SRT-2104

SRT-2104
Identifiers
	IUPAC name 4-methyl-N-[2-[3-(morpholin-4-ylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]-2-pyridin-3-yl-1,3-thiazole-5-carboxamide;
CAS Number	1093403-33-8;
PubChem CID	25108829;
DrugBank	DB12186 ;
ChemSpider	28637794;
UNII	4521NR0J09;
ChEMBL	ChEMBL4297436;
CompTox Dashboard ( EPA)	DTXSID00648729 ;
Chemical and physical data
Formula	C26H24N6O2S2
Molar mass	516.64 g·mol−1
3D model ( JSmol)	Interactive image;
	SMILES CC1=C(SC(=N1)C2=CN=CC=C2)C(=O)NC3=CC=CC=C3C4=CN5C(=CSC5=N4)CN6CCOCC6;
	InChI InChI=1S/C26H24N6O2S2/c1-17-23(36-25(28-17)18-5-4-8-27-13-18)24(33)29-21-7-3-2-6-20(21)22-15-32-19(16-35-26(32)30-22)14-31-9-11-34-12-10-31/h2-8,13,15-16H,9-12,14H2,1H3,(H,29,33); Key:LAMQVIQMVKWXOC-UHFFFAOYSA-N;

SRT-2104 is an experimental drug that was studied by Sirtris Pharmaceuticals as a small-molecule activator of the sirtuin subtype SIRT1. The compound progressed to Phase II human trials for Type II diabetes before development was discontinued, however it continues to be widely used in animal research into the functions of SIRT1.^[1]^[2]^[3]^[4]^[5]

References

^ Baksi A, Kraydashenko O, Zalevkaya A, Stets R, Elliott P, Haddad J, et al. (July 2014). "A phase II, randomized, placebo-controlled, double-blind, multi-dose study of SRT2104, a SIRT1 activator, in subjects with type 2 diabetes". British Journal of Clinical Pharmacology. 78 (1): 69–77. doi: 10.1111/bcp.12327. PMC 4168381. PMID 24446723.
^ Bonkowski MS, Sinclair DA (November 2016). "+ and sirtuin-activating compounds". Nature Reviews. Molecular Cell Biology. 17 (11): 679–690. doi: 10.1038/nrm.2016.93. PMC 5107309. PMID 27552971.
^ Miyaji N, Nishida K, Tanaka T, Araki D, Kanzaki N, Hoshino Y, et al. (January 2020). "Inhibition of Knee Osteoarthritis Progression in Mice by Administering SRT2014, an Activator of Silent Information Regulator 2 Ortholog 1". Cartilage. 13 (2_suppl): 1356S–1366S. doi: 10.1177/1947603519900795. PMC 8804762. PMID 31989845.
^ Gu C, Zhang Q, Ni D, Xiao QF, Cao LF, Fei CY, et al. (August 2020). "Therapeutic Effects of SRT2104 on Lung Injury in Rats with Emphysema via Reduction of Type II Alveolar Epithelial Cell Senescence". Copd. 17 (4): 444–451. doi: 10.1080/15412555.2020.1797657. PMID 32722945. S2CID 220852823.
^ Lei Y, Wang J, Wang D, Li C, Liu B, Fang X, et al. (May 2020). "SIRT1 in forebrain excitatory neurons produces sexually dimorphic effects on depression-related behaviors and modulates neuronal excitability and synaptic transmission in the medial prefrontal cortex". Molecular Psychiatry. 25 (5): 1094–1111. doi: 10.1038/s41380-019-0352-1. PMC 7192847. PMID 30705425.

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[1] Baksi A, Kraydashenko O, Zalevkaya A, Stets R, Elliott P, Haddad J, et al. (July 2014). "A phase II, randomized, placebo-controlled, double-blind, multi-dose study of SRT2104, a SIRT1 activator, in subjects with type 2 diabetes". British Journal of Clinical Pharmacology. 78 (1): 69–77. doi: 10.1111/bcp.12327. PMC 4168381. PMID 24446723.

[2] Bonkowski MS, Sinclair DA (November 2016). "+ and sirtuin-activating compounds". Nature Reviews. Molecular Cell Biology. 17 (11): 679–690. doi: 10.1038/nrm.2016.93. PMC 5107309. PMID 27552971.

[3] Miyaji N, Nishida K, Tanaka T, Araki D, Kanzaki N, Hoshino Y, et al. (January 2020). "Inhibition of Knee Osteoarthritis Progression in Mice by Administering SRT2014, an Activator of Silent Information Regulator 2 Ortholog 1". Cartilage. 13 (2_suppl): 1356S–1366S. doi: 10.1177/1947603519900795. PMC 8804762. PMID 31989845.

[4] Gu C, Zhang Q, Ni D, Xiao QF, Cao LF, Fei CY, et al. (August 2020). "Therapeutic Effects of SRT2104 on Lung Injury in Rats with Emphysema via Reduction of Type II Alveolar Epithelial Cell Senescence". Copd. 17 (4): 444–451. doi: 10.1080/15412555.2020.1797657. PMID 32722945. S2CID 220852823.

[5] Lei Y, Wang J, Wang D, Li C, Liu B, Fang X, et al. (May 2020). "SIRT1 in forebrain excitatory neurons produces sexually dimorphic effects on depression-related behaviors and modulates neuronal excitability and synaptic transmission in the medial prefrontal cortex". Molecular Psychiatry. 25 (5): 1094–1111. doi: 10.1038/s41380-019-0352-1. PMC 7192847. PMID 30705425.

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Identifiers

IUPAC name 4-methyl-N-[2-[3-(morpholin-4-ylmethyl)imidazo[2,1-b][1,3]thiazol-6-yl]phenyl]-2-pyridin-3-yl-1,3-thiazole-5-carboxamide
CAS Number	1093403-33-8
PubChem CID	25108829
DrugBank	DB12186^Y
ChemSpider	28637794
UNII	4521NR0J09
ChEMBL	ChEMBL4297436
CompTox Dashboard ( EPA)	DTXSID00648729
Chemical and physical data
Formula	C₂₆H₂₄N₆O₂S₂
Molar mass	516.64 g·mol⁻¹
3D model ( JSmol)	Interactive image
SMILES CC1=C(SC(=N1)C2=CN=CC=C2)C(=O)NC3=CC=CC=C3C4=CN5C(=CSC5=N4)CN6CCOCC6
InChI InChI=1S/C26H24N6O2S2/c1-17-23(36-25(28-17)18-5-4-8-27-13-18)24(33)29-21-7-3-2-6-20(21)22-15-32-19(16-35-26(32)30-22)14-31-9-11-34-12-10-31/h2-8,13,15-16H,9-12,14H2,1H3,(H,29,33) Key:LAMQVIQMVKWXOC-UHFFFAOYSA-N