SRT3025 HCl

製品コードS8481 バッチS848101

印刷

化学情報

 Chemical Structure Synonyms N/A Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C31H31N5O2S2.HCl

分子量 606.2 CAS No. 2070015-26-6
Solubility (25°C)* 体外 DMSO 100 mg/mL warmed with 50ºC water bath (164.96 mM)
Ethanol 5 mg/mL warmed with 50ºC water bath (8.24 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 SRT3025 is an orally available small molecule activator of the SIRT1 enzyme.
in vitro SRT3025 inhibits RANKL-induced osteoclast differentiation, fusion and resorptive capacity without affecting osteoclast survival. SRT3025 inhibits RANKL-induced osteoclastogenesis in bone marrow-derived macrophages (BMMs) by activating AMPK and deacetylating RelA/p65 lysine 310, critical for activation of the NF-κB signaling pathway[2]. SRT3025 acts faster than oxymetholone to improve hematopoiesis. It does not work by direct activation of Sirt1 in hematopoietic cells. SRT3025 might suppress p21 transcription through the down-regulation of Egr1[3]. SRT3025 is found to activate wild-type Sirt1 protein but failed to activate the E230K mutant, an activation-resistant Sirt1 protein (due to a mutation at position 230)[4].
in vivo SRT3025 treatment also inhibits tumor growth in Panc-1 xenografts, even though it is not as effective in inhibiting the viability of Panc-1 cells in culture. SRT3025 is well tolerated in mice and has the potential to be used in several diseases[1]. SRT3025 administration expands HSPCs and boosts blood counts while long term SRT3025 administration does not permanently increase or decrease HSC repopulating potential[3]. SRT3025 reduces plasma cholesterol, inflammation, and atherosclerosis in Apoe−/− mice, and it increases hepatic Ldlr expression and Pcsk9 accumulation[4].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HPDE, Panc-1, SU86.86, Patu8988t cells
濃度 0-5 μM
反応時間 72 h
実験の流れ

Cells are treated with vehicle or different concentrations of SRT3025 for 72 hours and submitted to MTT analysis. 

動物実験 動物モデル Female athymic nu/nu mice
投薬量 50-200 mg/kg
投与方法 oral administration

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Sirtuin activation targets IDH-mutant tumors [ Neuro Oncol, 2021, 23(1):53-62] PubMed: 32710757
Geriatric Fragility Fractures Are Associated With a Human Skeletal Stem Cell Defect [ Aging Cell, 2020, e13164] PubMed: 32537886
Sirt1 in the Regulation of Interferon Gamma in Severe Aplastic Anemia. [ Acta Haematol, 2019, 142(3):142-148] PubMed: 31141802

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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