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MedKoo Cat#: 206447 | Name: AR-13503

Description:

WARNING: This product is for research use only, not for human or veterinary use.

AR-13503, is an metabolite of Netarsudil (AR-11324), is a Rho-associated protein kinase inhibitor. Netarsudil is potential useful for treating glaucoma and​/or reducing intraocular pressure.

Chemical Structure

AR-13503
CAS#1254032-16-0

Theoretical Analysis

MedKoo Cat#: 206447

Name: AR-13503

CAS#: 1254032-16-0

Chemical Formula: C19H19N3O2

Exact Mass: 321.1477

Molecular Weight: 321.38

Elemental Analysis: C, 71.01; H, 5.96; N, 13.08; O, 9.96

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
1422144-42-0 (mesylate) 1254032-66-0 (free base) 1253952-02-1 (HCl) 1254032-16-0
Synonym
AR-13503; AR 13503; AR13503; AR-11324 metabolite; AR 11324 metabolite; AR11324 metabolite; Netarsudil metabolite
IUPAC/Chemical Name
Benzeneacetamide, alpha-(aminomethyl)-4-(hydroxymethyl)-N-6-isoquinolinyl-, (S)-
InChi Key
LTXBFJFJUIJOQE-GOSISDBHSA-N
InChi Code
InChI=1S/C19H19N3O2/c20-10-18(14-3-1-13(12-23)2-4-14)19(24)22-17-6-5-16-11-21-8-7-15(16)9-17/h1-9,11,18,23H,10,12,20H2,(H,22,24)/t18-/m1/s1
SMILES Code
O=C(NC1=CC2=C(C=NC=C2)C=C1)[C@H](CN)C3=CC=C(CO)C=C3
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Rho-associated protein kinase (ROCK) is a kinase belonging to the AGC (PKA/ PKG/PKC) family of serine-threonine kinases. It is involved mainly in regulating the shape and movement of cells by acting on the cytoskeleton. ROCK signaling plays an important role in many diseases including diabetes, neurodegenerative diseases such as Parkinson´s disease and amyotrophic lateral sclerosis, pulmonary hypertension and cancer. It has been shown to be involved in causing tissue thickening and stiffening around tumours in a mouse model of skin cancer, principally by increasing the amount of collagen in the tissue around the tumour.

