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Besifovir

Names

[ CAS No. ]:
1254032-66-0

[ Name ]:
Besifovir

[Synonym ]:
Benzoic acid, 2,4-dimethyl-, [4-[(1S)-1-(aminomethyl)-2-(6-isoquinolinylamino)-2-oxoethyl]phenyl]methyl ester
netarsudil
4-[(2S)-3-Amino-1-(6-isoquinolinylamino)-1-oxo-2-propanyl]benzyl 2,4-dimethylbenzoate

Biological Activity

[Description]:

Netarsudil (AR-13324) is a potent, selective ROCK inhibitor with Ki of 4.2 nM for ROCK2; 11 kinases are inhibited >90% in a panel of 422 kinases, only ROCK1 and ROCK2 (each 93% inhibition) and PKC (delta, 91%, and eta, 93% inhibition); exhibts improved bioavailability, demonstrates an effective and sustained IOP reduction for 24h after dosing; a novel ocular hypotensive agent for the treatment of glaucoma. Other Indication Approved

[References]

References 1. Sturdivant JM, et al. Bioorg Med Chem Lett. 2016 May 15;26(10):2475-80. 2. Li G, et al. Eur J Pharmacol. 2016 Sep 15;787:20-31. 3. Lin CW, et al. J Ocul Pharmacol Ther. 2017 Jun 13. doi: 10.1089/jop.2017.0023. View Related Products by Target ROCK Other Indication

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
711.9±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C28H27N3O3

[ Molecular Weight ]:
453.532

[ Flash Point ]:
384.3±32.9 °C

[ Exact Mass ]:
453.205231

[ LogP ]:
3.53

[ Vapour Pressure ]:
0.0±2.3 mmHg at 25°C

[ Index of Refraction ]:
1.667

Related Compounds