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Omidenepag Isopropyl

Cat. No. M21646
Omidenepag Isopropyl Structure
Synonym:

OMDI

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Biological Activity

Omidenepag isopropyl is a selective EP2 receptor agonist. Omidenepag isopropyl is converted to the active product Omidenepag during corneal penetration, and Omidenepag is a highly selective EP2 receptor agonist. In ocular hypertensive monkeys finds that Omidenepag isopropyl lowers IOP by increasing both trabecular outflow facility and uveoscleral outflow. Omidenepag isopropyl at 0.0001%, 0.001%, or 0.01%, Xalatan, or vehicle was topically administered to one eye in ocular normotensive monkeys. Omidenepag isopropyl shows significant and dose-dependent IOP-lowering effects at doses of 0.0001%, 0.001%, and 0.01% in ocular normotensive monkeys, with mean maximal IOP reductions of 2.4 ± 0.6, 7.6 ± 1.7, and 13.3 ± 1.2 mm Hg at each tested concentration, respectively.

Chemical Information
Molecular Weight 520.6
Formula C26H28N6O4S
CAS Number 1187451-19-9
Solubility (25°C) DMSO 45 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] No authors listed. Am J Health Syst Pharm. Omidenepag Isopropyl

[2] Masato Matsuo, et al. Clin Ophthalmol. Efficacy and Patient Tolerability of Omidenepag Isopropyl in the Treatment of Glaucoma and Ocular Hypertension

[3] Makoto Aihara, et al. Am J Ophthalmol. Omidenepag Isopropyl Versus Latanoprost in Primary Open-Angle Glaucoma and Ocular Hypertension: The Phase 3 AYAME Study

[4] L Ferro Desideri, et al. Drugs Today (Barc). Omidenepag isopropyl for the treatment of glaucoma and ocular hypertension

[5] Sean Duggan. Drugs. Omidenepag Isopropyl Ophthalmic Solution 0.002%: First Global Approval

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Keywords: Omidenepag Isopropyl, OMDI supplier, Prostaglandin Receptor, inhibitors, activators


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