PACAP (1-27), human, ovine, rat TFA
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 3261.68 |
| Molecular Formula | C144H225F3N40O41S |
| SMILES | - |
1 Publications Citing Use of MCE
Summary
PACAP (1-27), human, ovine, rat TFA (PACAP 1-27 TFA) is the N-terminal fragment of PACAP-38, and is a potent PACAP receptor antagonist with IC 50 s of 3 nM, 2 nM and 5 nM for rat PAC1 , rat VPAC1 and human VPAC2 , respectively [1] .
IC50 & Target
IC50: 3 nM (rat PAC1), 2 nM (rat VPAC1), 5 nM (human VPAC2) [1]
In Vitro
Radioligand receptor binding assays with I-monoiodinated PACAP (1-27), human, ovine, rat confirms the presence of PAC -receptors on AR4-2J cells, since PACAP (1-27), human, ovine, rat and PACAP(1–38) equipotently displaces radioligand binding with a K d of 1-2 nM, whereas vasoactive intestinal peptide (VIP) is 1000-fold less potent. PACAP (1-27), human, ovine, rat exhibits a distinct and much higher susceptibility to VIP-amino acid substitutions. PACAP (1-27), human, ovine, rat has potency and binding affinity to stimulate IP3 and cAMP formation in AR4-2J cells [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
The inhibitory effect of pituitary adenylate cyclase activating polypeptide (PACAP (1-27), human, ovine, rat) on the increase in total pulmonary resistance (RL) causes either by allergen or histamine in anaesthetized, ventilated guinea-pigs is studied. PACAP (1-27), human, ovine, rat given via i.v. infusion (0.045-4.5 nmol/kg/min) dose-dependently reduces the increase in RL caused by inhaled ovalbumin and histamine. At the highest dose, PACAP (1-27), human, ovine, rat prevents the increase in RL caused by ovalbumin and histamine completely. Infusion of PACAP (1-27), human, ovine, rat and the β2-adrenoceptor agonist, salbutamol (0.045-4.5 nmol/kg/min) inhibit the increase in RL similarly, but salbutamol increases the heart rate more than PACAP (1-27), human, ovine, rat [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Sealed storage, away from moisture and light, under nitrogen
| Powder | -80°C | 2 years |
|---|---|---|
| -20°C | 1 year |
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)
Solvent & Solubility
DMSO : 250 mg/mL ( 76.65 mM ; Need ultrasonic)
H 2 O : 100 mg/mL ( 30.66 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 0.3066 mL | 1.5330 mL | 3.0659 mL |
| 5 mM | 0.0613 mL | 0.3066 mL | 0.6132 mL |
| 10 mM | 0.0307 mL | 0.1533 mL | 0.3066 mL |
References
- [1] Gourlet P, et al. Fragments of pituitary adenylate cyclase activating polypeptide discriminate between type I and II recombinant receptors. Eur J Pharmacol. 1995 Dec 4;287(1):7-11.
- [2] Schäfer H, et al. Structural motifs of pituitary adenylate cyclase-activating polypeptide (PACAP) defining PAC1-receptor selectivity. Regul Pept. 1999 Feb 5;79(2-3):83-92.
- [3] Lindén A, et al. Inhibition of bronchoconstriction by pituitary adenylate cyclase activating polypeptide (PACAP 1-27) in guinea-pigs in vivo. Br J Pharmacol. 1995 Jul;115(6):913-6.