Bioactivity | PROTAC PIPIB degrader 1 (compound 75) is a CRBN-based PTP1B PROTAC degrader, with DC50 values of 0.2 μM (48 h) and 0.05 μM (72 h) (Red: PTP1B ligand Oleanolic acid (HY-N0156); Black: linker; Blue: CRBN ligand)[1]. |
In Vivo | PROTAC PIPIB degrader 1 (compound 75) 在口服葡萄糖耐量试验中将血糖 AUC0–2h 降低至29%,并在 HepG2 细胞中激活 IRS-1/PI3K/Akt 信号通路,显示出长期抗糖尿病的良好前景[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
Formula | C61H92N4O11 |
Molar Mass | 1057.40 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Zunhua Yang, et al. Discovery of Selective Proteolysis-Targeting Chimera Degraders Targeting PTP1B as Long-Term Hypoglycemic Agents. J Med Chem. 2024 May 9;67(9):7569-7584. |