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MGV354

Catalog No. T12888   CAS T12888

MGV354 is a soluble activator of guanylate cyclase(sGC) with EC 50 s of <0.5 nM, and 5 nM in CHO and GTM-3 E cells, respectively [1] [2].

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MGV354 Chemical Structure
MGV354, CAS T12888
Pack Size Availability Price/USD Quantity
25 mg 10-14 weeks $ 1,715.00
50 mg 10-14 weeks $ 2,885.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description MGV354 is a soluble activator of guanylate cyclase(sGC) with EC 50 s of <0.5 nM, and 5 nM in CHO and GTM-3 E cells, respectively [1] [2].
In vitro Treatment with MGV354, ranging from 0.1 nM to 10 μM, for one hour induces a dose-dependent elevation in cGMP levels within normal human trabecular meshwork (NTM) cells, showcasing an average effective concentration (EC50) of 2.5±1.6 nM after ODQ (20 μM) administration. The resultant average cGMP concentration achieved by MGV354 in NTM cells is 46±28 nM. Moreover, at a concentration of 1 μM, MGV354 consistently augments intracellular cGMP levels in NTM cells in a linear, time-dependent fashion, under assay conditions extending up to three hours [3].
In vivo MGV354 (Compound (+)-23) robustly lowers intraocular pressure in a cynomolgus model of elevated intraocular pressure over 24 h after a single topical ocular drop and has been selected for clinical evaluation [1].
Molecular Weight 575.7
Formula C35H37N5O3
CAS No. T12888

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Ehara T, et al. The Discovery of ( S)-1-(6-(3-((4-(1-(Cyclopropanecarbonyl)piperidin-4-yl)-2-methylphenyl)amino)-2,3-dihydro-1 H-inden-4-yl)pyridin-2-yl)-5-methyl-1 H-pyrazole-4-carboxylic Acid, a Soluble Guanylate Cyclase Activator Specifically Designed for Topical Ocular Delivery as a Therapy for Glaucoma. J Med Chem. 2018 Mar 22;61(6):2552-2570. 2. Stacy R, et al. A Randomized, Controlled Phase I/II Study to Evaluate the Safety and Efficacy of MGV354 for Ocular Hypertension or Glaucoma.Am J Ophthalmol. 2018 Aug;192:113-123. 3. Prasanna G, et al. A Novel Selective Soluble Guanylate Cyclase Activator, MGV354, Lowers Intraocular Pressure in Preclinical Models, Following Topical Ocular Dosing.Invest Ophthalmol Vis Sci. 2018 Apr 1;59(5):1704-1716.

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Keywords

MGV354 T12888 Others MGV 354 MGV-354 inhibitor inhibit

 

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