11beta-Hydroxyprogesterone
Based on 4 publication(s) in Google Scholar
11beta-Hydroxyprogesterone is a potent inhibitors of 11β-Hydroxysteroid dehydrogenase; also activates human mineralocorticoid receptor in COS-7 cells with an ED50 of 10 nM.
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- 純度: 99.52%
- CAS 番号: 600-57-7
- 分子式: C21H30O3
- 分子量:330.47
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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MedChemExpress（MCE）の使用を引用している文献 11beta-Hydroxyprogesterone
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生物活性
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Human Endogenous Metabolite |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-7 | EC50 |
50 nM
Compound: 1a
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Transactivation of wild-type human recombinant mineralocorticoid receptor expressed in COS7 cells after 24 hrs by luciferase reporter gene assay
Transactivation of wild-type human recombinant mineralocorticoid receptor expressed in COS7 cells after 24 hrs by luciferase reporter gene assay
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[PMID: 24074876] |
| HEK293 | EC50 |
14 μM
Compound: 1a
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Transactivation of human recombinant mineralocorticoid receptor expressed in HEK-293 cells after 24 hrs by luciferase reporter gene assay
Transactivation of human recombinant mineralocorticoid receptor expressed in HEK-293 cells after 24 hrs by luciferase reporter gene assay
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[PMID: 24074876] |
| HEK293 | IC50 |
0.49 μM
Compound: 1a
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Inhibition of human recombinant 11beta-HSD2 expressed in HEK293 cells assessed as inhibition of [1,2,6,7-3H]-cortisol to [3H]cortisone preincubated for 10 mins before substrate addition by scintillation counting
Inhibition of human recombinant 11beta-HSD2 expressed in HEK293 cells assessed as inhibition of [1,2,6,7-3H]-cortisol to [3H]cortisone preincubated for 10 mins before substrate addition by scintillation counting
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[PMID: 24074876] |
| HEK293 | IC50 |
1.16 μM
Compound: 1a
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Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cells assessed as inhibition of [1,2,-3H]-cortisone to [3H]cortisol preincubated for 10 mins before substrate addition by scintillation counting
Inhibition of human recombinant 11beta-HSD1 expressed in HEK293 cells assessed as inhibition of [1,2,-3H]-cortisone to [3H]cortisol preincubated for 10 mins before substrate addition by scintillation counting
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[PMID: 24074876] |
11OHP displays agonist mineralocorticoid activity. 11β-hydroxyprogesterone activates the transiently expressed hMR in COS-7 cells in a dose-dependent manner with an ED50 of 10 nM and stimulates Ams/sc in mpkCCDcl4 cells. Docking 11β-hydroxyprogesterone within the hMR-ligand-binding domain homology model reveals that the agonist activity of 11OHP is caused by contacts between its 11β-hydroxyl group and Asn770[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.
化学情報
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CAS 番号 600-57-7
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性状 Solid
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分子量 330.47
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分子式 C21H30O3
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Color White to off-white
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SMILES
C[C@@]12[C@]3([H])[C@](CCC1=CC(CC2)=O)([H])[C@@]4([H])[C@@](C)([C@@H](C(C)=O)CC4)C[C@@H]3O
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別名
11β-Hydroxyprogesterone
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Structure Classification
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Initial Source
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (4)
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Journal Impact Factor
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Most Recent
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Cell Metab
Sensing steroid hormone 17α-hydroxypregnenolone by GPR56 enables protection from ferroptosis-induced liver injury. [Abstract]2024 Nov 5;36(11):2402-2418.e10. PMID: 39389061 -
Nat Commun
Coronavirus envelope protein activates TMED10-mediated unconventional secretion of inflammatory factors. [Abstract]2024 Oct 8;15(1):8708. PMID: 39379362 -
Nat Chem Biol
2022 Nov;18(11):1196-1203. PMID: 35982227 -
Proc Natl Acad Sci U S A
2022 Apr 12;119(15):e2117004119. PMID: 35394864
溶剤 & 溶解度
DMSO : 100 mg/mL (302.60 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (7.56 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.56 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 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
プロトコル
Rats: 11α- and 11β-OHP are dissolved in propylene glycol (100%) and infused at 3 and 10 μg/h, respectively, for 14 days. Control rats received vehicle only. BP is measured the day before pumps were implanted and on days 3, 7, 10, and 14 after implantation. Indirect systolic BPs are measured with a modified tail-cuff method[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (280 KB)
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SDS (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Rafestin-Oblin ME, et al. 11beta-hydroxyprogesterone acts as a mineralocorticoid agonist in stimulating Na+ absorption in mammalian principal cortical collecting duct cells. Mol Pharmacol. 2002 Dec;62(6):1306-13. [Content Brief]
[2]. Souness GW, et al. 11 alpha- and 11 beta-hydroxyprogesterone, potent inhibitors of 11 beta-hydroxysteroid dehydrogenase, possess hypertensinogenic activity in the rat. Hypertension. 1996 Mar;27(3 Pt 1):421-5. [Content Brief]
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 (sealed storage, away from moisture). 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 | 3.0260 mL | 15.1300 mL | 30.2599 mL | 75.6498 mL |
| 5 mM | 0.6052 mL | 3.0260 mL | 6.0520 mL | 15.1300 mL | |
| 10 mM | 0.3026 mL | 1.5130 mL | 3.0260 mL | 7.5650 mL | |
| 15 mM | 0.2017 mL | 1.0087 mL | 2.0173 mL | 5.0433 mL | |
| 20 mM | 0.1513 mL | 0.7565 mL | 1.5130 mL | 3.7825 mL | |
| 25 mM | 0.1210 mL | 0.6052 mL | 1.2104 mL | 3.0260 mL | |
| 30 mM | 0.1009 mL | 0.5043 mL | 1.0087 mL | 2.5217 mL | |
| 40 mM | 0.0756 mL | 0.3782 mL | 0.7565 mL | 1.8912 mL | |
| 50 mM | 0.0605 mL | 0.3026 mL | 0.6052 mL | 1.5130 mL | |
| 60 mM | 0.0504 mL | 0.2522 mL | 0.5043 mL | 1.2608 mL | |
| 80 mM | 0.0378 mL | 0.1891 mL | 0.3782 mL | 0.9456 mL | |
| 100 mM | 0.0303 mL | 0.1513 mL | 0.3026 mL | 0.7565 mL |
11beta-Hydroxyprogesterone 関連分類
HY-N2337 関連分類
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