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1919853-46-5

中文名稱(chēng) 1919853-46-5
英文名稱(chēng) PTP1B-IN-2
CAS 1919853-46-5
分子式 C34H36N2O9S2
分子量 680.79
MOL 文件 1919853-46-5.mol
更新日期 2023/03/20 15:41:27
1919853-46-5 結(jié)構(gòu)式 1919853-46-5 結(jié)構(gòu)式

基本信息

中文別名
化合物PTP1B-IN-2
5-(N-(4-(N-(2-甲氧基-2-氧代乙基)甲基磺酰氨基)芐基)-1-苯基甲基磺酰氨基)-2-((4-甲基芐基)氧基)苯甲酸甲酯
英文別名
MDK3465
PTP1B-IN-2
PTP1B inhibitor 2
PTP1B-IN-2
PTP1B INHIBITOR 2

物理化學(xué)性質(zhì)

沸點(diǎn)813.4±75.0 °C(Predicted)
密度1.350±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMF: 10 mg/ml; DMSO: 10 mg/ml; Ethanol: insol; PBS (pH 7.2): insol
酸度系數(shù)(pKa)-3.81±0.50(Predicted)
形態(tài)固體
顏色White to off-white
1919853-46-5價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱(chēng)CAS號(hào)包裝價(jià)格
2024/11/08HY-1004621919853-46-5
PTP1B-IN-2
1919853-46-51mg681元
2024/11/08HY-1004621919853-46-5
PTP1B-IN-2
1919853-46-55mg1200元
2024/11/08HY-1004621919853-46-5
PTP1B-IN-2
1919853-46-510mg1700元

常見(jiàn)問(wèn)題列表

生物活性
PTP1B-IN-2 (MDK3465, Ptp1B-In-2, Compound P6)是一種有效的、選擇性的 protein tyrosine phosphatase-1B (PTP1B) 抑制劑,其IC50值為50 nM。PTP1B-IN-2 可增強(qiáng)胰島素介導(dǎo)的胰島素受體β(IRβ)磷酸化,以及胰島素刺激的葡萄糖的攝取。
靶點(diǎn)
TargetValue
PTP1B
(Cell-free assay)
50 nM
體外研究

PTP1B-IN-2 displays more than 40-fold selectivity for PTP1B over SHP-2 and LAR and 15-fold higher selectivity for PTP1B over the highly homologous TCPTP. PTP1B-IN-2 extends deep into the active site pocket, forming several hydrogen bonds and hydrophobic interactions with key residues of the catalytic site. The binding characteristics between PTP1B domain and ligand shows that PTP1B-IN-2 is an ABC type inhibitor which not only interacted with catalytic site but also B site and C site. PTP1B-IN-2 greatly enhances insulin-mediated IRβ phosphorylation at concentrations of 15 μM and 30 μM. Insulin-stimulated glucose uptake is also significantly increased in L6 myotubes treated with PTP1B-IN-2, and this increase is 16.0%, 19.0% and 38.1% at 5, 10 and 20 μM, respectively .

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