PACAP 6-38 |
| Catalog No.GC10061 |
PACAP 6-38 est un puissant antagoniste des récepteurs PACAP avec des IC50 de 30, 600 et 40 nM pour le récepteur PACAP de type I, le récepteur PACAP de type II VIP1 et le récepteur PACAP de type II VIP2, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 143748-18-9
Sample solution is provided at 25 µL, 10mM.
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PACAP (6-38), human, ovine, rat is a potent PACAP receptor antagonist with IC50s of 30, 600, and 40 nM for PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2, respectively.
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].
Intravesical administration of the PAC1 receptor antagonist, PACAP (6-38) (300 nM), significantly (p≤0.01) 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].
Reference:
[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.
Cell experiment: | PC12 cells (5×104 cells per well) are deposited in a 96-well flat-bottom culture plate. Cells are incubated with PACAP(6-38) (0.1 and 1.0 μM) for 2 h before the addition of Dexamethasone (DEX, 1 μM). Cells are harvested at 24 h later of treatment. At regular intervals after the additional treatments, 100 μL of 0.2 mg/mL MTT is added per each well, and cells are incubated for 3 h at 37°C. After incubation, the MTT reagent is discarded, and 100 μL of DMSO is then added. The experiment is performed at room temperature for 20 min. The absorbance is then measured with SPECTRA max 340PC ELISA reader at the wavelength of 570 nm[2]. |
Animal experiment: | Mice[3]Two groups of mice are evaluated: WT mice receiving intravesical administration of vehicle (0.9% saline) and PACAP (6-38) (300 nM) (n=8) and NGF-OE mice receiving intravesical administration of vehicle (0.9% saline) and PACAP (6-38) (300 nM) (n=8). For intravesical administration of PACAP (6-38), mice are anesthetized with 2% isoflurane and PACAP (6-38) (<1.0 mL) is injected through the bladder catheter; the animals are maintained under anesthesia to prevent expulsion of PACAP (6-38) via a voiding reflex. In this procedure, PACAP (6-38) remains in the bladder for 30 min at which time, the drug is drained, the bladder washed with saline and animals recover from anesthesia for 20 min before experimentation[3]. |
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. | |
| Cas No. | 143748-18-9 | SDF | |
| Formula | C182H300N56O45S | M.Wt | 4024.78 |
| Solubility | Soluble to 2 mg/ml in sterile water | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 248.5 μL | 1.2423 mL | 2.4846 mL |
| 5 mM | 49.7 μL | 248.5 μL | 496.9 μL |
| 10 mM | 24.8 μL | 124.2 μL | 248.5 μL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)
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