| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 100mg | |||
| 500mg |
| Targets |
11beta-Hydroxyprogesterone targets 11β-Hydroxysteroid dehydrogenase, acting as a potent inhibitor of this enzyme. It also targets the human mineralocorticoid receptor (hMR), functioning as a mineralocorticoid agonist and activating hMR in a dose-dependent manner with an ED50 of 10 nM. Docking studies within the hMR-ligand-binding domain reveal that its agonist activity is caused by contacts between its 11β-hydroxyl group and Asn770.
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| ln Vitro |
11OHP functions as a mineralocorticoid agonist. 11β-hydroxyprogesterone activates 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 its agonist activity is caused by contacts between its 11β-hydroxyl group and Asn770 [1].
In vitro, 11beta-Hydroxyprogesterone functions as a mineralocorticoid agonist. It activates hMR in COS-7 cells in a dose-dependent manner with an ED50 of 10 nM and stimulates Ams/sc in mpkCCDcl4 cells. Docking studies within the hMR-ligand-binding domain reveal that its agonist activity is caused by contacts between its 11β-hydroxyl group and Asn770. The compound is a potent inhibitor of 11β-Hydroxysteroid dehydrogenase. |
| ln Vivo |
11β-hydroxyprogesterone raises blood pressure significantly within 3 days and continues to do so throughout the 14-day infusion. In rats, 11β-hydroxyprogesterone has a strong hypertensive effect, which is dependent on an intact adrenal gland and the activation of mineralocorticoid receptors [2].
In vivo, 11beta-Hydroxyprogesterone raises blood pressure significantly within 3 days and continues to do so throughout a 14-day infusion in rats. In rats, the compound has a strong hypertensive effect which is dependent on an intact adrenal gland and the activation of mineralocorticoid receptors. It can confer mineralocorticoid activity on corticosterone in the rat in vivo. The compound is an endogenous metabolite with roles in progesterone regulation. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for 11beta-Hydroxyprogesterone involve measuring inhibition of 11β-Hydroxysteroid dehydrogenase activity. Enzyme activity is assessed by monitoring the conversion of substrates to products. Mineralocorticoid receptor binding is assessed using radioligand binding displacement studies with membranes from cells expressing hMR. Functional activation is measured by assessing hMR-mediated transcription in reporter gene assays. The compound's ED50 of 10 nM for hMR activation is determined through dose-response curves. Docking studies are performed to characterize receptor-ligand interactions.
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| Cell Assay |
In vitro cell-based assays for 11beta-Hydroxyprogesterone are conducted in COS-7 cells and mpkCCDcl4 cells expressing hMR. Cells are cultured in appropriate media and treated with the compound at varying concentrations. hMR activation is assessed by measuring mineralocorticoid receptor-mediated transcription using luciferase reporter gene assays. The ED50 of 10 nM is determined from dose-response curves. Stimulation of Ams/sc in mpkCCDcl4 cells is measured. Cell viability is assessed by standard assays. Experiments are performed in triplicate with appropriate positive and negative controls.
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| Animal Protocol |
11beta-Hydroxyprogesterone in vivo studies are conducted in rat models to assess its hypertensive effects. Animals are infused with the compound for 14 days, and blood pressure is monitored. The hypertensive effect is dependent on an intact adrenal gland and mineralocorticoid receptor activation. For metabolic studies, animals are administered the compound and its effects on progesterone levels are assessed. Blood samples are collected for pharmacokinetic and biochemical analysis. Animals are monitored for clinical signs. Studies are conducted in accordance with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
11beta-Hydroxyprogesterone (MW 330.46 g/mol, C21H30O3) is an endogenous metabolite and 11β-hydroxy steroid. It appears as a white to off-white solid powder with a density of 1.15 g/cm³ and a boiling point of 487.4°C. The compound has a logP of 3.694. It is a metabolite in both humans and mice. Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution would be determined in species-specific studies. The compound is typically used in endocrine and metabolic research.
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| Toxicity/Toxicokinetics |
11beta-Hydroxyprogesterone is generally well-tolerated in preclinical studies. The compound is an endogenous metabolite with a role in progesterone regulation. Its hypertensive effects have been demonstrated in rat models at certain doses. No significant adverse effects have been reported in the available literature at research-use concentrations beyond its pharmacological effects. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation would be required for therapeutic development.
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| References |
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| Additional Infomation |
11β-hydroxyprogesterone is an 11β-hydroxy steroid formed by replacing the β-hydroxy group at the 11-position of progesterone. It is a metabolite in both humans and mice. Its function is related to progesterone.
11beta-Hydroxyprogesterone (11β-Hydroxyprogesterone) is an endogenous metabolite and potent inhibitor of 11β-Hydroxysteroid dehydrogenase that activates the human mineralocorticoid receptor (hMR) with an ED50 of 10 nM. It raises blood pressure in rats through mineralocorticoid receptor activation. Docking studies reveal its agonist activity is mediated by contacts between its 11β-hydroxyl group and Asn770. The compound is a metabolite in humans and mice with function related to progesterone. All applications are limited to non-human research use. |
| Molecular Formula |
C21H30O3
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|---|---|
| Molecular Weight |
330.46100
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| Exact Mass |
330.219
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| CAS # |
600-57-7
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| PubChem CID |
101788
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| Appearance |
White to off-white solid powder
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| Density |
1.15g/cm3
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| Boiling Point |
487.4ºC at 760 mmHg
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| Flash Point |
262.7ºC
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| Index of Refraction |
1.557
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| LogP |
3.694
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
24
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| Complexity |
621
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| Defined Atom Stereocenter Count |
7
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| SMILES |
CC(=O)[C@H]1CC[C@@H]2[C@@]1(C[C@@H]([C@H]3[C@H]2CCC4=CC(=O)CC[C@]34C)O)C
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| InChi Key |
BFZHCUBIASXHPK-ATWVFEABSA-N
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| InChi Code |
InChI=1S/C21H30O3/c1-12(22)16-6-7-17-15-5-4-13-10-14(23)8-9-20(13,2)19(15)18(24)11-21(16,17)3/h10,15-19,24H,4-9,11H2,1-3H3/t15-,16+,17-,18-,19+,20-,21+/m0/s1
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| Chemical Name |
(8S,9S,10R,11S,13S,14S,17S)-17-acetyl-11-hydroxy-10,13-dimethyl-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-3-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~75.65 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.57 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.57 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0261 mL | 15.1304 mL | 30.2608 mL | |
| 5 mM | 0.6052 mL | 3.0261 mL | 6.0522 mL | |
| 10 mM | 0.3026 mL | 1.5130 mL | 3.0261 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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