英文名称 | netarsudil |
---|---|
别名 | AR-11324;AR11324;ester 60;Rhokiinsa,Rhopressa |
英文别名 | AR-11324;AR11324;ester 60;Rhokiinsa,Rhopressa |
EC号 | 817-239-9 |
---|---|
IUPAC Name | [4-[(2S)-3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl]phenyl]methyl 2,4-dimethylbenzoate |
INCHI | InChI=1S/C28H27N3O3/c1-18-3-10-25(19(2)13-18)28(33)34-17-20-4-6-21(7-5-20)26(15-29)27(32)31-24-9-8-23-16-30-12-11-22(23)14-24/h3-14,16,26H,15,17,29H2,1-2H3,(H,31,32)/t26-/m1/s1 |
InChi Key | OURRXQUGYQRVML-AREMUKBSSA-N |
Canonical SMILES | CC1=CC(=C(C=C1)C(=O)OCC2=CC=C(C=C2)C(CN)C(=O)NC3=CC4=C(C=C3)C=NC=C4)C |
关联CAS | 1254032-66-0 |
PubChem CID | 66599893 |
MeSH Entry Terms | AR-13324;netarsudil |
CAS Registry No. | 1254032-66-0 |
---|---|
PubChem CID | 66599893 |
Reactome Reaction | R-HSA-9680443 |
Reactome Drug | R-ALL-9686545 |
DrugCentral Ligand | 5269 |
Ligand ID | 9322 |
---|---|
名称 | netarsudil |
别名 | Rhopressa® |
类别 | Synthetic organic |
学名 | [4-[(2S)-3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl]phenyl]methyl 2,4-dimethylbenzoate |
生物活性评价 |
At 10 μM, AR-13324 inhibits NET by 96% and SERT by 94% |
评价 |
Netarsudil (AR-11324) is a combination Rho-associated protein kinase (Rho or ROCK) and norepinephrine transporter (NET) inhibitor |
1. Sturdivant JM, Royalty SM, Lin CW, Moore LA, Yingling JD, Laethem CL, Sherman B, Heintzelman GR, Kopczynski CC, deLong MA. (2016) Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma.. Bioorg Med Chem Lett, 26 (10): (2475-80). [PMID:27072905] |
2. Ren R, Li G, Le TD, Kopczynski C, Stamer WD, Gong H. (2016) Netarsudil Increases Outflow Facility in Human Eyes Through Multiple Mechanisms.. Invest Ophthalmol Vis Sci, 57 (14): (6197-6209). [PMID:27842161] |
3. Lin CW, Sherman B, Moore LA, Laethem CL, Lu DW, Pattabiraman PP, Rao PV, deLong MA, Kopczynski CC. (2018) Discovery and Preclinical Development of Netarsudil, a Novel Ocular Hypotensive Agent for the Treatment of Glaucoma.. J Ocul Pharmacol Ther, 34 (1-2): (40-51). [PMID:28609185] |
4. Serle JB, Katz LJ, McLaurin E, Heah T, Ramirez-Davis N, Usner DW, Novack GD, Kopczynski CC, ROCKET-1 and ROCKET-2 Study Groups. (2018) Two Phase 3 Clinical Trials Comparing the Safety and Efficacy of Netarsudil to Timolol in Patients With Elevated Intraocular Pressure: Rho Kinase?Elevated IOP Treatment Trial 1 and 2 (ROCKET-1 and ROCKET-2).. Am J Ophthalmol, 186 (13): (116-127). [PMID:29199013] |