Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C16H16N4O |
| Molecular Weight | 280.3244 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@@H](N)C1=CC=C(C=C1)C(=O)NC2=C3C=CNC3=NC=C2
InChI
InChIKey=JTVBXQAYBIJXRP-SNVBAGLBSA-N
InChI=1S/C16H16N4O/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)/t10-/m1/s1
| Molecular Formula | C16H16N4O |
| Molecular Weight | 280.3244 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionSources: http://adisinsight.springer.com/drugs/800023536https://www.ncbi.nlm.nih.gov/pubmed/23258382Curator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/20434334 | https://www.ncbi.nlm.nih.gov/pubmed/24684843 | https://www.ncbi.nlm.nih.gov/pubmed/24008512 |
https://www.ncbi.nlm.nih.gov/pubmed/21667088
Sources: http://adisinsight.springer.com/drugs/800023536https://www.ncbi.nlm.nih.gov/pubmed/23258382
Curator's Comment: The description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/20434334 | https://www.ncbi.nlm.nih.gov/pubmed/24684843 | https://www.ncbi.nlm.nih.gov/pubmed/24008512 |
https://www.ncbi.nlm.nih.gov/pubmed/21667088
Y-33075 is potent and selective ROCK (Rho-associated coiled-coil-forming protein kinase) inhibitor, developed by Yoshitomi Pharmaceutical Industries for encephalomyelitis treatment. In rabbits and in monkeys, Y-33075 lowers IOP in a dose-dependent fashion. An increase in regenerating axons of RGCs in 100 mM Y-33075-treated eyes is observed compared with saline-treated eyes. Y-33075 dose-dependently increases the number of RGCs with regenerating axons. Both Y-33075 induces a concentration-dependent relaxation in rabbit ciliary arteries precontracted with a high-potassium (high-K) solution. The amplitude of relaxation induced by Y-33075 is not affected by either 100 μM N (G)-nitro-L: -arginine methyl ester (L: -NAME) or 10 μM indomethacin. In Ca2 -free solution, Y-27632 and Y-39983 significantly inhibit the transient contraction of ciliary arteries induced by 10 μM histamine. However, neither Y-27632 nor Y-39983 affects the elevation of [Ca2 ](i) induced by high-K solution and histamine.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL3231 |
30.0 nM [IC50] | ||
Target ID: CHEMBL2973 |
58.0 nM [IC50] | ||
Target ID: CHEMBL2111459 |
3.6 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
|||
| Primary | Unknown Approved UseUnknown |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Efficacy and safety of SNJ-1656 in primary open-angle glaucoma or ocular hypertension. | 2015-08 |
|
| In vivo optimization of 2,3-diaminopyrazine Rho Kinase inhibitors for the treatment of glaucoma. | 2014-04-15 |
|
| Involvement of cyclin D and p27 in cell proliferation mediated by ROCK inhibitors Y-27632 and Y-39983 during corneal endothelium wound healing. | 2014-01-15 |
|
| Y-39983 downregulates RhoA/Rho-associated kinase expression during its promotion of axonal regeneration. | 2013-03 |
|
| Y-39983, a selective Rho-kinase inhibitor, attenuates experimental autoimmune encephalomyelitis via inhibition of demyelination. | 2013 |
|
| Effects of Y-39983, a selective Rho-associated protein kinase inhibitor, on blood flow in optic nerve head in rabbits and axonal regeneration of retinal ganglion cells in rats. | 2011-10 |
|
| Effects of Rho-associated protein kinase inhibitors Y-27632 and Y-39983 on isolated rabbit ciliary arteries. | 2011-07 |
|
| Rho-Rho kinase pathway in the actomyosin contraction and cell-matrix adhesion in immortalized human trabecular meshwork cells. | 2011 |
|
| Decreased intraocular pressure in mice following either pharmacological or genetic inhibition of ROCK. | 2009-06 |
|
| Effects of topical administration of y-39983, a selective rho-associated protein kinase inhibitor, on ocular tissues in rabbits and monkeys. | 2007-07 |
|
| A novel ROCK inhibitor, Y-39983, promotes regeneration of crushed axons of retinal ganglion cells into the optic nerve of adult cats. | 2007-05 |
|
| Contribution of ROCK in contraction of trabecular meshwork: proposed mechanism for regulating aqueous outflow in monkey and human eyes. | 2005-04 |
Sample Use Guides
Senju Pharmaceuticals completed a phase II trial that evaluated the dose-response relationship of ocular hypotensive efficacy and safety of Y 39983 at concentrations ranging from 0.003%, 0.01%, 0.03% or Y 39983 vehicle control given twice a day for 4 weeks in patients with primary open angle glaucoma or ocular hypertension (UMIN000018866)
Route of Administration:
Topical
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:22:47 GMT 2025
by
admin
on
Mon Mar 31 18:22:47 GMT 2025
|
| Record UNII |
00ALI1GAY2
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Common Name | English | ||
|
Preferred Name | English | ||
|
Systematic Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
199433-58-4
Created by
admin on Mon Mar 31 18:22:47 GMT 2025 , Edited by admin on Mon Mar 31 18:22:47 GMT 2025
|
PRIMARY | |||
|
00ALI1GAY2
Created by
admin on Mon Mar 31 18:22:47 GMT 2025 , Edited by admin on Mon Mar 31 18:22:47 GMT 2025
|
PRIMARY | |||
|
DTXSID50173718
Created by
admin on Mon Mar 31 18:22:47 GMT 2025 , Edited by admin on Mon Mar 31 18:22:47 GMT 2025
|
PRIMARY | |||
|
9810884
Created by
admin on Mon Mar 31 18:22:47 GMT 2025 , Edited by admin on Mon Mar 31 18:22:47 GMT 2025
|
PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
|
SALT/SOLVATE -> PARENT | |||
|
TARGET -> INHIBITOR |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
|
ACTIVE MOIETY |
