Verosudil(AR-12286)

Names

[ Name ]:
Verosudil(AR-12286)

[Synonym ]:
verosudil
UNII:MAF34143WM
2-(Dimethylamino)-N-(1-oxo-1,2-dihydro-6-isoquinolinyl)-2-(3-thienyl)acetamide
3-Thiopheneacetamide, N-(1,2-dihydro-1-oxo-6-isoquinolinyl)-α-(dimethylamino)-
UNII: MAF34143WM
AR-12286
MAF34143WM

Biological Activity

[Description]:

Verosudil (AR-12286) is a potent, selective Rho-kinase (ROCK) inhibitor with Kis of 2 and 2 nM for ROCK1 and ROCK2, respectively. AR-12286 lowers intraocular pressure (IOP) primarily by increasing aqueous humour outflow through the trabecular meshwork[1][2].

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> ROCK

Research Areas >> Neurological Disease

Signaling Pathways >> Stem Cell/Wnt >> ROCK

Signaling Pathways >> TGF-beta/Smad >> ROCK

[Target]

ROCK1:2 nM (Ki)

ROCK2:2 nM (Ki)

PKA:69 nM (Ki)

MRCKA:28 nM (Ki)

CAM2A:5855 nM (Ki)

PKC theta:9322 nM (Ki)

[References]

[1]. Lin CW, Sherman B, Moore LA, et al. Discovery and Preclinical Development of Netarsudil, a Novel Ocular Hypotensive Agent for the Treatment of Glaucoma. J Ocul Pharmacol Ther. 2018;34(1-2):40‐51.

[2]. Kopczynski C, Novack GD, Swearingen D, van Haarlem T. Ocular hypotensive efficacy, safety and systemic absorption of AR-12286 ophthalmic solution in normal volunteers. Br J Ophthalmol. 2013;97(5):567‐572.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
625.5±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₇H₁₇N₃O₂S

[ Molecular Weight ]:
327.401

[ Flash Point ]:
332.1±31.5 °C

[ Exact Mass ]:
327.104156

[ LogP ]:
0.84

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.666

Related Compounds

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