TC-S 7001

TC-S 7001 is an inhibitor of Rho-associated kinase (ROCK, IC50s = 0.6 and 1.1 nM, respectively, for human ROCK1 and ROCK2). It is selective for ROCK over myosin light-chain kinase (MLCK) and zipper-interacting protein kinase (ZIP-kinase, IC50s = 7,400 and 4,100 nM, respectively), as well as 110 kinases in a panel at 1-10 µM, but does inhibit TRK and FLT3 (IC50s = 252 and 303 nM, respectively). TC-S 7001 reduces ROCK2-induced phosphorylation of human myosin-binding subunit (MBS) when used at a concentration of 3 nM and decreases ROCK2 autophosphorylation. It inhibits contraction of isolated rabbit saphenous artery induced by phenylephrine (IC50 = 65 nM) and decreases blood pressure in normotensive and hypertensive rats when administered at doses of 3 and 10 mg/kg. TC-S 7001 also decreases right ventricular systolic pressure and total pulmonary resistance in a rat model of monocrotaline-induced pulmonary hypertension when administered at a dose of 10 mg/kg per day.Formal Name: 6-chloro-N4-[3,5-difluoro-4-[(3-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl]-2,4-pyrimidinediamine. CAS Number: 867017-68-3. Synonyms: Azaindole 1. Molecular Formula: C18H13ClF2N6O. Formula Weight: 402.8. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble, Ethanol: Soluble. lambdamax: 225, 266, 305, 311 nm. SMILES: ClC1=NC(N)=NC(NC2=CC(F)=C(OC3=CC=NC4=C3C(C)=CN4)C(F)=C2)=C1. InChi Code: InChI=1S/C18H13ClF2N6O/c1-8-7-24-17-15(8)12(2-3-23-17)28-16-10(20)4-9(5-11(16)21)25-14-6-13(19)26-18(22)27-14/h2-7H,1H3,(H,23,24)(H3,22,25,26,27). InChi Key: NRSGWEVTVGZDFC-UHFFFAOYSA-N.