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Purity: ≥98%
Netarsudil (formerly known as AR-13324; AR13324; trade name Rhopressa) is ROCK inhibitor approved in 2017 for the treatment of glaucoma and ocular hypertension. It inhibits ROCK with Ki of 0.2-10.3 nM. Netarsudil also inhibits norepinephrine transport activity which can reduce the production of aqueous humor. As of 2018, Netarsudil has been approved by FDA for the treatment of glaucoma and ocular hypertension. Previous study showed that at the cellular level, netarsudil was 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. Netarsudil primarily targets cells in the conventional outflow tract, efficiently decreasing IOP in both human and non-human primate eyes. In addition, netarsudil has been shown to increase outflow facility in non-human primate eyes and to decrease episcleral venous pressure in rabbit eyes.
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| References |
Eur J Pharmacol.2016 Sep 15;787:20-31;Invest Ophthalmol Vis Sci.2016 Nov1;57(14):6197-6209.
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| Molecular Formula |
C28H27N3O3
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| Molecular Weight |
453.54
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| CAS # |
1254032-66-0
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| Related CAS # |
1422144-42-0 (mesylate);1254032-66-0;1253952-02-1 (HCl);
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| SMILES |
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
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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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2049 mL | 11.0244 mL | 22.0488 mL | |
| 5 mM | 0.4410 mL | 2.2049 mL | 4.4098 mL | |
| 10 mM | 0.2205 mL | 1.1024 mL | 2.2049 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. |
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Netarsudil mesylate increased outflow facility in perfused mouse eyes ex vivo.Eur J Pharmacol.2016 Sep 15;787:20-31. |
 Enhanced tracer deposition in outflow tissues of living mice subjected to netarsudil mesylate treatment.Eur J Pharmacol.2016 Sep 15;787:20-31. |
 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. |
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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. |
 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. |
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