MGV354 

MGV354 is a soluble guanylate cyclase (sGC) activator with EC₅₀s of <0.5 nM, and 5 nM in CHO and GTM-3 E cells, respectively^[1][2].

soluble guanylate cyclase^[1][2]

MGV354 (0.1 nM-10 μM) treatment for 1 hour causes a dose-dependent increase in cGMP levels in normal human trabecular meshwork (NTM) cells (average EC₅₀=2.5±1.6 nM) following treatment with ODQ (20 μM). The average cGMP produced by MGV354 in human NTM cells is 46±28 nM. MGV354 (1 μM) causes a linear increase in intracellular cGMP levels in a time-dependent manner (assay conditions up to 3 hours) in NTM cells^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

MGV354 (Compound (+)-23) robustly lowers intraocular pressure in a cynomolgus model of elevated intraocular pressure over 24 h after a single topical ocular drop^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

575.70

C₃₅H₃₇N₅O₃

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]