Bioactivity | NPFF1-R antagonist 1 (compound 8b), a piperidine analogue, is a potent neuropeptide FF (NPFF) receptor antagonist. NPFF1-R antagonist 1 is 15-fold selective for the NPFF1-R subtype, with Ki values of 211 nM and 3270 nM for NPFF1-R and NPFF2-R, respectively[1]. |
Invitro | NPFF1-R antagonist 1 (compound 8b) 在阿片受体(DOR、KOR 和 MOR)上表现出一定的脱靶结合,Ki 值分别为 1540 ± 132、1390 ± 147 和 3560 ± 364 nM[1]。NPFF1-R antagonist 1 (0-10 μM) 无法抑制 cAMP 刺激,以剂量依赖性方式逆转 NPFF 对毛喉素 (HY-15371) 诱导的 cAMP 积累的抑制[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> NPFF1-R antagonist 1 相关抗体: |
Formula | C37H44N4O |
Molar Mass | 560.77 |
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]. Galal KA, et al. Guanidine-to-piperidine switch affords high affinity small molecule NPFF ligands with preference for NPFF1-R and NPFF2-R subtypes. Eur J Med Chem. 2024 Apr 5;269:116330. |