SRT-3025

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;
UNII	L4WQ6846SR;
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;

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 (December 2014). "Angiotensin II induces mitochondrial oxidative stress and mtDNA damage in osteoblasts by inhibiting SIRT1–FoxO3a–MnSOD pathway". Biochemical and Biophysical Research Communications. 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, et al. (2015). "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. 10 (7): e0134391. Bibcode:2015PLoSO..1034391G. doi:10.1371/journal.pone.0134391. PMC 4520518. PMID 26226624.
^ Kim HN, Han L, Iyer S, de Cabo R, Zhao H, O'Brien CA, et al. (October 2015). "Sirtuin1 Suppresses Osteoclastogenesis by Deacetylating FoxOs". Molecular Endocrinology. 29 (10): 1498–509. doi:10.1210/me.2015-1133. PMC 4588729. PMID 26287518.
^ Zainabadi K (May 2019). "Drugs targeting SIRT1, a new generation of therapeutics for osteoporosis and other bone related disorders?". Pharmacological Research. 143: 97–105. doi:10.1016/j.phrs.2019.03.007. PMID 30862606. S2CID 76663834.
^ Artsi H, Gurt I, El-Haj M, Müller R, Kuhn GA, Ben Shalom G, et al. (2019). "Sirt1 Promotes a Thermogenic Gene Program in Bone Marrow Adipocytes: From Mice to (Wo)Men". Frontiers in Endocrinology. 10: 126. doi:10.3389/fendo.2019.00126. PMC 6403178. PMID 30873124.
^ Zhang QS, Deater M, Schubert K, Marquez-Loza L, Pelz C, Sinclair DA, Grompe M (July 2015). "The Sirt1 activator SRT3025 expands hematopoietic stem and progenitor cells and improves hematopoiesis in Fanconi anemia mice". Stem Cell Research. 15 (1): 130–40. doi:10.1016/j.scr.2015.05.007. PMC 4516677. PMID 26046330.
^ Lin X, Liu C, Wang T, Wang H, Shao Z (2019). "Sirt1 in the Regulation of Interferon Gamma in Severe Aplastic Anemia". Acta Haematologica. 142 (3): 142–148. doi:10.1159/000497404. PMID 31141802. S2CID 169038775.

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[1] Li Y, Shen G, Yu C, Li G, Shen J, Gong J, Xu Y (December 2014). "Angiotensin II induces mitochondrial oxidative stress and mtDNA damage in osteoblasts by inhibiting SIRT1–FoxO3a–MnSOD pathway". Biochemical and Biophysical Research Communications. 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, et al. (2015). "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. 10 (7): e0134391. Bibcode:2015PLoSO..1034391G. doi:10.1371/journal.pone.0134391. PMC 4520518. PMID 26226624.

[3] Kim HN, Han L, Iyer S, de Cabo R, Zhao H, O'Brien CA, et al. (October 2015). "Sirtuin1 Suppresses Osteoclastogenesis by Deacetylating FoxOs". Molecular Endocrinology. 29 (10): 1498–509. doi:10.1210/me.2015-1133. PMC 4588729. PMID 26287518.

[4] Zainabadi K (May 2019). "Drugs targeting SIRT1, a new generation of therapeutics for osteoporosis and other bone related disorders?". Pharmacological Research. 143: 97–105. doi:10.1016/j.phrs.2019.03.007. PMID 30862606. S2CID 76663834.

[5] Artsi H, Gurt I, El-Haj M, Müller R, Kuhn GA, Ben Shalom G, et al. (2019). "Sirt1 Promotes a Thermogenic Gene Program in Bone Marrow Adipocytes: From Mice to (Wo)Men". Frontiers in Endocrinology. 10: 126. doi:10.3389/fendo.2019.00126. PMC 6403178. PMID 30873124.

[6] Zhang QS, Deater M, Schubert K, Marquez-Loza L, Pelz C, Sinclair DA, Grompe M (July 2015). "The Sirt1 activator SRT3025 expands hematopoietic stem and progenitor cells and improves hematopoiesis in Fanconi anemia mice". Stem Cell Research. 15 (1): 130–40. doi:10.1016/j.scr.2015.05.007. PMC 4516677. PMID 26046330.

[7] Lin X, Liu C, Wang T, Wang H, Shao Z (2019). "Sirt1 in the Regulation of Interferon Gamma in Severe Aplastic Anemia". Acta Haematologica. 142 (3): 142–148. doi:10.1159/000497404. PMID 31141802. S2CID 169038775.

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See also

References