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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Fòrmula: C35H37N5O3
- Peso molecular:575.70
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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Peso molecular 575.70
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Fòrmula C35H37N5O3
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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)
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