[CAS NO. 1414854-42-4]  Verosudil

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PRODUCTS SPECIFICATIONS [1414854-42-4]

Catalog
HY-16758
Brand
MCE
CAS
1414854-42-4

DESCRIPTION [1414854-42-4]

Overview

MDL-
Molecular Weight327.40
Molecular FormulaC17H17N3O2S
SMILESO=C(NC1=CC2=C(C(NC=C2)=O)C=C1)C(N(C)C)C3=CSC=C3

For research use only. We do not sell to patients.

Summary

Verosudil (AR-12286) is a potent, selective Rho-kinase (ROCK) inhibitor with K i s 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] .


IC50 & 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)


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT01302249 Aerie Pharmaceuticals
Glaucoma|Ocular Hypertension
February 2011 Phase 2
NCT01699464 Aerie Pharmaceuticals
Ocular Hypertension|Open-angle Glaucoma
October 2012 Phase 2
NCT01474135 Aerie Pharmaceuticals
Glaucoma|Ocular Hypertension
December 2011 Phase 2

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 16.67 mg/mL ( 50.92 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0544 mL 15.2718 mL 30.5437 mL
5 mM 0.6109 mL 3.0544 mL 6.1087 mL
10 mM 0.3054 mL 1.5272 mL 3.0544 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 1.67 mg/mL (5.10 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.67 mg/mL (5.10 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 1.67 mg/mL (5.10 mM); Clear solution

* All of the co-solvents are available by MCE.