A ROCK inhibitor (IC50s = 0.6 and 1.1 nM

TC-S 7001 – 5 mg

Brand:
Cayman
CAS:
867017-68-3
Storage:
-20
UN-No:
Non-Hazardous - /

TC-S 7001 is an inhibitor of Rho-associated kinase (ROCK; IC50s = 0.6 and 1.1 nM, respectively, for human ROCK-I and ROCK-II).{48172} 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 ROCK-II-induced phosphorylation of human myosin-binding subunit (MBS) when used at a concentration of 3 nM and decreases ROCK-II 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.{48173}  

 

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Description

A ROCK inhibitor (IC50s = 0.6 and 1.1 nM, respectively, for human ROCK-I and ROCK-II); selective for ROCK over MLCK and 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); reduces ROCK-II-induced MBS phosphorylation at 3 nM; inhibits phenylephrine-induced contraction of isolated rabbit saphenous artery (IC50 = 65 nM); decreases blood pressure in normotensive and hypertensive rats at 3 and 10 mg/kg; decreases right ventricular systolic pressure and total pulmonary resistance in a rat model of monocrotaline-induced pulmonary hypertension at 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

Synonyms:  Azaindole 1

Molecular weight: 402.8

CAS: 867017-68-3

Purity: ≥95%

Formulation: A solid

Product Type|Biochemicals|Kinase Inhibitors|ROCK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cell Biology|Cytoskeleton & Motor Proteins

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