Netarsudil (AR-13324)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Ki: 0.2-10.3 nM
Netarsudil (AR-13324) is a ROCK inhibitor.
The Rho kinases are serine/threonine protein kinases existing as 2 isoforms, ROCK1 and ROCK2, which are widely expressed in various tissues, such as the trabecular meshwork. ROCK can promote the assembly of actin stress fibers and focal adhesions and can also regulate cell contraction and motility.
In vitro: Previous study showed that at the cellular level, netarsudil had been shown to be able to induce loss of actin stress fibers, cell shape changes, loss of focal adhesions, as well as changes in extracellular matrix composition of TM cells [1].
In vivo: Animal efficacy study found that the topical treatment of netarsudil was able to affect both proximal (trabecular meshwork and Schlemm's Canal) and distal portions (intrascleral vessels) of the mouse conventional outflow tract [2].
Clinical trial: Previous two phase II clinical trials showed that netarsudil 0.02% treatment was shown to produce significant DIOPs that ranged from 5.7 to 6.3 mmHg after four weeks of dosing in patients with glaucoma and ocular hypertension. In addition, it was found that netarsudil was well tolerated, with trace to mild hyperemia being the most frequently reported adverse event. Currently, netarsudil is in phase III clinical trials for the treatment of ocular hypertension and open-angle glaucoma [1].
References:
[1] Sturdivant JM et al. Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma. Bioorg Med Chem Lett. 2016 May 15;26(10):2475-80.
[2] Li G et al. Visualization of conventional outflow tissue responses to netarsudil in living mouse eyes. Eur J Pharmacol. 2016 Sep 15;787:20-31.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 526.45 |
| Cas No. | 1253952-02-1 |
| Formula | C28H29Cl2N3O3 |
| Solubility | ≥26.3 mg/mL in H2O with gentle warming and ultrasonic; insoluble in EtOH; ≥7.783 mg/mL in DMSO |
| Chemical Name | (R)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate dihydrochloride |
| SDF | Download SDF |
| Canonical SMILES | [H]Cl.[H]Cl.O=C(OCC1=CC=C([[email protected]](CN)C(NC2=CC3=C(C=NC=C3)C=C2)=O)C=C1)C4=CC=C(C)C=C4C |
| Shipping Condition | Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request. |
| General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months. |
Quality Control & MSDS
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Chemical structure
