PACAP (6-38), human, ovine, rat TFA
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 4138.76 |
| Molecular Formula | C184H301N56FO47S |
| SMILES | - |
Summary
PACAP (6-38), human, ovine, rat TFA is a potent PACAP receptor antagonist with IC 50 s of 30, 600, and 40 nM for PACAP type I receptor , PACAP type II receptor VIP 1 , and PACAP type II receptor VIP 2 , respectively.
IC50 & Target
IC50: 30 nM (PACAP type I receptor), 600 nM (PACAP type II receptor VIP 1 ), 40 nM (PACAP type II receptor VIP 2 ) [1]
In Vitro
An increase of dopamine (DA) content by HPLC analysis and/or cell proliferation identified by MTT assay by Dexamethasone (DEX) is also observed which can be inhibited by PACAP (6-38) at concentration sufficient to block PACAP type 1 (PAC1) receptor. Pretreatment with PAC1 receptor antagonist PACAP (6-38) at 0.1 or 1 μM for 2 h significantly blocks this increase of DA content by 1 μM DEX. The MTT assay shows that DEX increases cell proliferation. Moreover, this action is also inhibited by the pre-incubation of PACAP (6-38). PACAP (6-38) at 1μM shows no effect on DA content and cell proliferation for 24 h. However, PACAP (6-38) at 0.3 μM has been mentioned to reduce the spontaneous tyrosine hydroxylase (TH) accumulation in differentiated retinal cultured cells for 5 days [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Intravesical administration of the PAC1 receptor antagonist, PACAP (6-38), significantly increases intercontraction interval (2.0-fold) and void volume (2.5-fold) in NGF-OE mice. Intravesical instillation of PACAP (6-38) also decreases baseline bladder pressure in NGF-OE mice. Intravesical administration of PACAP (6-38) (300 nM) significantly (p≤0.01) reduces pelvic sensitivity in NGF-OE mice but is without effect in WT mice [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
| Powder | -80°C | 2 years |
|---|---|---|
| -20°C | 1 year |
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL ( 24.16 mM ; Need ultrasonic)
H 2 O : 50 mg/mL ( 12.08 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 0.2416 mL | 1.2081 mL | 2.4162 mL |
| 5 mM | 0.0483 mL | 0.2416 mL | 0.4832 mL |
| 10 mM | 0.0242 mL | 0.1208 mL | 0.2416 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (24.16 mM); Clear solution; Need ultrasonic
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (0.60 mM); Clear solution
-
3.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (0.60 mM); Clear solution
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] Yang TT, et al. Changes of dopamine content and cell proliferation by dexamethsone via pituitary adenylate cyclase-activating polypeptide in PC12 cell. Neurosci Lett. 2007 Oct 9;426(1):45-8.
- [3] Girard BM, et al. Intravesical PAC1 Receptor Antagonist, PACAP(6-38), Reduces Urinary Bladder Frequency and Pelvic Sensitivity in NGF-OE Mice. J Mol Neurosci. 2016 Jun;59(2):290-9.