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.
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- 分子式: C35H37N5O3
- 分子量:575.70
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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 |
化学情報
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分子量 575.70
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)