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Omidenepag isopropyl

SKU: orb1706876

Description

Omidenepag isopropyl (DE-117) is a selective EP2 receptor agonist developed for lowering intraocular pressure. It is utilized in glaucoma research, with studies demonstrating its efficacy in both in vitro receptor binding assays and in vivo models of ocular hypertension.

Research Area

Immunology & Inflammation, Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number1187451-19-9
MW520.6
Purity99.86%
FormulaC26H28N6O4S
SMILESO=C(OC(C)C)CNC=1N=C(C=CC1)CN(CC2=CC=C(C=C2)N3N=CC=C3)S(=O)(=O)C=4C=NC=CC4
TargetProstaglandin Receptor
SolubilityDMSO:40 mg/mL (76.83 mM)

Bioactivity

In Vivo
METHODS: The effects of Omidenepag isopropyl on intraocular pressure and aqueous humor dynamics were evaluated in cynomolgus monkeys with unilateral laser-induced intraocular hypertension. In a crossover fashion, the hypertensive eye of each monkey was dosed once daily with 20 μL of 0.002% Omidenepag isopropyl or vehicle. On day 7 of dosing, IOP was measured by pneumometry, aqueous humor flow and outflow facilities were assessed by fluorophotometry, and uveoscleral outflow was calculated mathematically. Treatments were compared by paired t test. RESULTS: Omidenepag isopropyl significantly reduced intraocular pressure by 27%, 35% and 44% at 0.5, 1.5 and 4 hours after the last administration; Omidenepag isopropyl treatment group and uveoscleral outflow significantly increased by 71% and 176% respectively. (P<0.05).
In Vitro
METHODS: All binding studies were performed on prostaglandin receptors DP1, EP1-4, FP, and IP at OMDI (0.1, 0.3, 1, 3, and 10 μM) in all assays, calculated using the Cheng-Prusoff equation. RESULTS: OMDI binds weakly to the EP1 receptor with Ki = 1700 nM, to the EP2 receptor with Ki > 4600 nM, and to the FP receptor with Ki > 4500 nM.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Omidenepag isopropyl, EP1, EP2, DE 117, DE117, DE-117, Prostaglandin Receptor, ProstaglandinReceptor
Quality Guarantee

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Key Properties

No computed properties available.

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Omidenepag isopropyl (orb1706876)

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Available Sizes

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1 mg
¥ 1,300.00
5 mg
¥ 2,210.00
10 mg
¥ 3,120.00
25 mg
¥ 6,500.00
50 mg
¥ 10,790.00
100 mg
¥ 17,160.00
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