TC-S 7001

TC-S 7001
Identifiers
	IUPAC name 6-chloro-4-N-[3,5-difluoro-4-[(3-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl]pyrimidine-2,4-diamine;
CAS Number	867017-68-3;
PubChem CID	11524200;
CompTox Dashboard (EPA)	DTXSID00468040 ;
Chemical and physical data
Formula	C18H13ClF2N6O
Molar mass	402.79 g·mol−1
3D model (JSmol)	Interactive image;
	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;

TCS-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.^[1] It has vasodilatory effects and has been used in research for a variety of applications.^[2]^[3]^[4]

References

^ Kast R, Schirok H, Figueroa-Pérez S, Mittendorf J, Gnoth MJ, Apeler H, Lenz J, Franz JK, Knorr A, Hütter J, Lobell M, Zimmermann K, Münter K, Augstein KH, Ehmke H, Stasch JP. Cardiovascular effects of a novel potent and highly selective azaindole-based inhibitor of Rho-kinase. Br J Pharmacol. 2007 Dec;152(7):1070-80. doi:10.1038/sj.bjp.0707484 Template:Pmid17934515
^ Dahal BK, Kosanovic D, Pamarthi PK, Sydykov A, Lai YJ, Kast R, Schirok H, Stasch JP, Ghofrani HA, Weissmann N, Grimminger F, Seeger W, Schermuly RT. Therapeutic efficacy of azaindole-1 in experimental pulmonary hypertension. Eur Respir J. 2010 Oct;36(4):808-18. doi:10.1183/09031936.00140309 PMID 20530035
^ Pankey EA, Byun RJ, Smith WB 2nd, Bhartiya M, Bueno FR, Badejo AM, Stasch JP, Murthy SN, Nossaman BD, Kadowitz PJ. The Rho kinase inhibitor azaindole-1 has long-acting vasodilator activity in the pulmonary vascular bed of the intact chest rat. Can J Physiol Pharmacol. 2012 Jul;90(7):825-35. doi:10.1139/y2012-061 PMID 22591047
^ Lasker GF, Pankey EA, Allain AV, Murthy SN, Stasch JP, Kadowitz PJ. The selective Rho-kinase inhibitor azaindole-1 has long-lasting erectile activity in the rat. Urology. 2013 Feb;81(2):465.e7-14. doi:10.1016/j.urology.2012.10.039 PMID 23374844

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[1] Kast R, Schirok H, Figueroa-Pérez S, Mittendorf J, Gnoth MJ, Apeler H, Lenz J, Franz JK, Knorr A, Hütter J, Lobell M, Zimmermann K, Münter K, Augstein KH, Ehmke H, Stasch JP. Cardiovascular effects of a novel potent and highly selective azaindole-based inhibitor of Rho-kinase. Br J Pharmacol. 2007 Dec;152(7):1070-80. doi:10.1038/sj.bjp.0707484 Template:Pmid17934515

[2] Dahal BK, Kosanovic D, Pamarthi PK, Sydykov A, Lai YJ, Kast R, Schirok H, Stasch JP, Ghofrani HA, Weissmann N, Grimminger F, Seeger W, Schermuly RT. Therapeutic efficacy of azaindole-1 in experimental pulmonary hypertension. Eur Respir J. 2010 Oct;36(4):808-18. doi:10.1183/09031936.00140309 PMID 20530035

[3] Pankey EA, Byun RJ, Smith WB 2nd, Bhartiya M, Bueno FR, Badejo AM, Stasch JP, Murthy SN, Nossaman BD, Kadowitz PJ. The Rho kinase inhibitor azaindole-1 has long-acting vasodilator activity in the pulmonary vascular bed of the intact chest rat. Can J Physiol Pharmacol. 2012 Jul;90(7):825-35. doi:10.1139/y2012-061 PMID 22591047

[4] Lasker GF, Pankey EA, Allain AV, Murthy SN, Stasch JP, Kadowitz PJ. The selective Rho-kinase inhibitor azaindole-1 has long-lasting erectile activity in the rat. Urology. 2013 Feb;81(2):465.e7-14. doi:10.1016/j.urology.2012.10.039 PMID 23374844

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