| Identification | Back Directory | [Name]
SRT2104 (GSK2245840) | [CAS]
1093403-33-8 | [Synonyms]
CS-2293
GSK2245840
SRT-2104;SRT 2104
sirtuin Modulator
SRT2104 (GSK2245840)
SRT2104 (GSK2245840) USP/EP/BP
(E)-3-(3-HYDROXY-4-METHOXYPHENYL)PROP-2-ENOIC ACID
4-methyl-N-(2-(3-(morpholinomethyl)imidazo[2,1-b]thiazol-6-yl)phenyl)-2-(yridine-3-yl)thiazole-5-carboxamide
4-Methyl-N-[2-[3-(morpholinomethyl)imidazo[2,1-b]thiazol-6-yl]phenyl]-2-(pyridin-3-yl)thiazole-5-carboxamide
5-ThiazolecarboxaMide, 4-Methyl-N-[2-[3-(4-MorpholinylMethyl)iMidazo[2,1-b]thiazol-6-yl]phenyl]-2-(3-pyridinyl)-
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 | [Molecular Formula]
C26H24N6O2S2 | [MDL Number]
MFCD22572733 | [MOL File]
1093403-33-8.mol | [Molecular Weight]
516.638 |
| Chemical Properties | Back Directory | [density ]
1.46±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; insoluble in EtOH; ≥6.46 mg/mL in DMSO with gentle warming | [form ]
Powder | [pka]
11.40±0.70(Predicted) | [color ]
Light yellow to yellow | [InChIKey]
LAMQVIQMVKWXOC-UHFFFAOYSA-N | [SMILES]
S1C(C(NC2=CC=CC=C2C2=CN3C(CN4CCOCC4)=CSC3=N2)=O)=C(C)N=C1C1=CC=CN=C1 |
| Hazard Information | Back Directory | [Uses]
SRT 2104 is a first-in-class, highly selective and brain-permeable activator of the NAD+ dependent deacetylase Sirt1, increases Sirt1 protein, but shows no effect on Sirt1 mRNA. Used in the research of diabetes mellitus and Huntington’s disease[1][2][3]. | [Biological Activity]
srt2104 (gsk2245840) is a selective sirt1 activator involved in the regulation of energy homeostasis. sirt1, also known as nad-dependent deacetylase sirtuin-1, is a member of the sirtuin family of proteins. | [in vitro]
in c2c12 myoblasts stably transfected with small hairpin rna to knock-down sirt1, srt2104 increased ap activity, a marker for osteogenic differentiation. this effect was totally dependent on sirt1 expression [1]. | [in vivo]
in male c57bl/6j mice, administration of srt2104 (100 mg/kg, p.o.) extended both mean and maximal lifespan of mice fed a standard diet, and enhanced bone mineral density, motor coordination, and insulin sensitivity and decreased inflammation. short-term srt2104 administration preserved bone and muscle mass in an experimental model of atrophy [1]. in male n171-82q hd mice with huntington's disease, srt2104 (diet containing 0.5% srt2104) effectively penetrated the blood-brain barrier, attenuated brain atrophy, improved motor function, and extended survival [2]. | [IC 50]
SIRT1 | [storage]
Store at -20°C | [References]
[1]. mercken e m, mitchell s j, martin‐montalvo a, et al. srt2104 extends survival of male mice on a standard diet and preserves bone and muscle mass[j]. aging cell, 2014, 13(5): 787-796.
[2]. jiang m, zheng j, peng q, et al. sirtuin 1 activator srt2104 protects huntington's disease mice[j]. annals of clinical and translational neurology, 2014, 1(12): 1047-1052. |
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| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
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| Website: |
www.spiropharma.com.cn |
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