Verosudil hydrochloride
Verosudil (AR-12286) hydrochloride is the hydrochloride form of Verosudil (HY-16758). Verosudil hydrochloride is a ROCK inhibitor. Verosudil hydrochloride has equal inhibitory activity against ROCK1 and ROCK2 (Ki: 2 nM). Verosudil hydrochloride is less selective for PKA, PKCT, MRCKA, and CAM2A (Ki: 69 nM, 9322 nM, 28 nM, 5855 nM, respectively). Verosudil hydrochloride increases trabecular outflow capacity to reduce intraocular pressure. Verosudil hydrochloride is useful in the study of glaucoma and ocular hypertension.
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- CAS No.: 1414854-44-6
- Formule: C17H18ClN3O2S
- Masse moléculaire:363.86
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
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ROCK1 2 nM (Ki) |
ROCK2 2 nM (Ki) |
In Vitro
Verosudil (AR-12286) hydrochloride has significant inhibitory activity against both ROCK1 and ROCK2 (Ki: 2 nM)[1].
Verosudil (0.001-100 μM, 6 hours) hydrochloride dose-dependently reduces the length of actin stress fibers in porcine primary trabecular meshwork cells (PTM)[1].
Verosudil (0.001-100 μM, 6 hours) hydrochloride reduces the number of focal adhesions in immortalized human trabecular meshwork (HTM) cells[1].
Verosudil hydrochloride has the ability to disrupt actin stress fibers and focal adhesions in PTM cells and HTM cells (IC50: 924 nM and IC50: 818 nM, respectively)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Verosudil (10 μL, eye drops, twice daily for five weeks) hydrochloride can reverse the changes in intraocular pressure, trabecular meshwork effective filtration area and morphology in a mouse model of ocular hypertension induced by Dexamethasone (HY-14648) [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Dexamethasone-induced ocular hypertension model in C57BL/6 mice (aged 6 weeks) [2]
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Dosage:10 μL
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Administration:eye drops, twice daily for five weeks
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Result:Reduced intraocular pressure in steroid-induce ocular hypertensive (SIOH) mice.
Increased the effective filtration area (EFA) in SIOH mouse eyes.
Reduced extracellular matrix (ECM) in eyes of SIOH mice.
Expanded the dense juxtatubular connective tissue (JCT) in the eyes of SIOH mice.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1414854-44-6
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Masse moléculaire 363.86
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Formule C17H18ClN3O2S
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SMILES
O=C(C(C1=CSC=C1)N(C)C)NC2=CC3=C(C=C2)C(NC=C3)=O.Cl
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Synonyms
AR-12286 hydrochloride
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Lin CW, 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. [Content Brief]
[2]. Ren R, et al. Rho Kinase Inhibitor AR-12286 Reverses Steroid-Induced Changes in Intraocular Pressure, Effective Filtration Areas, and Morphology in Mouse Eyes. Invest Ophthalmol Vis Sci. 2023 Feb 1;64(2):7. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Verosudil hydrochloride Related Classifications
HY-16758A Related Classifications
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