| CAS | 2243219-86-3 |
| Sequence | Myristoyl-His-Ser-Asp-Ala-Val-Phe-Thr-Asp-Asn-Tyr-Thr-Lys-Leu-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys-Tyr-Leu-Asn-Ser-Ile-Lys-Lys-Gly-Gly-Thr-OH |
| Sequence Single | Myristoyl-HSDAVFTDNYTKLRKQMAVKKYLNSIKKGGT |
| Molecular Formula | C171H283N45O47S |
| Molecular Weight | 3753.47 |
| Synonyms | Myristoyl-(Lys12.27.28)-VIP-Gly-Gly-Thr (free acid) |
| Technology | Synthetic |
| Storage | -20°C, avoid light, cool and dry place |
| Application | Cancer Research |
| Description | PG 99-465 also called Myristoyl-(Lys12.27.28)-VIP-Gly-Gly-Thr (free acid), is a high affinity, selective VPAC2 receptor antagonist. It exhibited a 100-fold preference for the VPAC2 over the VPAC1 receptor. The compound showed partial agonistic activity on the VPAC1 receptor and was inactive on the VPAC2 receptor transfected in CHO cells, as well as on naturally expressed human VPAC2 receptors in the SUP T1 cell line. Dickson et al. observed an agonistic effect of PG99-465 on the human VPAC1 and PAC1 receptors. When applied singly, PG99-465 increased [cAMP](i) at all three hVPAC/PAC receptor subtypes. |
| References | 1. A new Antennapedia-derived vector for intracellular delivery of exogenous compounds. C.Garcia-Echeverria et al., Bioorg. Med. Chem. Lett., 11, 1363 (2001) 2. The mouse VPAC2 receptor confers suprachiasmatic nuclei cellular rhythmicity and responsiveness to vasoactive intestinal polypeptide in vitro. D.J.Cutler et al., Eur. J. Neurosci., 17, 197 (2003) 3. Identification and characterization of a small molecule antagonist of human VPAC(2) receptor. A.Chu et al., Mol. Pharmacol., 77, 95 (2010) 4. Effects of vasoactive intestinal polypeptide on neurones of the rat suprachiasmatic nuclei in vitro. H.E.Reed et al., J. Neuroendocrinol., 14, 639 (2002) 5. Development of selective agonists and antagonists for the human vasoactive intestinal polypeptide VPAC(2) receptor. D.Moreno et al., Peptides, 21, 1543 (2000) 6. VIP enhances synaptic transmission to hippocampal CA1 pyramidal cells through activation of both VPAC1 and VPAC2 receptors. D.Cunha-Reis et al., Brain Res., 1049, 52 (2005) 7. Inhibitory pathways in the circular muscle of rat jejunum. G.Vanneste et al., Br. J. Pharmacol., 143, 107 (2004) |