| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
Omidenepag targets the prostaglandin E2 receptor 2 (EP2), a G-protein-coupled receptor. As a selective and potent EP2 receptor agonist, it activates the EP2 receptor, which is involved in the regulation of intraocular pressure. Activation of EP2 receptors in the eye leads to increased uveoscleral outflow of aqueous humor, thereby reducing intraocular pressure.
|
|---|---|
| ln Vitro |
In vitro, Omidenepag acts as a selective and potent EP2 receptor agonist with an EC50 of 1.1 nM. It demonstrates high selectivity for the EP2 receptor over other prostanoid receptors, making it a promising candidate for the treatment of glaucoma and ocular hypertension. Its in vitro activity is assessed using receptor binding and functional assays in cells expressing the EP2 receptor.
|
| ln Vivo |
In vivo activity of Omidenepag has been demonstrated in animal models of ocular hypertension, where it reduces intraocular pressure. As a topical ocular hypotensive agent, it is administered as eye drops and has been shown to effectively lower intraocular pressure in preclinical studies. Its in vivo efficacy supports its development for the treatment of glaucoma and ocular hypertension.
|
| Enzyme Assay |
The in vitro receptor binding assay for Omidenepag involves measuring its affinity for the EP2 receptor using radioligand binding techniques. These assays use membrane preparations from cells expressing the EP2 receptor and measure the displacement of a labeled ligand by Omidenepag. The compound's potency (EC50) and selectivity are determined by assessing its activity at the EP2 receptor compared to other prostanoid receptors.
|
| Cell Assay |
In vitro cellular assays for Omidenepag are performed using cells expressing the human EP2 receptor. These assays measure the compound's ability to activate the EP2 receptor by assessing downstream signaling pathways, such as cAMP accumulation. The compound's potency (EC50 of 1.1 nM) and efficacy are determined by measuring the concentration-dependent activation of the receptor. These assays confirm its selective and potent agonist activity.
|
| Animal Protocol |
In vivo animal studies for Omidenepag are conducted in normotensive or hypertensive animal models of ocular hypertension. These studies typically involve topical ocular administration of the compound, followed by measurement of intraocular pressure using tonometry. The compound's ability to reduce intraocular pressure and its duration of action are assessed. These studies support its development as a topical ocular hypotensive agent.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Omidenepag are optimized for topical ocular delivery. As the active form of the prodrug Omidenepag Isopropyl, it is designed to achieve high local concentrations in the eye following topical administration. Systemic absorption is minimal, reducing the potential for systemic side effects. The compound's pharmacokinetic profile supports once-daily dosing for the management of glaucoma and ocular hypertension.
|
| Toxicity/Toxicokinetics |
Toxicology studies of Omidenepag have been conducted to support its clinical development for glaucoma and ocular hypertension. These studies include local tolerance assessments following topical ocular administration, as well as systemic toxicity evaluations. The compound is generally well-tolerated in preclinical studies, with minimal systemic toxicity due to its limited absorption. Ocular safety studies are also conducted to evaluate potential effects on the eye.
|
| References | |
| Additional Infomation |
Omidenepag is a prostaglandin E2 receptor agonist. The mechanism of action of omedepag is as a prostaglandin E2 receptor agonist.
See also: Omidenepag isopropyl (active moiety). Omidenepag is a novel selective, non-prostanoid EP2 receptor agonist developed for the treatment of glaucoma and ocular hypertension. It is the active form of the prodrug Omidenepag Isopropyl (OMDI), which is a first-in-class, selective, non-prostaglandin prostanoid EP2 receptor agonist. The compound offers a new mechanism of action for lowering intraocular pressure, providing an alternative to existing prostaglandin analogs. |
| Molecular Formula |
C23H22N6O4S
|
|---|---|
| Molecular Weight |
478.523582935333
|
| Exact Mass |
478.142
|
| CAS # |
1187451-41-7
|
| PubChem CID |
44230575
|
| Appearance |
White to off-white solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
769.4±70.0 °C at 760 mmHg
|
| Flash Point |
419.1±35.7 °C
|
| Vapour Pressure |
0.0±2.8 mmHg at 25°C
|
| Index of Refraction |
1.680
|
| LogP |
1.75
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
9
|
| Rotatable Bond Count |
10
|
| Heavy Atom Count |
34
|
| Complexity |
755
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
YHGSTSNEOJUIRN-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C23H22N6O4S/c30-23(31)15-25-22-6-1-4-19(27-22)17-28(34(32,33)21-5-2-11-24-14-21)16-18-7-9-20(10-8-18)29-13-3-12-26-29/h1-14H,15-17H2,(H,25,27)(H,30,31)
|
| Chemical Name |
(6-((N-(4-(1H-pyrazol-1-yl)benzyl)pyridine-3-sulfonamido)methyl)pyridin-2-yl)glycine
|
| Synonyms |
UR-7276 UR 7276 UR7276
|
| 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) |
DMSO : ~250 mg/mL (~522.44 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.35 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 20.8 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: ≥ 2.08 mg/mL (4.35 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 20.8 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: ≥ 2.08 mg/mL (4.35 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 | 2.0898 mL | 10.4489 mL | 20.8978 mL | |
| 5 mM | 0.4180 mL | 2.0898 mL | 4.1796 mL | |
| 10 mM | 0.2090 mL | 1.0449 mL | 2.0898 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
