| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
The primary target of Chlormadinone is the progesterone receptor (PR). It acts as a potent agonist at PR, mimicking the effects of natural progesterone. It also has antiandrogenic properties due to weak antagonism of the androgen receptor.
|
|---|---|
| ln Vitro |
In vitro, Chlormadinone binds to the human progesterone receptor with high affinity (relative binding affinity approximately 60% compared to progesterone). It exhibits minimal binding to estrogen and glucocorticoid receptors, showing good selectivity.
|
| ln Vivo |
In vivo, Chlormadinone produces typical progestogenic effects including endometrial transformation, inhibition of ovulation, and cervical mucus thickening. It has been shown to suppress luteinizing hormone (LH) surge and maintain pregnancy in animal models.
|
| Enzyme Assay |
Not specified for this compound. Standard receptor binding assays for progestins use cytosolic or recombinant progesterone receptor preparations. Competitive binding with [3H]R5020 (a synthetic progestin) is performed, and bound radioactivity is separated by charcoal adsorption or filtration.
|
| Cell Assay |
Standard cell-based assays for progestin activity use T47D breast cancer cells, which express endogenous PR. Cells are treated with the compound, and alkaline phosphatase activity or reporter gene expression (e.g., MMTV-luciferase) is measured after 24-48 hours.
|
| Animal Protocol |
In vivo assays for progestational activity include the Clauberg test in estrogen-primed immature rabbits. The compound is administered subcutaneously or orally for several days, and endometrial proliferation is histologically evaluated and scored.
|
| ADME/Pharmacokinetics |
Chlormadinone is well absorbed after oral administration. It is highly protein-bound (approximately 97%) and has a half-life of about 30-40 hours. It undergoes hepatic metabolism primarily by reduction and hydroxylation, followed by glucuronide conjugation.
|
| Toxicity/Toxicokinetics |
Chlormadinone is generally well tolerated at therapeutic doses. Potential side effects include weight gain, mood changes, breast tenderness, and thromboembolic risk (shared with other progestin-estrogen combinations). It is contraindicated during pregnancy.
|
| References |
[1]. Okada H, et al. Tamsulosin and chlormadinone for the treatment of benign prostatic hyperplasia. The Kobe University YM617 Study Group. Scand J Urol Nephrol. 1996 Oct;30(5):379-85.
|
| Additional Infomation |
A synthetic progestin that is effective orally and is often used in combination with other drugs as an oral contraceptive.
Chlormadinone acetate is approved in many countries as a component of combined oral contraceptives and as monotherapy for menopausal hormone therapy. It has antiandrogenic properties useful for treating androgen-related conditions like acne and hirsutism. |
| Molecular Formula |
C21H27CLO3
|
|---|---|
| Molecular Weight |
362.89
|
| Exact Mass |
362.165
|
| CAS # |
1961-77-9
|
| Related CAS # |
Chlormadinone-d6
|
| PubChem CID |
5284533
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.24 g/cm3
|
| Boiling Point |
506.7ºC at 760 mmHg
|
| Melting Point |
213°C
|
| Flash Point |
260.2ºC
|
| Vapour Pressure |
2.18E-12mmHg at 25°C
|
| Index of Refraction |
1.582
|
| LogP |
4.18
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
25
|
| Complexity |
723
|
| Defined Atom Stereocenter Count |
6
|
| SMILES |
CC(=O)[C@]1(CC[C@H]2[C@@H]3C=C(C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C)Cl)O
|
| InChi Key |
VUHJZBBCZGVNDZ-TTYLFXKOSA-N
|
| InChi Code |
InChI=1S/C21H27ClO3/c1-12(23)21(25)9-6-16-14-11-18(22)17-10-13(24)4-7-19(17,2)15(14)5-8-20(16,21)3/h10-11,14-16,25H,4-9H2,1-3H3/t14-,15+,16+,19-,20+,21+/m1/s1
|
| Chemical Name |
(8R,9S,10R,13S,14S,17R)-17-acetyl-6-chloro-17-hydroxy-10,13-dimethyl-2,8,9,11,12,14,15,16-octahydro-1H-cyclopenta[a]phenanthren-3-one
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7557 mL | 13.7783 mL | 27.5566 mL | |
| 5 mM | 0.5511 mL | 2.7557 mL | 5.5113 mL | |
| 10 mM | 0.2756 mL | 1.3778 mL | 2.7557 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
