Netarsudil (AR-13324) is a Rho-kinase (ROCK) inhibitor with Ki values of 0.2-10.3 nM with potential intraocular pressure (IOP) lowering activity that inhibits both the ROCK and Rho pathways and increases atrial humor (AH) outflow and lowers IOP via the trabecular pathway, and may be used in glaucoma-related studies.
Molecular Weight | 526.45416 |
Formula | C28H29Cl2N3O3 |
CAS Number | 1253952-02-1 |
Solubility (25°C) | DMSO ≥ 60 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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Akt/ROCK-IN-1
Akt/ROCK-IN-1 (B12) is a dual inhibitor for Akt and ROCK, with the IC50s of 0.023 nM and 1.47 nM, respectively. |
Scaff10-8
Scaff10-8, bound to RhoA, inhibits the AKAP-Lbc-mediated RhoA activation. |
ROCK-IN-6
ROCK-IN-6 is a potent and selectiveROCK2 inhibitor with an IC50 of 2.19 nM. |
ROCK-IN-4
ROCK-IN-4 is a potent ROCK inhibitor maintaining NO releasing ability. |
ROCK-IN-32
ROCK-IN-32 is a ROCK inhibitor, with an IC50 value of 11 nM for ROCK2. |
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