PTP1B-IN-3

目录号: PL09538
PTP1B-IN-3 是有效的,有选择性的 PTP1B 抑制剂,对 PTP1B 和 TCPTP 的 IC50 值均为 120 nM。PTP1B-IN-3 具有抗糖尿病和抗癌作用。
CAS No. :809272-64-8
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中文名称
PTP1B-IN-3
中文别名
P-[(3-溴-7-氰基-2-萘)二氟甲基]磷酸
英文名称
PTP1B-IN-3
英文别名
Phosphonic acid, [(3-bromo-7-cyano-2-naphthalenyl)difluoromethyl]-;P-[(3-Bromo-7-cyano-2-naphthalenyl)difluoromethyl]phosphonic Acid Diammonium Salt;[(3-bromo-7-cyano-2-naphthyl)-(difluoro)methyl]phosphonic acid;P-[(3-Bromo-7-cyano-2-naphthalenyl)difluoromethyl]phosphonic Acid;PHOSPHONIC ACID, [(3-BROMO-7-CYANO-2-NAPHTHALENYL)DIFLUOROMETHYL]- (9CI);PTP1B-IN-3;[(3-bromo-7-cyano-2-naphthalenyl)-difluoromethyl]phosphonic acid;BWJOQFMMTKEZGA-UHFFFAOYSA-N;BDBM50239833;Q27166757;[(3-bromo-7-cyano-2-naphthyl)(difluoro)methyl]phosphonic acid;(3-bromo-7-cyanonaphthalen-2-yl)difluoromethylphosphonic acid
Cas No.
809272-64-8
分子式
C12H7BrF2NO3P
分子量
362.06
包装储存
Please store the product under the recommended conditions in the Certificate of Analysis.
详情描述
PTP1B-IN-3 是有效的,有选择性的 PTP1B 抑制剂,对 PTP1B 和 TCPTP 的 IC50 值均为 120 nM。PTP1B-IN-3 具有抗糖尿病和抗癌作用。
产品详情
PTP1B-IN-3 是有效的,有选择性的 PTP1B 抑制剂,对 PTP1B 和 TCPTP 的 IC50 值均为 120 nM。PTP1B-IN-3 具有抗糖尿病和抗癌作用。
生物活性
PTP1B-IN-3 is a potent and orally active PTP1B inhibitor with IC 50 s of 120 nM for both PTP1B and TCPTP. PTP1B-IN-3 has antidiabetic and anticancer effects.
IC50 & Target[1][2]
IC50: 120 nM (PTP1B), 120 nM (TCPTP)
体内研究(In Vivo)
In diet-induced obese (DIO) mice, PTP1B-IN-3 (compounds 3g) exhibits dose dependent inhibition (60%, 80% and 100% inhibition at 1, 3 and 10 mg/kg, respectively) of glucose excursion when given orally 2 h before oral glucose challenge with an estimated ED 50 of 0.8 mg/kg.
In the NDL2 Ptpn1 transgenic mice, PTP1B-IN-3 (compounds 3g; orally; 30 mg/kg for 21 days) shows a significant delay in the onset of tumor development in NDL2 Ptpn1 mice, extending the median tumor free days (T50) from 28 days to 75 days.
In diet-induced obese (DIO) mice, PTP1B-IN-3 (compounds 3g) exhibits good oral bioavailability (F of 24%), slow clearance (CL of 0.71 mL/kg/min), and good elimination half live (t 1/2 of 6 h).
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献
[1]. Yongxin Han, et al. Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3200-5.
[2]. Patel D, .Discovery of orally active, potent, and selective benzotriazole-based PTP1B inhibitors. ChemMedChem. 2011 Jun 6; 6(6):1011-6.
搜索质检报告(COA)
[1]. Yongxin Han, et al. Discovery of [(3-bromo-7-cyano-2-naphthyl)(difluoro)methyl]phosphonic acid, a potent and orally active small molecule PTP1B inhibitor. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3200-5.
[2]. Patel D, .Discovery of orally active, potent, and selective benzotriazole-based PTP1B inhibitors. ChemMedChem. 2011 Jun 6; 6(6):1011-6.

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