| Bioactivity | PL-017 TFA is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 TFA produces long-lasting, reversible analgesia in rats[1]. |
| Target | IC50: 5.5 nM (125I-FK 33,824 binding to μ site) |
| Invitro | PL-017 TFA has an IC50 of 10000 nM for 125I-DADLE binding to δ site[1]. |
| In Vivo | PL-017 TFA (0.22, 0.45, 0.9 nmol/rat; i.c.v.) has the time of maximum effect of approximately 15 to 30 mm after injection at lower doses and produces analgesia lasting as long as 4 hours with larger doses in male Sprague-Dawley rats weighing 250 to 375 g[1]. |
| Name | PL-017 TFA |
| Shortening | YP-{N(Me)Phe}-P-NH2 |
| Formula | C31H38F3N5O7 |
| Molar Mass | 649.66 |
| 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]. K J Chang, et al. Potent morphiceptin analogs: structure activity relationships and morphine-like activities. J Pharmacol Exp Ther. 1983 Nov;227(2):403-8. |