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TC-S 7001

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Chemical compound Pharmaceutical compound
TC-S 7001
Identifiers
IUPAC name
  • 6-chloro-4-N-pyridin-4-yl)oxy]phenyl]pyrimidine-2,4-diamine
CAS Number
PubChem CID
ChemSpider
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC18H13ClF2N6O
Molar mass402.79 g·mol
3D model (JSmol)
SMILES
  • CC1=CNC2=NC=CC(=C12)OC3=C(C=C(C=C3F)NC4=CC(=NC(=N4)N)Cl)F
InChI
  • 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)
  • Key:NRSGWEVTVGZDFC-UHFFFAOYSA-N

TC-S 7001 (Azaindole-1) is a drug which acts as a potent and selective inhibitor of the enzyme Rho kinase, with an IC50 of 0.6 nM at ROCK1 and 1.1 nM at ROCK2. It has vasodilatory effects and has been used in research for a variety of applications.

See also

References

  1. Kast R, Schirok H, Figueroa-Pérez S, Mittendorf J, Gnoth MJ, Apeler H, et al. (December 2007). "Cardiovascular effects of a novel potent and highly selective azaindole-based inhibitor of Rho-kinase". British Journal of Pharmacology. 152 (7): 1070–80. doi:10.1038/sj.bjp.0707484. PMC 2095102. PMID 17934515.
  2. Dahal BK, Kosanovic D, Pamarthi PK, Sydykov A, Lai YJ, Kast R, et al. (October 2010). "Therapeutic efficacy of azaindole-1 in experimental pulmonary hypertension". The European Respiratory Journal. 36 (4): 808–18. doi:10.1183/09031936.00140309. PMID 20530035. S2CID 10991200.
  3. Pankey EA, Byun RJ, Smith WB, Bhartiya M, Bueno FR, Badejo AM, et al. (July 2012). "The Rho kinase inhibitor azaindole-1 has long-acting vasodilator activity in the pulmonary vascular bed of the intact chest rat". Canadian Journal of Physiology and Pharmacology. 90 (7): 825–35. doi:10.1139/y2012-061. PMID 22591047.
  4. Lasker GF, Pankey EA, Allain AV, Murthy SN, Stasch JP, Kadowitz PJ (February 2013). "The selective Rho-kinase inhibitor azaindole-1 has long-lasting erectile activity in the rat". Urology. 81 (2): 465.e7–14. doi:10.1016/j.urology.2012.10.039. PMC 3564057. PMID 23374844.
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