SRT2183

製品コードS8270 バッチS827001

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₇H₂₄N₄O₂S

分子量

468.57

CAS No.

1001908-89-9

Solubility (25°C)*

体外

DMSO

93 mg/mL (198.47 mM)

Ethanol

3 mg/mL (6.4 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	4.65mg/ml (9.92mM)	Taking the 1 mL working solution as an example, add 50 μL of 93 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.465mg/ml (0.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 9.3 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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	SRT2183は、現在Sirtris Pharmaceuticals社によって開発されている、サーチュインサブタイプSIRT1の低分子活性化因子です。
in vitro	SRT2183 is potent with growth arrest and apoptosis induced at doses ranging from 1-20 μM. This compound treatment leads to increased mRNA levels of pro-apoptosis, growth arrest, and DNA damage response genes. SRT1720, this chemical, SRT1460, and resveratrol exhibit multiple off-target activities against receptors, enzymes, transporters, and ion channels. They are not direct activators of SIRT1. It has little or no effect on SIRT1 deacetylating activity with native full-length substrates. This compound activates AMPK, increases Sirt1 expression and decreases RelA/p65 lysine310 acetylation, critical for NF-κB activation, and an established Sirt1 target and inhibits RANKL-induced osteoclast generation and resorptive capacity in bone marrow macrophages.

製品説明

SRT2183は、現在Sirtris Pharmaceuticals社によって開発されている、サーチュインサブタイプSIRT1の低分子活性化因子です。

in vitro

SRT2183 is potent with growth arrest and apoptosis induced at doses ranging from 1-20 μM. This compound treatment leads to increased mRNA levels of pro-apoptosis, growth arrest, and DNA damage response genes. SRT1720, this chemical, SRT1460, and resveratrol exhibit multiple off-target activities against receptors, enzymes, transporters, and ion channels. They are not direct activators of SIRT1. It has little or no effect on SIRT1 deacetylating activity with native full-length substrates. This compound activates AMPK, increases Sirt1 expression and decreases RelA/p65 lysine310 acetylation, critical for NF-κB activation, and an established Sirt1 target and inhibits RANKL-induced osteoclast generation and resorptive capacity in bone marrow macrophages.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Bone-marrow derived macrophages(BMMs)
	濃度	1μM
	反応時間	72 h
	実験の流れ	BMMs are harvested, plated and 24-hrs later non-adherent cells were re-plated at a density of 20,000 cells/well in α-MEM/15%FBS/5% M-CSF. For determining cell proliferation, cells are treated with SRT2183 or a vehicle for 72 hours post plating and BrdU reagent is added 48 hrs post this compound or vehicle administration according to the manufacturer's instructions to determine cell proliferation 3 days post plating.

参考

https://pubmed.ncbi.nlm.nih.gov/18046409/
http://www.bloodjournal.org/content/114/22/3083?sso-checked=true
https://pubmed.ncbi.nlm.nih.gov/20061378/

https://pubmed.ncbi.nlm.nih.gov/20061378/

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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：

Neutrophils shape the therapeutic efficacy of sirtuin 1 activity modulators in murine influenza virus infection [ Biochim Biophys Acta Mol Basis Dis, 2025, 1871(7):167915]	PubMed: 40419167
SIRT1 and HSP90α feed-forward circuit safeguards chromosome segregation integrity in diffuse large B cell lymphomas [ Cell Death Dis, 2023, 14(10):667]	PubMed: 37816710
SRT2183 and SRT1720, but not Resveratrol, Inhibit Osteoclast Formation and Resorption in the Presence or Absence of Sirt1 [ J Bone Res, 2023, 11(4)1000235]	PubMed: 37711761
Sirtuin activation targets IDH-mutant tumors [ Neuro Oncol, 2021, 23(1):53-62]	PubMed: 32710757
Lactate promotes macrophage HMGB1 lactylation, acetylation, and exosomal release in polymicrobial sepsis [ Cell Death Differ, 2021, 10.1038/s41418-021-00841-9]	PubMed: 34363018
Sirt1 attenuates diabetic keratopathy by regulating the endoplasmic reticulum stress pathway [ Life Sci, 2020, S0024-3205(20)31542-3]	PubMed: 33220291

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。