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- SRT2104 (GSK2245840)
SRT2104 (GSK2245840)
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].
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.
| Storage | Store at -20°C |
| M.Wt | 516.64 |
| Cas No. | 1093403-33-8 |
| Formula | C26H24N6O2S2 |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥6.46 mg/mL in DMSO with gentle warming |
| Chemical 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 |
| SDF | Download SDF |
| Canonical SMILES | CC1=C(SC(=N1)C2=CN=CC=C2)C(=O)NC3=CC=CC=C3C4=CN5C(=CSC5=N4)CN6CCOCC6 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
C2C12 myoblasts |
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Preparation method |
Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
3 μM, 24 h |
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Applications |
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. SRT2104 treatment increased mitochondrial content and suppressed the inflammatory response. |
| Animal experiment [1]: | |
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Animal models |
Male C57BL/6J mice |
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Dosage form |
Oral administration, 100 mg/kg, 6 weeks |
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Application |
In male C57BL/6J mice, SRT2104 (100 mg/kg, p.o.) treatment improved whole-body physiology and extended lifespan and enhanced bone mineral density, motor coordination, and insulin sensitivity and decreased inflammation in mice fed a standard diet. Short-term SRT2104 administration preserved bone and muscle mass in an experimental model of atrophy. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. |
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