weight:311.35
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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CYP11B2 2.3 nM (IC50) |
CYP11B1 142 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-7 | IC50 |
>10000 nM
Compound: 32
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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
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[PMID: 26005536] |
| COS-7 | IC50 |
>10000 nM
Compound: 32
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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
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[PMID: 26005536] |
| V79 | IC50 |
0.3 nM
Compound: 32
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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
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[PMID: 26005536] |
| V79 | IC50 |
142 nM
Compound: 32
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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
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[PMID: 26005536] |
| V79 | IC50 |
2.3 nM
Compound: 32
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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
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[PMID: 26005536] |
| V79 | IC50 |
1.4 nM
Compound: 1
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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
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[PMID: 27979595] |
| V79 | IC50 |
100 nM
Compound: 1
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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
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[PMID: 27979595] |
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.
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
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CAS No. 1356479-78-1
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Appearance Solid
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Molecular Weight 311.35
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Formula C18H18FN3O
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Color Off-white to light yellow
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SMILES
OC(C)(C)C1=CC(C2=NC3=CC=C(F)C=C3N2C4CC4)=CN=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (273 KB)
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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)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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.
| 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 |
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