SR3677 is an isoform-selective inhibitor of ROCK2 kinase activity.
Chemical Formula: C22H24N4O4
Exact Mass: 408.1798
Molecular Weight: 408.45
Elemental Analysis: C, 64.69; H, 5.92; N, 13.72; O, 15.67
Chemical Name: N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxine-3-carboxamide
InChi Code: InChI=1S/C22H24N4O4/c1-26(2)9-10-28-20-11-15(16-12-23-24-13-16)7-8-17(20)25-22(27)21-14-29-18-5-3-4-6-19(18)30-21/h3-8,11-13,21H,9-10,14H2,1-2H3,(H,23,24)(H,25,27)
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: >3 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: 2934.99.03.00
SR-3677 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 SR-3677 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 SR-3677.
ExVivo: Pharmacology studies shows that SR-3677 is efficacious in both, increasing ex vivo aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation. Continuous exposure of 25 µM SR-3677 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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- Kasahara DI, Mathews JA, Park CY, Cho Y, Hunt G, Wurmbrand AP, Liao JK, Shore SA. ROCK insufficiency attenuates ozone-induced airway hyperresponsiveness in mice. Am J Physiol Lung Cell Mol Physiol. 2015 Oct 1;309(7):L736-46. doi: 10.1152/ajplung.00372.2014. Epub 2015 Aug 14. PubMed PMID: 26276827; PubMed Central PMCID: PMC4593838.
- Herskowitz JH, Feng Y, Mattheyses AL, Hales CM, Higginbotham LA, Duong DM, Montine TJ, Troncoso JC, Thambisetty M, Seyfried NT, Levey AI, Lah JJ. Pharmacologic inhibition of ROCK2 suppresses amyloid-β production in an Alzheimer's disease mouse model. J Neurosci. 2013 Dec 4;33(49):19086-98. doi: 10.1523/JNEUROSCI.2508-13.2013. PubMed PMID: 24305806; PubMed Central PMCID: PMC3850036.
Products are for research use only. Not for human use.
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