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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
Netarsudil mesylate, the mesylate salt form of Netarsudil (formerly known as AR-13324; Rhopressa), is novel ROCK inhibitor with Ki of 0.2-10.3 nM. Additionally, it suppresses norepinephrine transport activity, which may lessen aqueous humor production. The FDA approved Netarsudil in 2018 to treat ocular hypertension and glaucoma.
Targets |
norepinephrine transporter (NET)
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ln Vitro |
Netarsudil has been demonstrated in prior research to be able to cause TM cells' extracellular matrix composition to alter, focal adhesions to disappear, actin stress fiber loss, and cell shape alterations.
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ln Vivo |
Netarsudil effectively lowers intraocular pressure (IOP) in the eyes of both humans and non-human primates by primarily targeting cells in the conventional outflow tract. Furthermore, it has been demonstrated that netarsudil lowers episcleral venous pressure in rabbit eyes and increases outflow facility in non-human primate eyes[2].
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Enzyme Assay |
Netarsudil (formerly known as AR-13324) is an inhibitor of ROCK having a Ki of 0.2-10.3 nM. Moreover, it suppresses norepinephrine transport activity, which may lessen aqueous humor production.
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Cell Assay |
Prior research revealed that netarsudil could cause TM cells' extracellular matrix composition to alter, as well as the loss of focal adhesions, actin stress fibers, and cell shape.
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Animal Protocol |
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References |
Molecular Formula |
C30H35N3O9S2
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Molecular Weight |
645.74
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Exact Mass |
645.18
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Elemental Analysis |
C, 55.80; H, 5.46; N, 6.51; O, 22.30; S, 9.93
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CAS # |
1422144-42-0
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Related CAS # |
Netarsudil hydrochloride;1253952-02-1;AR-13324 analog mesylate
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Appearance |
Solid powder
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SMILES |
CC1=CC(=C(C=C1)C(=O)OCC2=CC=C(C=C2)[C@@H](CN)C(=O)NC3=CC4=C(C=C3)C=NC=C4)C.CS(=O)(=O)O.CS(=O)(=O)O
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InChi Key |
QQDRLKRHJOAQDC-FBHGDYMESA-N
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InChi Code |
InChI=1S/C28H27N3O3.2CH4O3S/c1-18-3-10-25(19(2)13-18)28(33)34-17-20-4-6-21(7-5-20)26(15-29)27(32)31-24-9-8-23-16-30-12-11-22(23)14-24;2*1-5(2,3)4/h3-14,16,26H,15,17,29H2,1-2H3,(H,31,32);2*1H3,(H,2,3,4)/t26-;;/m1../s1
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Chemical Name |
[4-[(2S)-3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl]phenyl]methyl 2,4-dimethylbenzoate;methanesulfonic acid
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.87 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.87 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.5486 mL | 7.7431 mL | 15.4861 mL | |
5 mM | 0.3097 mL | 1.5486 mL | 3.0972 mL | |
10 mM | 0.1549 mL | 0.7743 mL | 1.5486 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Netarsudil lowered intraocular pressure (IOP) in both pigmented and nonpigmented mice. Netarsudil mesylate enhanced IOP recovery in living mouse eyes.Eur J Pharmacol.2016 Sep 15;787:20-31. th> |
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Netarsudil mesylate increased outflow facility in perfused mouse eyes ex vivo.Eur J Pharmacol.2016 Sep 15;787:20-31. td> |
Enhanced tracer deposition in outflow tissues of living mice subjected to netarsudil mesylate treatment.Eur J Pharmacol.2016 Sep 15;787:20-31. td> |
Netarsudil-induced changes in conventional outflow tissue morphology of living mice visualized by optical coherence tomography (OCT).Eur J Pharmacol.2016 Sep 15;787:20-31. th> |
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Netarsudil increased cross-sectional area of Schlemms canal (SC) lumen in living mice with elevated intraocular pressure (IOP) visualized by optical coherence tomography (OCT).Eur J Pharmacol.2016 Sep 15;787:20-31. td> |
Netarsudil-induced changes in flow area and intensity in scleral vessels visualized on OCT speckle variance images.Eur J Pharmacol.2016 Sep 15;787:20-31. td> |