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.
For research use only. We do not sell to patients.
- Formula: C35H37N5O3
- Molecular Weight:575.70
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
In Vitro
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
Molecular Weight 575.70
-
Formula C35H37N5O3
-
SMILES
O=C(C1=C(C)N(C2=NC(C3=CC=CC4=C3[C@@H](NC5=CC=C(C6CCN(C(C7CC7)=O)CC6)C=C5C)CC4)=CC=C2)N=C1)O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)