| CAS NO: | 1253952-02-1 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 526.45 |
|---|---|
| Formula | C28H27N3O3.2HCl |
| CAS No. | 1253952-02-1 (DiHCl); |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 20 mg/mL (38 mM) |
| Water: 54 mg/mL (102.6 mM) | |
| Ethanol: 2 mg/mL (3.8 mM) | |
| SMILES Code | O=C(OCC1=CC=C([C@@H](CN)C(NC2=CC3=C(C=NC=C3)C=C2)=O)C=C1)C4=CC=C(C)C=C4C.[H]Cl.[H]Cl |
| Synonyms | AR13324 HCl; Rhopressa; AR-13324 HCl; AR 13324; AR 13324 HCl; Netarsudil; AR-13324; Netarsudil hydrochloride Chemical Name: [4-[(2S)-3-Amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl]phenyl]methyl 2,4-dimethylbenzoate dihydrochloride Exact Mass: 525.1586 |
| In Vitro | In vitro activity: 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 Kinase Assay: Netarsudil (formerly known as AR-13324) is ROCK inhibitor with Ki of 0.2-10.3 nM. It also inhibits norepinephrine transport activity which can reduce the production of aqueous humor. Cell Assay: 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. |
|---|---|
| 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. |
| Animal model | Mice with elevated intraocular pressure (IOP) |
| Formulation & Dosage | Topical application |
| References | Eur J Pharmacol. 2016 Sep 15;787:20-31; Invest Ophthalmol Vis Sci. 2016 Nov 1;57(14):6197-6209. |
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