TCS 401
目录号 : GC12020A selective PTP1B inhibitor
Cas No.:243966-09-8
Sample solution is provided at 25 µL, 10mM.
TCS 401 is a selective inhibitor of protein tyrosine phosphatase 1B (PTP1B).
TCS-401 (0.5, 1, 2 μM) significantly increases the proliferation of RPE cells. TCS-401 significantly increases the expression of cyclin A and cyclin D1 at the concentrations of 1 and 2 μM in a concentration-dependent manner. TCS-401 at concentrations of 0.5, 1, and 2 μM significantly increases phosphorylation of Erk and Akt compared to the control group. The activation of Erk and Akt by TCS-401 is blocked by pretreatment with PD98059 and LY294002, respectively. CS-401 treatment activates the MEK/Erk and PI3K/Akt signaling pathways and induces proliferation, differentiation, and migration in RPE cells[1]. CS-401 dose dependently inhibits the RPTC-Sup-induced reduction of fibronectin and α-SMA. At 1 μM, TCS-401 reverses the levels of fibronectin and α-SMA about onefold and at a dose of 2 μM, TCS-401 brings back fibronectin and α-SMA expression to near normal levels[2].
References:
[1]. Du ZD, et al. Protein tyrosine phosphatase 1B regulates the activity of retinal pigment epithelial cells. Mol Vis. 2015 May 1;21:523-31.
[2]. Ponnusamy M, et al. Necrotic renal epithelial cell inhibits renal interstitial fibroblast activation: role of protein tyrosine phosphatase 1B. Am J Physiol Renal Physiol. 2013 Mar 15;304(6):F698-709.
Cell experiment: | Cell proliferation are examined using MTT assay. The 5×103 cells grown in a 96-well plate for 24 h are partially starved in DMEM/F12 supplemented with 1% FBS for 12 h, and then stimulated with various concentrations of TCS-401 for an additional 24 h. MTT are added to the culture medium, and the cells are incubated for an additional 4 h. The formazan crystals formed are then dissolved by adding dimethyl sulfoxide (100 μL per well). Absorbance at 490 nm are measured using a microplate reader. |
References: [1]. Du ZD, et al. Protein tyrosine phosphatase 1B regulates the activity of retinal pigment epithelial cells. Mol Vis. 2015 May 1;21:523-31. |
Cas No. | 243966-09-8 | SDF | |
化学名 | 2-(carboxyformamido)-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3-carboxylic acid hydrochloride | ||
Canonical SMILES | O=C(C(O)=O)NC1=C(C(O)=O)C2=C(S1)CNCC2.Cl | ||
分子式 | C10H10N2O5S.HCl | 分子量 | 306.72 |
溶解度 | 0.1 M NaOH: 5 mg/ml | 储存条件 | Desiccate at RT |
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。 |
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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 | 3.2603 mL | 16.3015 mL | 32.603 mL |
5 mM | 0.6521 mL | 3.2603 mL | 6.5206 mL |
10 mM | 0.326 mL | 1.6302 mL | 3.2603 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
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- Purity: >98.00%
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