| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
1a,1b-Dihomo PGE1 targets the Prostaglandin E (EP) receptors, specifically the EP1, EP2, EP3, and EP4 subtypes. As an analog of PGE1, it is predicted to have affinity for these GPCRs. The modification of the side chain length affects its binding affinity and selectivity profile compared to the parent compound. The exact binding affinities (Ki values) have not been reported for this specific analog. The compound is a member of the class of prostaglandin E compounds.
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| ln Vitro |
Specific in vitro activity data for 1a,1b-Dihomo Prostaglandin E1 has not been published. As a structural analog of PGE1, it is expected to exhibit biological activities similar to, but potentially distinct from, the parent compound. PGE1 is known to be a potent vasodilator, inhibit platelet aggregation, and have cytoprotective effects. The dihomo modification is predicted to alter its potency and duration of action by changing its susceptibility to enzymatic degradation.
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| ln Vivo |
Specific in vivo activity data for 1a,1b-Dihomo Prostaglandin E1 is not detailed in standard databases. As a prostaglandin analog, it could be studied in animal models to compare its biological profile to PGE1. For example, PGE1 is clinically used to treat erectile dysfunction and maintain ductus arteriosus patency in neonates. The dihomo analog might exhibit different pharmacokinetic or pharmacodynamic properties, such as altered vascular effects or metabolic stability.
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| Enzyme Assay |
The protocol for assessing the binding of 1a,1b-Dihomo PGE1 to EP receptors would involve a competitive radioligand binding assay using [3H]-PGE2. Membranes from CHO-K1 cells overexpressing each human EP receptor subtype (EP1, EP2, EP3, EP4) are separately incubated with 0.5 nM of the radioligand and increasing concentrations of the unlabeled test compound (0.1 nM to 10 uM) in assay buffer (50 mM HEPES, pH 7.4, 1 mM EDTA, 10 mM MgCl2). After 60 minutes at room temperature, bound and free radioligand are separated by rapid filtration. Filters are washed and counted. Ki values are calculated using the Cheng-Prusoff equation.
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| Cell Assay |
A standard in vitro cell-based assay for evaluating prostaglandin E analogs uses human blood platelets to measure inhibition of platelet aggregation. Platelet-rich plasma (PRP) is prepared from fresh human blood by centrifugation. PRP is pre-incubated with 1a,1b-Dihomo PGE1 (0.1 nM to 10 uM) for 2 minutes at 37degC. Platelet aggregation is induced by the addition of ADP (5-10 uM) or other agonists. Aggregation is measured using a light transmission aggregometer. The extent of inhibition is calculated by comparing the aggregation response to that of a vehicle control. The EC50 for inhibition of aggregation can be determined.
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| Animal Protocol |
An in vivo protocol for assessing the vasodilatory activity of prostaglandins uses the Langendorff isolated perfused rat heart model. Male Sprague-Dawley rats are euthanized, and the heart is rapidly excised and mounted on a Langendorff apparatus. The heart is perfused with Krebs-Henseleit buffer at a constant flow rate (10 mL/min). Left ventricular pressure and coronary perfusion pressure (CPP) are continuously monitored. 1a,1b-Dihomo PGE1 is administered as a bolus injection (0.1-100 ug) into the perfusion line. The change in CPP (a measure of coronary vasodilation) is recorded. The potency (EC50) for coronary vasodilation is calculated and compared to that of PGE1.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for 1a,1b-Dihomo Prostaglandin E1 is not available. Prostaglandins are generally rapidly metabolized in the body, primarily in the lungs and liver, via 15-hydroxyprostaglandin dehydrogenase (15-PGDH) and subsequent beta-oxidation. The dihomo modification might alter the rate of this degradation, potentially leading to a longer half-life compared to PGE1. The compound is likely to have very low oral bioavailability, necessitating parenteral or topical administration for in vivo studies.
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| Toxicity/Toxicokinetics |
Specific toxicity data for this analog is not available. As a prostaglandin E analog, the primary adverse effects are dose-dependent and include vasodilation (resulting in hypotension and flushing), gastrointestinal disturbances (nausea, vomiting, diarrhea), and possible smooth muscle contraction (abdominal cramps). At high concentrations, it may induce pyrexia (fever). Standard toxicology for PGE1 indicates that it has a wide therapeutic window.
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| Additional Infomation |
1a,1b-PGE1 is a prostaglandin.
1a,1b-Dihomo Prostaglandin E1 is a research-grade chemical and is not approved for clinical use. Its molecular formula is C22H38O5 with a molecular weight of 382.53 and a purity of ≥98%. It is supplied as a colorless to light yellow liquid. This compound is a valuable tool for structure-activity relationship (SAR) studies of the prostaglandin E family. By comparing its activity to PGE1 and other analogs, researchers can determine which structural features are critical for receptor binding and biological activity. |
| Molecular Formula |
C22H38O5
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|---|---|
| Molecular Weight |
382.53
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| Exact Mass |
382.271
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| CAS # |
23452-98-4
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| PubChem CID |
5283099
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| Appearance |
Colorless to light yellow liquid
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
550.1±50.0 °C at 760 mmHg
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| Flash Point |
300.6±26.6 °C
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| Vapour Pressure |
0.0±3.4 mmHg at 25°C
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| Index of Refraction |
1.539
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| LogP |
3.31
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
27
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| Complexity |
460
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CCCCC[C@@H](/C=C/[C@H]1[C@@H](CC(=O)[C@@H]1CCCCCCCCC(=O)O)O)O
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| InChi Key |
YMDDELUTDBQEMT-QZCLESEGSA-N
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| InChi Code |
InChI=1S/C22H38O5/c1-2-3-8-11-17(23)14-15-19-18(20(24)16-21(19)25)12-9-6-4-5-7-10-13-22(26)27/h14-15,17-19,21,23,25H,2-13,16H2,1H3,(H,26,27)/b15-14+/t17-,18+,19+,21+/m0/s1
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| Chemical Name |
9-[(1R,2R,3R)-3-hydroxy-2-[(E,3S)-3-hydroxyoct-1-enyl]-5-oxocyclopentyl]nonanoic acid
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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 |
| 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) |
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
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| 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 | 2.6142 mL | 13.0709 mL | 26.1417 mL | |
| 5 mM | 0.5228 mL | 2.6142 mL | 5.2283 mL | |
| 10 mM | 0.2614 mL | 1.3071 mL | 2.6142 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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