3-TYP
(Synonyms: 吡啶-3-乙炔) 目录号 : GC19013
3-TYP 抑制 SIRT3，IC50 为 16 nM，比 SIRT1 和 SIRT2 更有效，IC50 分别为 88 nM 和 92 nM。
Cas No.:120241-79-4
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
3-TYP inhibit SIRT3 with an IC50 of 16 nM, and is more potent over SIRT1 and SIRT2 with IC50 of 88 nM and 92 nM, respectively.[1]
In vitro, with 50 μM 3-TYP abrogated the barrier protective effect of PD in multiple organs of septic mice. In HUVECs, 3-TYP (50 μM) diminished PD-mediated protection against F-actin redistribution, cadherin–catenin complex dissociation, and endothelial monolayer hyperpermeability.[3] In vitro study it demonstrated that at 100 μM, 3-TYP decreased expression of genes involved in lipolysis and glucose transport GLUT4 compared to HNK. At the meantime, 3-TYP also caused an increase in gene expression of adipocyte-specific cytokines, including IL6, resistin, and TNF-α. In vitro, treatment with 100 μM 3-TYP obviously inhibited glucose uptake in 3T3-L1 adipocytes in contrast to control in the presence of insulin.[5] In A/R-treated H9c2 cells, 4-P-PDOT (10 μM) and 3-TYP (5 μM) treatment resulted in no notable difference in cell viability. In addition, combination wiith 4-P-PDOT and 3-TYP elevated apoptotic signaling by increasing cleaved caspase-3 and Bax expression while decreasing Bcl-2 expression compared with that in the A/R + Mel group.[6]
In vivo experiment it suggested that treatment with 50 mgkg intraperitoneally 3-TYP reversed the induction of mitophagy by decreasing the expression levels of FOXO3α, BINP3, LC3-II/LC3-I, SOD2, PRDX3, and P62.[2] In vivo efficacy test it indicated that C57BL/6 mice were administrated 50 mg/kg 3-TYP abolished TBM's antioxidative effects.[4]
References:
[1].Pi H, et al. SIRT3-SOD2-mROS-dependent autophagy in cadmium-induced hepatotoxicity and salvage by melatonin. Autophagy. 2015;11(7):1037-51.
[2].Yu W, et al. Dexmedetomidine Ameliorates Hippocampus Injury and Cognitive Dysfunction Induced by Hepatic Ischemia/Reperfusion by Activating SIRT3-Mediated Mitophagy and Inhibiting Activation of the NLRP3 Inflammasome in Young Rats. Oxid Med Cell Longev. 2020 Nov 20;2020:7385458.
[3].Wu J, et al. Polydatin protects against lipopolysaccharide-induced endothelial barrier disruption via SIRT3 activation. Lab Invest. 2020 Apr;100(4):643-656.
[4].Lv D, et al. Tubeimoside I Ameliorates Myocardial Ischemia-Reperfusion Injury through SIRT3-Dependent Regulation of Oxidative Stress and Apoptosis. Oxid Med Cell Longev. 2021 Nov 9;2021:5577019.
[5]. Lee AY, et al. Sirt3 Pharmacologically Promotes Insulin Sensitivity through PI3/AKT/mTOR and Their Downstream Pathway in Adipocytes. Int J Mol Sci. 2022 Mar 29;23(7):3740.
[6].Wu J, et al. Melatonin Attenuates Anoxia/Reoxygenation Injury by Inhibiting Excessive Mitophagy Through the MT2/SIRT3/FoxO3a Signaling Pathway in H9c2 Cells. Drug Des Devel Ther. 2020 May 25;14:2047-2060.
3-TYP 抑制 SIRT3，IC50 为 16 nM，比 SIRT1 和 SIRT2 更有效，IC50 分别为 88 nM 和 92 nM。[1]
在体外，50 μM 3-TYP 消除了 PD 在脓毒症小鼠多个器官中的屏障保护作用。在 HUVEC 中，3-TYP (50 μM) 降低了 PD 介导的针对肌动蛋白再分布、钙粘蛋白-连环蛋白复合物解离和内皮单层高渗透性的保护作用。[3] 体外研究表明，在 100与 HNK 相比，μM、3-TYP 降低了参与脂肪分解和葡萄糖转运 GLUT4 的基因的表达。同时，3-TYP 还引起脂肪细胞特异性细胞因子的基因表达增加，包括 IL6、抵抗素和 TNF-α。在体外，与胰岛素存在的对照相比，100 μM 3-TYP 处理明显抑制 3T3-L1 脂肪细胞的葡萄糖摄取。[5] 在 A/R 处理的 H9c2 细胞中，4- P-PDOT (10 μM) 和 3-TYP (5 μM) 处理导致细胞活力没有显着差异。此外，与 A/R + Mel 组相比，4-P-PDOT 和 3-TYP 的组合通过增加裂解的 caspase-3 和 Bax 表达同时降低 Bcl-2 表达来提高细胞凋亡信号。[6]
体内实验表明，腹膜内注射 50 mg/kg 3-TYP 通过降低 FOXO3α、BINP3、LC3-II/LC3-I、SOD2、PRDX3 和 P62 的表达水平来逆转线粒体自噬的诱导。 [2] 体内药效试验表明，C57BL/6 小鼠给予 50 mg/kg 3-TYP 可消除 TBM 的抗氧化作用。[4]
| Cell experiment [1]: | |
|
Cell lines |
HepG2 cells |
|
Preparation Method |
HepG2 cells were pretreated with 3-TYP (50 μM) or the vehicle for 1 h, followed by the treatment with DHM (20 μM) for 2 h and 0.2 mM of PA for 16 h. |
|
Reaction Conditions |
50 μM, 16h |
|
Applications |
DHM treatment attenuates PA-induced autophagy arrest and oxidative stress in hepatocytes, which was mediated via SIRT3. |
| Animal experiment [2]: | |
|
Animal models |
C57BL/6 J male mice |
|
Preparation Method |
Both 3-TYP and 2-methoxyestradiol were administered by intraperitoneal injection starting 1 week prior to NE for 7 days 3-TYP was administered at 50 mg/kg/day, and 2-ME was administered at 16 mg/kg/day. |
|
Dosage form |
50 mg/kg/day,i.p. |
|
Applications |
3-TYP exacerbates noise-induced hair cell damage; 3-TYP increases the acetylation level of SOD2 and aggravates oxidative stress and apoptosis. |
|
References: [1]. Huang L, et al. Dihydromyricetin attenuates palmitic acid-induced oxidative stress by promoting autophagy via SIRT3-ATG4B signaling in hepatocytes. Nutr Metab (Lond). 2021 Sep 9;18(1):83. [2].Liang W, et al. Sirtuin-3 Protects Cochlear Hair Cells Against Noise-Induced Damage via the Superoxide Dismutase 2/Reactive Oxygen Species Signaling Pathway. Front Cell Dev Biol. 2021 Nov 18;9:766512. |
|
| Cas No. | 120241-79-4 | SDF | |
| 别名 | 吡啶-3-乙炔 | ||
| Canonical SMILES | C1(C2=CN=NN2)=CC=CN=C1 | ||
| 分子式 | C7H6N4 | 分子量 | 146.15 |
| 溶解度 | DMSO : 100 mg/mL (684.23 mM);Ethanol : 16.67 mg/mL (114.06 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 6.8423 mL | 34.2114 mL | 68.4229 mL |
| 5 mM | 1.3685 mL | 6.8423 mL | 13.6846 mL |
| 10 mM | 0.6842 mL | 3.4211 mL | 6.8423 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet