Biological Activity
Potent and competitive pituitary adenylate cyclase-activating polypeptide receptor (PAC)1 antagonist (IC50 = 2 nM). Inhibits PACAP(1-27)-induced stimulation of adenylate cyclase (Ki = 1.5 nM). Antitumor activity in vivo.
Technical Data
| M. Wt | 4024.78 |
| Formula | C182H300N56O45S |
| Sequence |
FTDSYSRYRKQMAVKKYLAAVLGKRYKQRVKNK (Modifications: Lys-33 = C-terminal amide) |
| Storage | Desiccate at -20°C |
| CAS Number | 143748-18-9 |
| PubChem ID | 24868185 |
| InChI Key | BGZYREVJBMQLGS-ONKNJJKASA-N |
| Smiles | [H]N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(N)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 2 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 4024.78. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.25 mL | 1.24 mL | 2.48 mL |
| 5 mM | 0.05 mL | 0.25 mL | 0.5 mL |
| 10 mM | 0.02 mL | 0.12 mL | 0.25 mL |
| 50 mM | 0 mL | 0.02 mL | 0.05 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Robberecht et al (1992) Structural requirements for the occupancy of pituitary adenylate-cyclase-activating-peptide (PACAP) receptors and adenylate cyclase activation in human neuroblastoma NB-OK-1 cell membranes. Discovery of PACAP(6-38) as a potent antagonist. Eur.J.Biochem. 207 239 PMID: 1321043
Leyton et al (1998) PACAP(6-38) inhibits growth of prostate cancer cells. Cancer Lett. 125 131 PMID: 9566707
Kojro et al (2006) The neuropeptide PACAP promotes a-secretase pathway for processing Alzheimer amyloid precursor protein. FASEB J. 20 512 PMID: 16401644
Keywords: PACAP 6-38, supplier, Potent, PAC1, receptors, antagonists, Pituitary, Adenylate, Cyclase, Activating, Peptide, PACAP638, PACAP, Receptors, PACAP, Receptors, Tocris Bioscience
