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PKC&ROCK

AR-13324 Hydrochloride (1253952-02-1)

AR-13324 hydrochloride is a ROCK, and norepinephrine transporter inhibitor.AR-13324 Hydrochloride (Netarsudil) is a Rho kinase inhibitor with norepinephrine transport inhibitory activity that reduces production of aqueous humor.

Not Intended for Therapeutic Use. For research use only.

CAS: 1253952-02-1 Category

AR-13324 Hydrochloride (1253952-02-1) Description:

AR-13324 Hydrochloride (Netarsudil) is a Rho kinase inhibitor with norepinephrine transport inhibitory activity that reduces production of aqueous humor. AR-13324 is ROCK inhibitor with Ki value of 0.2-10.3 nM. It is currently in clinical trials for the treatment of glaucoma and ocular hypertension.Target: ROCK in vitro: AR-13324 is a small-molecule inhibitor of Rho kinase and a norepinephrine transporter; reduces intraocular pressure (IOP) in normotensive monkey eyes. AR-13324 is a small-molecule inhibitor of Rho kinase and a norepinephrine transporter.in vivo: AR-13324 produces statistically significant lowering of episcleral venous pressure (EVP) in Dutch Belted (DB) rabbits.

AR-13324 Hydrochloride (1253952-02-1) Specifications:

Product Name AR-13324 hydrochloride
Synonym AR-13324 HCL; Netarsudil; Netarsudil hydrochloride; AR-13324 (HCL); AR-13324-HCL; AR 13324 HCL; AR13324 HCL
Chemical Name [4-[(2S)-3-Amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl]phenyl]methyl 2,4-dimethylbenzoate dihydrochloride
Drug Class Inhibitor
Purity ≥98% (HPLC)
CAS Number 1253952-02-1
Molecular Formula C28H29Cl2N3O3
Molecular Weight 526.45
Monoisotopic Mass 525.1586 g/mol
MDL number N/A
InChIKey LDKTYVXXYUJVJM-FBHGDYMESA-N
InChi Code InChI=1S/C28H27N3O3.2ClH/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;;/h3-14,16,26H,15,17,29H2,1-2H3,(H,31,32);2*1H/t26-;;/m1../s1
SMILES 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.[H]Cl.[H]Cl
Form Powder
Color iris color
Solubility  Soluble in DMSO
Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application A ROCK and norepinephrine transporter inhibitor

 


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RIDADR NONH for all modes of transport

References:

[1]. Shaw PX, Sang A, Wang Y, Ho D, Douglas C, Dia L, Goldberg JL. Topical administration of a Rock/Net inhibitor promotes retinal ganglion cell survival and axon regeneration after optic nerve injury. Exp Eye Res. 2017 May;158:33-42. doi: 10.1016/j.exer.2016.07.006. Epub 2016 Jul 18. PubMed PMID: 27443501.

[2]. Sturdivant JM, Royalty SM, Lin CW, Moore LA, Yingling JD, Laethem CL, Sherman B, Heintzelman GR, Kopczynski CC, deLong MA. Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma. Bioorg Med Chem Lett. 2016 May 15;26(10):2475-80. doi: 10.1016/j.bmcl.2016.03.104. Epub 2016 Apr 1. PubMed PMID: 27072905.

[3]. Kiel JW, Kopczynski CC. Effect of AR-13324 on episcleral venous pressure in Dutch belted rabbits. J Ocul Pharmacol Ther. 2015 Apr;31(3):146-51. doi: 10.1089/jop.2014.0146. Epub 2015 Mar 10. PubMed PMID: 25756366; PubMed Central PMCID: PMC4397991.

[4]. Levy B, Ramirez N, Novack GD, Kopczynski C. Ocular hypotensive safety and systemic absorption of AR-13324 ophthalmic solution in normal volunteers. Am J Ophthalmol. 2015 May;159(5):980-5.e1. doi: 10.1016/j.ajo.2015.01.026. Epub 2015 Jan 28. PubMed PMID: 25637177.

[5]. Wang RF, Williamson JE, Kopczynski C, Serle JB. Effect of 0.04% AR-13324, a ROCK, and norepinephrine transporter inhibitor, on aqueous humor dynamics in normotensive monkey eyes. J Glaucoma. 2015 Jan;24(1):51-4. doi: 10.1097/IJG.0b013e3182952213. PubMed PMID: 25535688.

1 review for AR-13324 Hydrochloride (1253952-02-1)

  1. Cofttek

    Never had such good experience before,The AR-13324 Hydrochloride (1253952-02-1) is high purity,also customer service is pretty nice !gotta try!!

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