Preparing Stock Solutions

The following data is based on the product molecular weight 321.38 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Lee MH, Kundu JK, Chae JI, Shim JH. Targeting ROCK/LIMK/cofilin signaling pathway in cancer. Arch Pharm Res. 2019 Apr 27. doi: 10.1007/s12272-019-01153-w. [Epub ahead of print] Review. PubMed PMID: 31030376. 2: Roskoski R Jr. Properties of FDA-approved small molecule protein kinase inhibitors. Pharmacol Res. 2019 Mar 13;144:19-50. doi: 10.1016/j.phrs.2019.03.006. [Epub ahead of print] Review. PubMed PMID: 30877063. 3: Khouri AS, Serle JB, Bacharach J, Usner DW, Lewis RA, Braswell P, Kopczynski CC, Heah T; Rocket-4 Study Group. Once-Daily Netarsudil vs Twice-Daily Timolol in Patients with Elevated Intraocular Pressure, the Randomized Phase 3 ROCKET-4 Study. Am J Ophthalmol. 2019 Mar 9. pii: S0002-9394(19)30098-4. doi: 10.1016/j.ajo.2019.03.002. [Epub ahead of print] PubMed PMID: 30862500. 4: Lusthaus J, Goldberg I. Current management of glaucoma. Med J Aust. 2019 Mar;210(4):180-187. doi: 10.5694/mja2.50020. Epub 2019 Feb 14. Review. PubMed PMID: 30767238. 5: Hussar DA. New Drugs 2019, part 1. Nursing. 2019 Feb;49(2):28-36. doi: 10.1097/01.NURSE.0000552697.50502.91. PubMed PMID: 30676555. 6: Kahook MY, Serle JB, Mah FS, Kim T, Raizman MB, Heah T, Ramirez-Davis N, Kopczynski CC, Usner DW, Novack GD; ROCKET-2 Study Group. Long-term Safety and Ocular Hypotensive Efficacy Evaluation of Netarsudil Ophthalmic Solution: Rho Kinase Elevated IOP Treatment Trial (ROCKET-2). Am J Ophthalmol. 2019 Apr;200:130-137. doi: 10.1016/j.ajo.2019.01.003. Epub 2019 Jan 15. PubMed PMID: 30653957. 7: Abbhi V, Piplani P. Rho-kinase (ROCK) Inhibitors- A Neuroprotective Therapeutic Paradigm with a Focus on Ocular Utility. Curr Med Chem. 2018 Oct 30. doi: 10.2174/0929867325666181031102829. [Epub ahead of print] PubMed PMID: 30378487. 8: Dasso L, Al-Khaled T, Sonty S, Aref AA. Profile of netarsudil ophthalmic solution and its potential in the treatment of open-angle glaucoma: evidence to date. Clin Ophthalmol. 2018 Oct 4;12:1939-1944. doi: 10.2147/OPTH.S154001. eCollection 2018. Review. PubMed PMID: 30323550; PubMed Central PMCID: PMC6177382. 9: Fernandez MM. Reticular Epithelial Edema in Edematous Corneas Treated with Netarsudil. Ophthalmology. 2018 Nov;125(11):1709. doi: 10.1016/j.ophtha.2018.08.004. PubMed PMID: 30318038. 10: Kopczynski CC, Heah T. Netarsudil ophthalmic solution 0.02% for the treatment of patients with open-angle glaucoma or ocular hypertension. Drugs Today (Barc). 2018 Aug;54(8):467-478. doi: 10.1358/dot.2018.54.8.2849627. Review. PubMed PMID: 30209441. 11: Two new drugs for glaucoma. Med Lett Drugs Ther. 2018 Jul 16;60(1551):117-120. PubMed PMID: 30036347. 12: Sharif NA. Glaucomatous optic neuropathy treatment options: the promise of novel therapeutics, techniques and tools to help preserve vision. Neural Regen Res. 2018 Jul;13(7):1145-1150. doi: 10.4103/1673-5374.235017. Review. PubMed PMID: 30028313; PubMed Central PMCID: PMC6065230. 13: Tanna AP, Johnson M. Rho Kinase Inhibitors as a Novel Treatment for Glaucoma and Ocular Hypertension. Ophthalmology. 2018 Nov;125(11):1741-1756. doi: 10.1016/j.ophtha.2018.04.040. Epub 2018 Jul 12. Review. PubMed PMID: 30007591; PubMed Central PMCID: PMC6188806. 14: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-. Available from http://www.ncbi.nlm.nih.gov/books/NBK513055/ PubMed PMID: 30000985. 15: Choy M. Pharmaceutical Approval Update. P T. 2018 Apr;43(4):205-227. PubMed PMID: 29622939; PubMed Central PMCID: PMC5871239. 16: Kazemi A, McLaren JW, Kopczynski CC, Heah TG, Novack GD, Sit AJ. The Effects of Netarsudil Ophthalmic Solution on Aqueous Humor Dynamics in a Randomized Study in Humans. J Ocul Pharmacol Ther. 2018 Jun;34(5):380-386. doi: 10.1089/jop.2017.0138. Epub 2018 Feb 22. PubMed PMID: 29469601; PubMed Central PMCID: PMC5995263. 17: Hoy SM. Netarsudil Ophthalmic Solution 0.02%: First Global Approval. Drugs. 2018 Mar;78(3):389-396. doi: 10.1007/s40265-018-0877-7. Review. PubMed PMID: 29453668. 18: Serle JB, Katz LJ, McLaurin E, Heah T, Ramirez-Davis N, Usner DW, Novack GD, Kopczynski CC; ROCKET-1 and ROCKET-2 Study Groups. Two Phase 3 Clinical Trials Comparing the Safety and Efficacy of Netarsudil to Timolol in Patients With Elevated Intraocular Pressure: Rho Kinase Elevated IOP Treatment Trial 1 and 2 (ROCKET-1 and ROCKET-2). Am J Ophthalmol. 2018 Feb;186:116-127. doi: 10.1016/j.ajo.2017.11.019. Epub 2017 Dec 1. PubMed PMID: 29199013. 19: Liebmann JM, Lee JK. Current therapeutic options and treatments in development for the management of primary open-angle glaucoma. Am J Manag Care. 2017 Sep;23(15 Suppl):S279-S292. PubMed PMID: 29164845. 20: Lin CW, Sherman B, Moore LA, Laethem CL, Lu DW, Pattabiraman PP, Rao PV, deLong MA, Kopczynski CC. Discovery and Preclinical Development of Netarsudil, a Novel Ocular Hypotensive Agent for the Treatment of Glaucoma. J Ocul Pharmacol Ther. 2018 Jan/Feb;34(1-2):40-51. doi: 10.1089/jop.2017.0023. Epub 2017 Jun 13. PubMed PMID: 28609185; PubMed Central PMCID: PMC5963640.

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