| Size | Price | Stock | Qty |
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| 1mg |
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| 50mg | |||
| Other Sizes |
| Targets |
Aganepag targets the prostanoid EP2 receptor, a G protein-coupled receptor that mediates the effects of prostaglandin E2 (PGE2). EP2 receptor activation is involved in various physiological processes, including vasodilation, wound healing, and modulation of inflammation. Aganepag is a potent and selective EP2 receptor agonist with an EC50 of 0.19 nM. It shows no activity at the EP4 receptor, indicating high selectivity. By activating EP2 receptors, Aganepag stimulates the cAMP/PKA signaling pathway. This leads to vasodilation, improved blood flow, and modulation of inflammatory responses.
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| ln Vitro |
Compound 3, aganepag, has an EC50 of 0.19 nM and is inert against EP4, making it a strong prostaglandin EP2 receptor agonist. Research on wound healing, scar prevention, scar reduction, and wrinkle treatment and prevention can all benefit from the usage of aganepag [1].
In vitro, Aganepag is a potent activator of the EP2 receptor, with an EC50 of 0.19 nM. It is highly selective for EP2 over EP4. Its activity is typically measured using cell-based functional assays, such as cAMP accumulation assays in cells expressing the EP2 receptor. Aganepag's ability to stimulate cAMP production in a concentration-dependent manner confirms its agonist activity. Its selectivity is confirmed by testing it against other prostanoid receptors, including EP4, where it shows no activity. |
| ln Vivo |
In vivo, Aganepag is being investigated for its potential in wound healing, scar reduction, scar prevention, and wrinkle treatment and prevention. It is also being studied for its applications in glaucoma and retinal blood flow. By activating EP2 receptors, Aganepag stimulates the cAMP/PKA signaling pathway, leading to vasodilation and improved blood flow. These effects are expected to promote tissue repair and reduce scarring. However, specific in vivo protocols and results, such as efficacy in animal models, are not detailed in the available literature. The compound is a research tool for studying EP2 receptor-mediated effects.
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| Enzyme Assay |
The in vitro assays for Aganepag measure its binding to and activation of the EP2 receptor. Receptor binding assays are performed using membranes from cells expressing the EP2 receptor and a radiolabeled ligand. Aganepag's affinity (Ki) for the receptor can be determined. Functional assays measure the activation of downstream signaling, such as cAMP accumulation. Cells expressing the EP2 receptor are treated with Aganepag, and the levels of cAMP are measured using a competitive immunoassay. The EC50 is determined from the dose-response curve. To assess selectivity, the compound is tested against other prostanoid receptors, including EP4.
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| Cell Assay |
In vitro cell-based assays for Aganepag are conducted using cells expressing the human EP2 receptor. In a typical assay, cells are seeded in multi-well plates and treated with Aganepag at various concentrations. The production of cAMP is measured using a competitive ELISA or a homogeneous time-resolved fluorescence (HTRF) assay. The EC50 is determined from the dose-response curve. For Aganepag, the EC50 is 0.19 nM. These assays confirm that Aganepag is a potent agonist of the EP2 receptor. Its selectivity is confirmed by testing it against other prostanoid receptors, including EP4, where it shows no activity.
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| Animal Protocol |
In vivo animal experiments for Aganepag are not extensively described in the available literature. As a compound being investigated for wound healing and scar reduction, it could be evaluated in animal models of skin injury. In a typical study, wounds would be created on the backs of animals, and Aganepag would be applied topically or administered systemically. Wound healing would be assessed by measuring wound closure rates, scar formation, and histological analysis. For glaucoma applications, it could be evaluated in animal models of elevated intraocular pressure. However, specific protocols for Aganepag are not detailed.
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| ADME/Pharmacokinetics |
Aganepag has a molecular weight of 429.57 g/mol and a molecular formula of C24H31NO4S. It has a purity of >98%. For storage, it is recommended to keep the powder at -20°C for up to 3 years or at -20°C in solution for up to 6 months. It should be stored desiccated and protected from light. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized. As a research compound, its stability is maintained by proper storage as a dry powder.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for Aganepag is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. Aganepag is a selective EP2 receptor agonist, and its toxicity would be related to its effects on EP2 receptor-mediated signaling in normal tissues. However, comprehensive toxicological studies have not been reported. As with all research chemicals, standard laboratory safety precautions should be followed when handling Aganepag. Its use is limited to research applications and it is not intended for human or veterinary use.
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| References | |
| Additional Infomation |
Aganepag (AGN 210937) is a research compound and is not approved for any clinical or therapeutic use. It is a potent and selective agonist of the prostanoid EP2 receptor, with an EC50 of 0.19 nM. It shows no activity at the EP4 receptor. Aganepag is being investigated for applications in wound healing, scar reduction, scar prevention, and wrinkle treatment and prevention. It is also being studied for its potential in glaucoma and retinal blood flow applications. Its mechanism of action involves activating EP2 receptors, which stimulates the cAMP/PKA signaling pathway, leading to vasodilation and modulation of inflammatory responses. It is a valuable tool for studying EP2 receptor biology.
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| Molecular Formula |
C24H31NO4S
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|---|---|
| Molecular Weight |
429.575
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| Exact Mass |
429.197
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| CAS # |
910562-18-4
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| PubChem CID |
24759922
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| Appearance |
White to off-white solid powder
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| LogP |
5.643
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
30
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| Complexity |
563
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| Defined Atom Stereocenter Count |
2
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| SMILES |
CCCCC[C@@H](C1=CC=C(C=C1)N2[C@H](CCC2=O)CCCC3=CC=C(S3)C(=O)O)O
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| InChi Key |
WXWCSPFQIXPFLD-RXVVDRJESA-N
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| InChi Code |
InChI=1S/C24H31NO4S/c1-2-3-4-8-21(26)17-9-11-19(12-10-17)25-18(13-16-23(25)27)6-5-7-20-14-15-22(30-20)24(28)29/h9-12,14-15,18,21,26H,2-8,13,16H2,1H3,(H,28,29)/t18-,21-/m0/s1
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| Chemical Name |
5-[3-[(2S)-1-[4-[(1S)-1-hydroxyhexyl]phenyl]-5-oxopyrrolidin-2-yl]propyl]thiophene-2-carboxylic acid
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| Synonyms |
AGN-210937 AGN210937 AGN 210937
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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) |
DMSO : ≥ 45 mg/mL (~104.76 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.3 mg/mL (5.35 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 23.0 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: ≥ 2.3 mg/mL (5.35 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 23.0 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: ≥ 2.3 mg/mL (5.35 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 | 2.3279 mL | 11.6393 mL | 23.2786 mL | |
| 5 mM | 0.4656 mL | 2.3279 mL | 4.6557 mL | |
| 10 mM | 0.2328 mL | 1.1639 mL | 2.3279 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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