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{{Short description|Chemical compound}}
{{Drugbox
{{Drugbox
| 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
| 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
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| CAS_number = 867017-68-3
| CAS_number = 867017-68-3
| PubChem = 11524200
| PubChem = 11524200
| ChemSpiderID =
| ChemSpiderID = 9698986
| ChEMBL = 1971943
<!--Chemical data-->
<!--Chemical data-->
| C=18 | H=13 | Cl=1 | F=2 | N=6 | O=1
| C=18 | H=13 | Cl=1 | F=2 | N=6 | O=1
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}}
}}


'''TCS-7001''' ('''Azaindole-1''') is a drug which acts as a potent and selective inhibitor of the [[enzyme]] [[Rho kinase]], with an IC<sub>50</sub> of 0.6 nM at [[ROCK1]] and 1.1 nM at [[ROCK2]].<ref>{{cite journal | vauthors = 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 | display-authors = 6 | title = Cardiovascular effects of a novel potent and highly selective azaindole-based inhibitor of Rho-kinase | journal = British Journal of Pharmacology | volume = 152 | issue = 7 | pages = 1070–80 | date = December 2007 | pmid = 17934515 | doi = 10.1038/sj.bjp.0707484 }}</ref> It has [[vasodilator]]y effects and has been used in research for a variety of applications.<ref>{{cite journal | vauthors = 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 | display-authors = 6 | title = Therapeutic efficacy of azaindole-1 in experimental pulmonary hypertension | journal = The European Respiratory Journal | volume = 36 | issue = 4 | pages = 808–18 | date = October 2010 | pmid = 20530035 | doi = 10.1183/09031936.00140309 }}</ref><ref>{{cite journal | vauthors = Pankey EA, Byun RJ, Smith WB, Bhartiya M, Bueno FR, Badejo AM, Stasch JP, Murthy SN, Nossaman BD, Kadowitz PJ | display-authors = 6 | title = The Rho kinase inhibitor azaindole-1 has long-acting vasodilator activity in the pulmonary vascular bed of the intact chest rat | journal = Canadian Journal of Physiology and Pharmacology | volume = 90 | issue = 7 | pages = 825–35 | date = July 2012 | pmid = 22591047 | doi = 10.1139/y2012-061 }}</ref><ref>{{cite journal | vauthors = Lasker GF, Pankey EA, Allain AV, Murthy SN, Stasch JP, Kadowitz PJ | title = The selective Rho-kinase inhibitor azaindole-1 has long-lasting erectile activity in the rat | journal = Urology | volume = 81 | issue = 2 | pages = 465.e7-14 | date = February 2013 | pmid = 23374844 | doi = 10.1016/j.urology.2012.10.039 }}</ref>
'''TC-S 7001''' ('''Azaindole-1''') is a drug which acts as a potent and selective inhibitor of the [[enzyme]] [[Rho kinase]], with an IC<sub>50</sub> of 0.6 nM at [[ROCK1]] and 1.1 nM at [[ROCK2]].<ref>{{cite journal | vauthors = 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 | display-authors = 6 | title = Cardiovascular effects of a novel potent and highly selective azaindole-based inhibitor of Rho-kinase | journal = British Journal of Pharmacology | volume = 152 | issue = 7 | pages = 1070–80 | date = December 2007 | pmid = 17934515 | doi = 10.1038/sj.bjp.0707484 | pmc = 2095102 }}</ref> It has [[vasodilator]]y effects and has been used in research for a variety of applications.<ref>{{cite journal | vauthors = 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 | display-authors = 6 | title = Therapeutic efficacy of azaindole-1 in experimental pulmonary hypertension | journal = The European Respiratory Journal | volume = 36 | issue = 4 | pages = 808–18 | date = October 2010 | pmid = 20530035 | doi = 10.1183/09031936.00140309 | s2cid = 10991200 | doi-access = free }}</ref><ref>{{cite journal | vauthors = Pankey EA, Byun RJ, Smith WB, Bhartiya M, Bueno FR, Badejo AM, Stasch JP, Murthy SN, Nossaman BD, Kadowitz PJ | display-authors = 6 | title = The Rho kinase inhibitor azaindole-1 has long-acting vasodilator activity in the pulmonary vascular bed of the intact chest rat | journal = Canadian Journal of Physiology and Pharmacology | volume = 90 | issue = 7 | pages = 825–35 | date = July 2012 | pmid = 22591047 | doi = 10.1139/y2012-061 }}</ref><ref>{{cite journal | vauthors = Lasker GF, Pankey EA, Allain AV, Murthy SN, Stasch JP, Kadowitz PJ | title = The selective Rho-kinase inhibitor azaindole-1 has long-lasting erectile activity in the rat | journal = Urology | volume = 81 | issue = 2 | pages = 465.e7–14 | date = February 2013 | pmid = 23374844 | doi = 10.1016/j.urology.2012.10.039 | pmc = 3564057 }}</ref>


== See also ==
== See also ==

Latest revision as of 10:26, 23 April 2022

TC-S 7001
Identifiers
  • 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
PubChem CID
ChemSpider
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC18H13ClF2N6O
Molar mass402.79 g·mol−1
3D model (JSmol)
  • CC1=CNC2=NC=CC(=C12)OC3=C(C=C(C=C3F)NC4=CC(=NC(=N4)N)Cl)F
  • 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.[1] It has vasodilatory effects and has been used in research for a variety of applications.[2][3][4]

See also

[edit]

References

[edit]
  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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