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AR-13324 mesylate (1422144-42-0)

AR-13324 is a small-molecule inhibitor of Rho kinase and a norepinephrine transporter; reduces intraocular pressure (IOP) in normotensive monkey eyes..

Not Intended for Therapeutic Use. For research use only.

CAS: 1422144-42-0 Category

AR-13324 mesylate (1422144-42-0) Description:

AR-11324, also known as Netarsudil, is a Rho-associated protein kinase inhibitor. Netarsudil is potential useful for treating glaucoma and​/or reducing intraocular pressure. Netarsudil Increases Outflow Facility in Human Eyes Through Multiple Mechanisms. Netarsudil inhibited kinases ROCK1 and ROCK2 with a Ki of 1 nM each, disrupted actin stress fibers and focal adhesions in TM cells with IC50s of 79 and 16 nM, respectively, and blocked the profibrotic effects of TGF-β2 in HTM cells. Netarsudil produced large reductions in IOP in rabbits and monkeys that were sustained for at least 24 h after once daily dosing, with transient, mild hyperemia observed as the only adverse effect.

AR-13324 mesylate (1422144-42-0) Specifications:

Product Name AR-13324 mesylate
Synonym AR-13324; AR13324; AR 13324; Netarsudil Mesylate
Chemical Name (S)-4-(3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl)benzyl 2,4-dimethylbenzoate dimethanesulfonate
Drug Class Inhibitor
Purity ≥98% (HPLC)
CAS Number 1422144-42-0
Molecular Formula C30H35N3O9S2
Molecular Weight 645.18147
Monoisotopic Mass 645.742 g/mol
MDL number N/A
InChIKey QQDRLKRHJOAQDC-FBHGDYMESA-N
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
SMILES CS(=O)(O)=O.CS(=O)(O)=O.O=C(OCC1=CC=C([[email protected]@H](CN)C(NC2=CC3=C(C=NC=C3)C=C2)=O)C=C1)C4=CC=C(C)C=C4C
Form Powder
Color iris color
Solubility  Soluble in DMSO, not in water
Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application A Rho-associated protein kinase inhibitor

 


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RIDADR NONH for all modes of transport

References:

[1]. Discovery and Preclinical Development of Netarsudil, a Novel Ocular Hypotensive Agent for the Treatment of Glaucoma. Lin CW, Sherman B, Moore LA, Laethem CL, Lu DW, Pattabiraman PP, Rao PV, deLong MA, Kopczynski CC. J Ocul Pharmacol Ther. 2018 Jan/Feb;34(1-2):40-51. doi: 10.1089/jop.2017.0023. Epub 2017 Jun 13. PMID: 28609185

[2]. Netarsudil Increases Outflow Facility in Human Eyes Through Multiple Mechanisms. Ren R, Li G, Le TD, Kopczynski C, Stamer WD, Gong H. Invest Ophthalmol Vis Sci. 2016 Nov 1;57(14):6197-6209. doi: 10.1167/iovs.16-20189. PMID: 27842161

[3].  Visualization of conventional outflow tissue responses to netarsudil in living mouse eyes. Li G, Mukherjee D, Navarro I, Ashpole NE, Sherwood JM, Chang J, Overby DR, Yuan F, Gonzalez P, Kopczynski CC, Farsiu S, Stamer WD. Eur J Pharmacol. 2016 Sep 15;787:20-31. doi: 10.1016/j.ejphar.2016.04.002. Epub 2016 Apr 13. PMID: 27085895

[4]. Study in Humans. Kazemi A, McLaren JW, Kopczynski CC, Heah TG, Novack GD, Sit AJ. J Ocul Pharmacol Ther. 2018 Jun;34(5):380-386. doi: 10.1089/jop.2017.0138. Epub 2018 Feb 22. PMID: 29469601

[5]. Netarsudil ophthalmic solution 0.02% for the treatment of patients with open-angle glaucoma or ocular hypertension. Kopczynski CC, Heah T. Drugs Today (Barc). 2018 Aug;54(8):467-478. doi: 10.1358/dot.2018.54.8.2849627. Review.PMID: 30209441

1 review for AR-13324 mesylate (1422144-42-0)

  1. Rated 5 out of 5

    Cofttek

    Never had such good experience before,The AR-13324 mesylate (1422144-42-0) is high purity,also customer service is pretty nice !gotta try!!

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