WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 319562
CAS#: 1414854-42-4 (free base)
Description: Verosudil, also known as AR-12286, is a potent and selective Rho kinase inhibitor. AR-12286 was well tolerated and provided statistically significant reduction in IOP (intraocular pressure) in patients with XFS (exfoliation syndrome) and OHT (ocular hypertension) or XFG (exfoliative glaucoma). This drug may represent an additional therapeutic paradigm for the treatment of XFG.
MedKoo Cat#: 319562
CAS#: 1414854-42-4 (free base)
Chemical Formula: C17H17N3O2S
Exact Mass: 327.1041
Molecular Weight: 327.4
Elemental Analysis: C, 62.37; H, 5.23; N, 12.83; O, 9.77; S, 9.79
Synonym: AR-12286; AR12286; AR 12286; Verosudil; Verosudil free base.
IUPAC/Chemical Name: 2-(dimethylamino)-N-(1-oxo- 1,2-dihydroisoquinolin-6-yl)-2-(thiophen-3-yl)acetamide
InChi Key: VDYRZXYYQMMFJW-UHFFFAOYSA-N
InChi Code: InChI=1S/C17H17N3O2S/c1-20(2)15(12-6-8-23-10-12)17(22)19-13-3-4-14-11(9-13)5-7-18-16(14)21/h3-10,15H,1-2H3,(H,18,21)(H,19,22)
SMILES Code: O=C(NC1=CC2=C(C(NC=C2)=O)C=C1)C(N(C)C)C3=CSC=C3
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
|Biological target:||Verosudil (AR-12286) is a potent, selective Rho-kinase (ROCK) inhibitor with Kis of 2 and 2 nM for ROCK1 and ROCK2, respectively.|
|In vitro activity:||TBD|
|In vivo activity:||TBD|
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 327.4 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
|In vitro protocol:||TBD|
|In vivo protocol:||TBD|
1: Skaat A, Jasien JV, Ritch R. Efficacy of Topically Administered Rho-Kinase Inhibitor AR-12286 in Patients With Exfoliation Syndrome and Ocular Hypertension or Glaucoma. J Glaucoma. 2016 Sep;25(9):e807-14. doi: 10.1097/IJG.0000000000000508. PMID: 27552517.
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 May;97(5):567-72. doi: 10.1136/bjophthalmol-2012-302466. Epub 2013 Feb 22. PMID: 23435190.
3: Williams RD, Novack GD, van Haarlem T, Kopczynski C; AR-12286 Phase 2A Study Group. Ocular hypotensive effect of the Rho kinase inhibitor AR-12286 in patients with glaucoma and ocular hypertension. Am J Ophthalmol. 2011 Nov;152(5):834-41.e1. doi: 10.1016/j.ajo.2011.04.012. Epub 2011 Jul 27. PMID: 21794845.
4: Hookes L. Association for Research in Vision and Ophthalmology (ARVO)--2010 Annual Meeting. For Sight: The Future of Eye and Vision Research--part 2. IDrugs. 2010 Jul;13(7):430-2. PMID: 20582863.