Y-33075 is a selective inhibitor of ROCK derived from Y-27632, and is more potent than Y-27632, with an IC50 of 3.6 nM.
| Pack Size | Availability | Price/USD | Quantity |
|---|---|---|---|
| 10 mg | 2-3 weeks | $ 284 | |
| 20 mg | 2-3 weeks | $ 511 | |
| 40 mg | 2-3 weeks | $ 674 | |
| 100 mg | 2-3 weeks | $ 1637 | |
| 200 mg | 2-3 weeks | $ 2570 |
| Description | Y-33075 is a selective inhibitor of ROCK derived from Y-27632, and is more potent than Y-27632, with an IC50 of 3.6 nM. |
| Targets&IC50 | PKC:420 nM, ROCK:3.6 nM, CaMKII:810 nM |
| In vitro | Y-33075 (Y-39983) is a potent inhibitor of ROCK(IC50 of 3.6 nM). Y-33075 also inhibits PKC and CaMKII more potently than Y-27632(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. |
| In vivo | Y-39983 (≥0.01%) significantly lowers intraocular pressure (IOP) at 2 hours after topical administration in rabbits. Y-39983 (0.05%)-treated eyes show significant reduction of IOP between 2 and 7 hours after topical administration in monkeys. Y-39983 (100 μM) increases the regenerating axons of retinal ganglion cells (RGCs) in the eyes of the rats. |
| Synonyms | Y 39983 |
| CAS No. | 199433-58-4 |
| Chemical Formula | C16H16N4O |
| Molecular Weight | 280.331 |
| Solubility | DMSO: 50 mg/mL (178.37 mM), Need ultrasonic and warming |
| Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
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