Table 5.
Sequences of KP1–5 and their reported biological properties [78].
| Comp. | Sequence | Stability after 6 h [%] b,c | EC50 [nM] d |
|---|---|---|---|
| KP1 a | Tyr-Asn-Trp-Asn-Ser-Phe-Gly-Leu-Arg-Tyr-NH2 | n.d. | 2.5 ± 2.2 |
| KP2 | Ac-Tyr-Asn-Trp-Asn-Ser-Phe-Gly-Leu-Arg-Tyr-NH2 | 2.6 ± 0.4 | 0.07 ± 0.06 |
| KP3 | Ac-Tyr-Asn-Trp-Asn-Ser-Phe-GlyΨ[Tz]Leu-Arg-Tyr-NH2 | 40.8 ± 2.9 | 0.07 ± 0.06 |
| KP4 | Ac-Tyr-Asn-Trp-Asn-Ser-PheΨ[Tz]Gly-Leu-Arg-Tyr-NH2 | 61.4 ± 6.4 | 0.6 ± 0.05 |
| KP5 | Ac-Tyr-Asn-Trp-Asn-Ser-PheΨ[Tz]GlyΨ[Tz]Leu-Arg-Tyr-NH2 | 50.7 ± 3.2 | 120 ± 87 |
a Reference compound. b Determined in blood serum at 39 °C. c n.d.: not detectable d Determined by a calcium mobilization assay on HEK-293 cells transfected with KISS1R.