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.
For research use only. We do not sell to patients.
- CAS No.: 1414854-44-6
- Formula: C17H18ClN3O2S
- Molecular Weight:363.86
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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ROCK1 2 nM (Ki) |
ROCK2 2 nM (Ki) |
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1414854-44-6
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Molecular Weight 363.86
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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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