SRT-3025: Difference between revisions

SRT-3025
Identifiers
	IUPAC name 5-(3-methoxypropyl)-2-phenyl-N-[2-[6-(pyrrolidin-1-ylmethyl)-[1,3]thiazolo[5,4-b]pyridin-2-yl]phenyl]-1,3-thiazole-4-carboxamide;
CAS Number	1231952-55-8;
PubChem CID	46245047;
CompTox Dashboard (EPA)	DTXSID301336673 ;
Chemical and physical data
Formula	C31H31N5O2S2
Molar mass	569.74 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES COCCCC1=C(N=C(S1)C2=CC=CC=C2)C(=O)NC3=CC=CC=C3C4=NC5=C(S4)N=CC(=C5)CN6CCCC6;
	InChI InChI=1S/C31H31N5O2S2/c1-38-17-9-14-26-27(35-29(39-26)22-10-3-2-4-11-22)28(37)33-24-13-6-5-12-23(24)30-34-25-18-21(19-32-31(25)40-30)20-36-15-7-8-16-36/h2-6,10-13,18-19H,7-9,14-17,20H2,1H3,(H,33,37); Key:MRRXPMZNBRXCPZ-UHFFFAOYSA-N;

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Revision as of 23:55, 23 December 2020

SRT-3025 is an experimental drug that was studied by Sirtris Pharmaceuticals as a small-molecule activator of the sirtuin subtype SIRT1. It has been investigated as a potential treatment for osteoporosis,^[1]^[2]^[3]^[4]^[5] and anemia.^[6]^[7]

References

^ Li Y, Shen G, Yu C, Li G, Shen J, Gong J, Xu Y. Angiotensin II induces mitochondrial oxidative stress and mtDNA damage in osteoblasts by inhibiting SIRT1–FoxO3a–MnSOD pathway. Biochem Biophys Res Commun. 2014 Dec 5;455(1-2):113-8. doi:10.1016/j.bbrc.2014.10.123 PMID 25450701
^ Gurt I, Artsi H, Cohen-Kfir E, Hamdani G, Ben-Shalom G, Feinstein B, El-Haj M, Dresner-Pollak R. The Sirt1 Activators SRT2183 and SRT3025 Inhibit RANKL-Induced Osteoclastogenesis in Bone Marrow-Derived Macrophages and Down-Regulate Sirt3 in Sirt1 Null Cells. PLoS One. 2015 Jul 30;10(7):e0134391. doi:10.1371/journal.pone.0134391 PMID 26226624
^ Kim HN, Han L, Iyer S, de Cabo R, Zhao H, O'Brien CA, Manolagas SC, Almeida M. Sirtuin1 Suppresses Osteoclastogenesis by Deacetylating FoxOs. Mol Endocrinol. 2015 Oct;29(10):1498-509. doi:10.1210/me.2015-1133 PMID 26287518
^ Zainabadi K. Drugs targeting SIRT1, a new generation of therapeutics for osteoporosis and other bone related disorders? Pharmacol Res. 2019 May;143:97-105. doi:10.1016/j.phrs.2019.03.007 PMID 30862606
^ Artsi H, Gurt I, El-Haj M, Müller R, Kuhn GA, Ben Shalom G, Cohen-Kfir E, Abramowitz E, Kandel L, Safran O, Dresner-Pollak R. Sirt1 Promotes a Thermogenic Gene Program in Bone Marrow Adipocytes: From Mice to (Wo)Men. Front Endocrinol (Lausanne). 2019 Feb 28;10:126. doi:10.3389/fendo.2019.00126 PMID 30873124
^ Zhang QS, Deater M, Schubert K, Marquez-Loza L, Pelz C, Sinclair DA, Grompe M. The Sirt1 activator SRT3025 expands hematopoietic stem and progenitor cells and improves hematopoiesis in Fanconi anemia mice. Stem Cell Res. 2015 Jul;15(1):130-40. doi:10.1016/j.scr.2015.05.007 PMID 26046330
^ Lin X, Liu C, Wang T, Wang H, Shao Z. Sirt1 in the Regulation of Interferon Gamma in Severe Aplastic Anemia. Acta Haematol. 2019;142(3):142-148. doi:10.1159/000497404 PMID 31141802

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[1] Li Y, Shen G, Yu C, Li G, Shen J, Gong J, Xu Y. Angiotensin II induces mitochondrial oxidative stress and mtDNA damage in osteoblasts by inhibiting SIRT1–FoxO3a–MnSOD pathway. Biochem Biophys Res Commun. 2014 Dec 5;455(1-2):113-8. doi:10.1016/j.bbrc.2014.10.123 PMID 25450701

[2] Gurt I, Artsi H, Cohen-Kfir E, Hamdani G, Ben-Shalom G, Feinstein B, El-Haj M, Dresner-Pollak R. The Sirt1 Activators SRT2183 and SRT3025 Inhibit RANKL-Induced Osteoclastogenesis in Bone Marrow-Derived Macrophages and Down-Regulate Sirt3 in Sirt1 Null Cells. PLoS One. 2015 Jul 30;10(7):e0134391. doi:10.1371/journal.pone.0134391 PMID 26226624

[3] Kim HN, Han L, Iyer S, de Cabo R, Zhao H, O'Brien CA, Manolagas SC, Almeida M. Sirtuin1 Suppresses Osteoclastogenesis by Deacetylating FoxOs. Mol Endocrinol. 2015 Oct;29(10):1498-509. doi:10.1210/me.2015-1133 PMID 26287518

[4] Zainabadi K. Drugs targeting SIRT1, a new generation of therapeutics for osteoporosis and other bone related disorders? Pharmacol Res. 2019 May;143:97-105. doi:10.1016/j.phrs.2019.03.007 PMID 30862606

[5] Artsi H, Gurt I, El-Haj M, Müller R, Kuhn GA, Ben Shalom G, Cohen-Kfir E, Abramowitz E, Kandel L, Safran O, Dresner-Pollak R. Sirt1 Promotes a Thermogenic Gene Program in Bone Marrow Adipocytes: From Mice to (Wo)Men. Front Endocrinol (Lausanne). 2019 Feb 28;10:126. doi:10.3389/fendo.2019.00126 PMID 30873124

[6] Zhang QS, Deater M, Schubert K, Marquez-Loza L, Pelz C, Sinclair DA, Grompe M. The Sirt1 activator SRT3025 expands hematopoietic stem and progenitor cells and improves hematopoiesis in Fanconi anemia mice. Stem Cell Res. 2015 Jul;15(1):130-40. doi:10.1016/j.scr.2015.05.007 PMID 26046330

[7] Lin X, Liu C, Wang T, Wang H, Shao Z. Sirt1 in the Regulation of Interferon Gamma in Severe Aplastic Anemia. Acta Haematol. 2019;142(3):142-148. doi:10.1159/000497404 PMID 31141802

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Revision as of 23:55, 23 December 2020

See also

References