Verosudil Free Base | AR-12286 | CAS#1414854-42-4 | CAS#1414854-44-6 | Rho Kinase Inhibitor

Verosudil
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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.

Chemical Structure

Verosudil

CAS# 1414854-42-4 (free base)

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 319562
Name: Verosudil
CAS#: 1414854-42-4 (free base)
Chemical Formula: C17H17N3O2S
Exact Mass: 327.10
Molecular Weight: 327.400
Elemental Analysis: C, 62.37; H, 5.23; N, 12.83; O, 9.77; S, 9.79

Price and Availability

Size	Price	Availability
5mg	USD 90	Ready to ship
10mg	USD 150	Ready to ship
25mg	USD 250	Ready to ship
50mg	USD 450	Ready to ship
100mg	USD 750	Ready to ship
200mg	USD 1350	Ready to ship
500mg	USD 2650	Ready to ship
1g	USD 3750	Ready to ship
2g	USD 6250	Ready to ship
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 1414854-42-4 (free base) 1414854-44-6 (HCl)

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

More Info:

Product Data:

Product Data

Certificate of Analysis:

View CoA: current batch, Lot#Y7X08M22

QC Data:

View QC data: current batch, Lot#Y7X08M22

Safety Data Sheet (SDS):

View Safety Data Sheet (SDS)

Instruction:

View handling instruction

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

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	0.0	0.00

Preparing Stock Solutions

The following data is based on the product molecular weight 327.40 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

Formulation protocol:	TBD
In vitro protocol:	TBD
In vivo protocol:	TBD

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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.

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