Y-39983 HCl


Catalog No. size PriceQuantity
M6858-2 2mg solid $127
M6858-10 10mg solid $526

Description

Cas:173897-44-4 (2HCl)

Product Information

Y-39983, also known as Y-33075, is a potent and selective inhibitor of ROCK family with IC50 value of 3.6nM for ROCK. Y-39983 attenuates experimental autoimmune encephalomyelitis via inhibition of demyelination. Y-39983 downregulates RhoA/Rho-associated kinase expression during its promotion of axonal regeneration. Y-39983, promotes regeneration of crushed axons of retinal ganglion cells into the optic nerve of adult cats.

 

Chemical Formula: C16H18Cl2N4O

 

Molecular Weight: 353.247

 

Elemental Analysis: C, 54.40; H, 5.14; Cl, 20.07; N, 15.86; O, 4.53

 

Related CAS #: 173897-44-4 (2HCl)   199433-58-4 (free base)    

 

Synonym:

 

Y-39983 HCl

Y33075

 

Chemical Name: 4-[(1R)-1-aminoethyl]-N-(1H-pyrrolo[2,3-b]pyridin-4-yl)benzamide dihydrochloride

 

InChi Key: 

CKFHAVRPVZNMGT-YQFADDPSSA-N

 

InChi Code: InChI=1S/C16H16N4O.2ClH/c1-10(17)11-2-4-12(5-3-11)16(21)20-14-7-9-19-15-13(14)6-8-18-15;;/h2-10H,17H2,1H3,(H2,18,19,20,21);2*1H/t10-;;/m1../s1

 

Smiles Code:

O=C(NC1=C2C(NC=C2)=NC=C1)C3=CC=C([C@H](N)C)C=C3.[H]Cl.[H]Cl

Technical Data:

 

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

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

 

In Vitro:

Y-33075 (Y-39983) is a potent ROCK inhibitor, with an IC50 of 3.6 nM. Y-33075 also inhibits PKC and CaMKII more potently than Y-27632, and the IC50s of Y-27632 and Y-33075 for PKC are 9.0 μM and 0.42 μM, respectively, whereas the IC50s of Y-27632 and Y-33075 for CaMKII are 26 μM and 0.81 μM, respectively. The IC50s of Y-27632 and Y-33075 for PKC is 82 and 117 times those for ROCK, respectively, whereas the IC50s of Y-27632 and Y-33075 for CaMKII is 236 and 225 times those for ROCK, respectively. Y-33075 (Y-39983, 10 μM) extends neurites in the retinal ganglion cells (RGCs) compared with those in RGCs treated without Y-39983. Y-33075 (Y-39983, 1 μM) inhibits the contraction of rabbit ciliary artery segments evoked by histamine in Ca2+-free solutions. Y-33075 (10 μM) shows no effect on the [Ca2+]i increase with the high-potassium (high-K) solution .

 

In Vivo

In rabbits, Y-39983 (≥0.01%) significantly lowers intraocular pressure (IOP) at 2 hours after topical administration. In monkeys, Y-39983 (0.05%)-treated eyes show significant reduction of IOP between 2 and 7 hours after topical administration. Y-39983 (100 μM) increases the regenerating axons of retinal ganglion cells (RGCs) in the eyes of the rats.

 

 

References

 

  1. Inoue T, Tanihara H, Tokushige H, Araie M. Efficacy and safety of SNJ-1656 in primary open-angle glaucoma or ocular hypertension. Acta Ophthalmol. 2015 Aug;93(5):e393-5. doi: 10.1111/aos.12641. Epub 2015 Mar 17. PubMed PMID: 25783615.

 

  1. Chen KG, Hamilton RS, Robey PG, Mallon BS. Alternative cultures for human pluripotent stem cell production, maintenance, and genetic analysis. J Vis Exp. 2014 Jul 24;(89). doi: 10.3791/51519. PubMed PMID: 25077932; PubMed Central PMCID: PMC4206262.

 

  1. Chen HH, Namil A, Severns B, Ward J, Kelly C, Drace C, McLaughlin MA, Yacoub S, Li B, Patil R, Sharif N, Hellberg MR, Rusinko A, Pang IH, Combrink KD. In vivo optimization of 2,3-diaminopyrazine Rho Kinase inhibitors for the treatment of glaucoma. Bioorg Med Chem Lett. 2014 Apr 15;24(8):1875-9. doi: 10.1016/j.bmcl.2014.03.017. Epub 2014 Mar 19. PubMed PMID: 24684843.

 

  1. Van de Velde S, Van Bergen T, Sijnave D, Hollanders K, Castermans K, Defert O, Leysen D, Vandewalle E, Moons L, Stalmans I. AMA0076, a novel, locally acting Rho kinase inhibitor, potently lowers intraocular pressure in New Zealand white rabbits with minimal hyperemia. Invest Ophthalmol Vis Sci. 2014 Feb 18;55(2):1006-16. doi: 10.1167/iovs.13-13157. PubMed PMID: 24474276.

 

  1. Okumura N, Nakano S, Kay EP, Numata R, Ota A, Sowa Y, Sakai T, Ueno M, Kinoshita S, Koizumi N. Involvement of cyclin D and p27 in cell proliferation mediated by ROCK inhibitors Y-27632 and Y-39983 during corneal endothelium wound healing. Invest Ophthalmol Vis Sci. 2014 Jan 15;55(1):318-29. doi: 10.1167/iovs.13-12225. PubMed PMID: 24106120.

 

Products are for research use only. Not for human use.

 

 

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