SR3677 is an isoform-selective inhibitor of ROCK2 kinase activity.
CAS Number: 1072959-67-1
Molecular Weight: 408.45
Chemical Name: N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxine-3-carboxamide
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
SR3677 has an IC50 of ~3 nM in enzyme and cell based assays and has an off-target hit rate of 1.4% against 353 kinases, and inhibits only 3 out of 70 nonkinase enzymes and receptors. The IC50 value of SR3677 for ROCK-I is 56±12 nM. The hydrophobic interaction of the benzodioxane phenyl ring with the hydrophobic surface of the pocket is the dominating factor that contributes to the high potency of SR3677.
ExVivo: Pharmacology studies shows that SR3677 is efficacious in both, increasing ex vivo aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation. Continuous exposure of 25 µM SR3677 increases the outflow facility by 60% at 1 h perfusion, increasing to 70–80% for the 2–5 h time points.
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