BMS-816336
Based on 1 Customer Validation
BMS-816336 is a novel, potent and orally bioavailable inhibitor against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with an IC50 of 3.0 nM.
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- Purity: 99.86%
- CAS No.: 1009583-20-3
- 화학식: C21H27NO3
- 분자량:341.44
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보관: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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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Metabolism/Protease Compound Library
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Biological Activity
IC50: 3.0 nM (11β-HSD1)[1]
11β-HSD1 inhibition may be useful in the treatment of type II diabetes and other potential clinical utilities such as atheroprotection and cognitive protection. BMS-816336 (6n-2) inhibits 11β-HSD1 enzyme in HEK and 3T3L1 cells with IC50s of 37.3 and 28.6 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nonfasting diet-induced obese male mice[1]
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Dosage:1, 3, 10, 30, 100 mg/kg
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Administration:Oral, 120 mintues
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Result:ED50=8.6 mg/kg and a plasma EC50 of 0.85 μM in this model[1].
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1009583-20-3
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Appearance Solid
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분자량 341.44
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화학식 C21H27NO3
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Color White to off-white
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SMILES
O[C@@H]1[C@H]2C[C@@H]3[C@@](C4=CC=CC=C4)(CC(N5CC(O)C5)=O)[C@@H](C[C@H]1C3)C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 300 mg/mL (878.63 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: ≥ 7.5 mg/mL (21.97 mM); Clear solution
This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 7.5 mg/mL (21.97 mM); Clear solution
This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
순도&문서
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Data Sheet (275 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)
- Korean - KR (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 |
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| DMSO | 1 mM | 2.9288 mL | 14.6439 mL | 29.2877 mL | 73.2193 mL |
| 5 mM | 0.5858 mL | 2.9288 mL | 5.8575 mL | 14.6439 mL | |
| 10 mM | 0.2929 mL | 1.4644 mL | 2.9288 mL | 7.3219 mL | |
| 15 mM | 0.1953 mL | 0.9763 mL | 1.9525 mL | 4.8813 mL | |
| 20 mM | 0.1464 mL | 0.7322 mL | 1.4644 mL | 3.6610 mL | |
| 25 mM | 0.1172 mL | 0.5858 mL | 1.1715 mL | 2.9288 mL | |
| 30 mM | 0.0976 mL | 0.4881 mL | 0.9763 mL | 2.4406 mL | |
| 40 mM | 0.0732 mL | 0.3661 mL | 0.7322 mL | 1.8305 mL | |
| 50 mM | 0.0586 mL | 0.2929 mL | 0.5858 mL | 1.4644 mL | |
| 60 mM | 0.0488 mL | 0.2441 mL | 0.4881 mL | 1.2203 mL | |
| 80 mM | 0.0366 mL | 0.1830 mL | 0.3661 mL | 0.9152 mL | |
| 100 mM | 0.0293 mL | 0.1464 mL | 0.2929 mL | 0.7322 mL |
BMS-816336 Related Classifications
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