| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| Other Sizes |
| Targets |
33.9 nM (mPRα)[1]
Org OD 02-0 targets the membrane progesterone receptor alpha (mPRα), functioning as a specific agonist. It exhibits an IC₅₀ of 33.9 nM for mPRα. Unlike classical nuclear progesterone receptors, mPRα is a G protein-coupled receptor that mediates rapid, non-genomic effects of progestins. By activating mPRα, Org OD 02-0 activates MAPK activity and inhibits prolactin (PRL) secretion in the pituitary. The compound's selectivity for mPRα makes it a valuable tool for studying mPRα-mediated signaling pathways. |
|---|---|
| ln Vitro |
In vitro, Org OD 02-0 demonstrates potent and selective mPRα agonist activity with an IC₅₀ of 33.9 nM. The compound activates MAPK activity in mPRα-expressing cells. It mimics the protective effects of progestin hormones on serum starvation-induced cell death and apoptosis in both granulosa and breast cancer cells without altering caspase 3 activity. The compound inhibits prolactin (PRL) secretion in the pituitary. These activities are assessed in cell-based assays measuring MAPK phosphorylation, cell viability, apoptosis markers, and prolactin secretion.
|
| ln Vivo |
Specific in vivo activity data for Org OD 02-0 are not extensively documented in the publicly available literature. As a selective mPRα agonist, the compound has potential applications in studying the physiological roles of membrane progesterone receptor signaling. Its effects on prolactin secretion suggest potential applications in reproductive endocrinology research. The compound's protective effects against cell death suggest potential applications in neuroprotection or tissue protection. Further in vivo studies are needed to fully characterize its efficacy and safety.
|
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Org OD 02-0 typically involve competitive binding experiments using mPRα preparations and radiolabeled or fluorescently labeled progestins as tracers. The compound's binding affinity to mPRα is assessed, with an IC₅₀ of 33.9 nM determined through dose-response binding experiments. Assays are conducted in buffered solutions at physiological pH with appropriate receptor preparations. Binding affinity is expressed as IC₅₀ or Kd values. The compound's agonist activity is confirmed through functional assays measuring MAPK activation.
|
| Cell Assay |
In vitro cell-based assays for Org OD 02-0 utilize cell lines expressing mPRα to assess its agonist activity. Cells are treated with varying concentrations of the compound for appropriate time periods. MAPK activation is assessed by measuring phosphorylation levels of ERK1/2 or other MAPK pathway components by Western blot or ELISA. Cell viability and apoptosis are assessed using MTT, Annexin V, or caspase activity assays. Prolactin secretion is measured by ELISA or radioimmunoassay in pituitary cell cultures. Standard cell culture conditions (37°C, 5% CO₂) with appropriate media are employed.
|
| Animal Protocol |
In vivo animal studies with Org OD 02-0 would typically involve administration of the compound to rodent models to evaluate its effects on mPRα-mediated signaling and reproductive function. Potential study designs include models of reproductive function, neuroprotection, or tissue protection. Typical endpoints would include measurements of prolactin levels, assessment of MAPK activation in target tissues, evaluation of cell survival markers, and pharmacokinetic profiling. All procedures must comply with institutional animal care and use guidelines.
|
| ADME/Pharmacokinetics |
Specific pharmacokinetic data for Org OD 02-0 are not extensively documented in the publicly available literature. The compound has a molecular weight of 326.47 g/mol and a molecular formula of C₂₂H₃₀O₂. As a small molecule with favorable physicochemical properties, it may have suitable characteristics for oral bioavailability, though detailed PK parameters have not been published. The compound's chemical name is 10-Ethenyl-19-norprogesterone. Further studies are needed to characterize its absorption, distribution, metabolism, and excretion profile.
|
| Toxicity/Toxicokinetics |
Org OD 02-0 is intended for research use only and is not approved for human therapeutic applications. As a research chemical, comprehensive toxicological data are not available in the publicly accessible literature. Standard safety precautions should be observed when handling this compound, including the use of appropriate personal protective equipment. As with all research chemicals, comprehensive toxicological profiling would be required before any consideration for clinical development.
|
| References |
|
| Additional Infomation |
Org OD 02-0 (10-Ethenyl-19-norprogesterone) (CAS#: 13258-85-0) has a molecular formula of C₂₂H₃₀O₂ and a molecular weight of 326.47 g/mol. It is a selective agonist for membrane progesterone receptor alpha (mPRα) with an IC₅₀ of 33.9 nM. The compound activates MAPK activity and inhibits prolactin (PRL) secretion in the pituitary. It mimics the protective effects of progestin hormones on serum starvation-induced cell death. This compound is not a drug and has not undergone clinical trials.
|
| Molecular Formula |
C22H30O2
|
|---|---|
| Molecular Weight |
326.472
|
| Exact Mass |
326.225
|
| CAS # |
13258-85-0
|
| PubChem CID |
22212907
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.889
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
24
|
| Complexity |
630
|
| Defined Atom Stereocenter Count |
6
|
| SMILES |
O=C1CC[C@@]2([C@H]3CC[C@@]4([C@H](CC[C@H]4[C@@H]3CCC2=C1)C(=O)C)C)C=C
|
| InChi Key |
VFNRBPBEOXXVPX-GCOBIYGJSA-N
|
| InChi Code |
InChI=1S/C22H30O2/c1-4-22-12-9-16(24)13-15(22)5-6-17-19-8-7-18(14(2)23)21(19,3)11-10-20(17)22/h4,13,17-20H,1,5-12H2,2-3H3/t17-,18+,19-,20-,21+,22-/m0/s1
|
| Chemical Name |
(8S,9S,10S,13S,14S,17S)-17-acetyl-10-ethenyl-13-methyl-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[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 | 3.0631 mL | 15.3153 mL | 30.6307 mL | |
| 5 mM | 0.6126 mL | 3.0631 mL | 6.1261 mL | |
| 10 mM | 0.3063 mL | 1.5315 mL | 3.0631 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
