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127317-03-7

127317-03-7 structure

Name: PACAP-27 (human, mouse, ovine, porcine, rat) trifluoroacetate salt
Chemical Name: L-Histidyl-L-seryl-L-α-aspartylglycyl-L-isoleucyl-L-phenylalanyl-L-threonyl-L-α-aspartyl-L-seryl-L-tyrosyl-L-seryl-L-arginyl-L-tyrosyl-L-arginyl-L-lysyl-L-glutaminyl-L-methionyl-L-alanyl-L-valyl-L-lysyl-L-lysyl-L-tyrosyl-L-leucyl-L-alanyl-L-alanyl-L-valyl-L-leucinamide
CAS Number: 127317-03-7
Molecular Formula: C₁₄₂H₂₂₄N₄₀O₃₉S
Molecular Weight: 3147.608
Catalog: Biochemical Peptide
Create Date: 2018-03-26 08:00:00
Modify Date: 2024-01-02 15:08:25
PACAP (1-27), human, ovine, rat, the N-terminal fragment of PACAP-38, is a potent PACAP receptor antagonist with IC50s of 3, 2, and 5 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2.

Name	L-Histidyl-L-seryl-L-α-aspartylglycyl-L-isoleucyl-L-phenylalanyl-L-threonyl-L-α-aspartyl-L-seryl-L-tyrosyl-L-seryl-L-arginyl-L-tyrosyl-L-arginyl-L-lysyl-L-glutaminyl-L-methionyl-L-alanyl-L-valyl-L-lysyl-L-lysyl-L-tyrosyl-L-leucyl-L-alanyl-L-alanyl-L-valyl-L-leucinamide
Synonyms	MFCD00167418 L-Leucinamide, L-histidyl-L-seryl-L-α-aspartylglycyl-L-isoleucyl-L-phenylalanyl-L-threonyl-L-α-aspartyl-L-seryl-L-tyrosyl-L-seryl-L-arginyl-L-tyrosyl-L-arginyl-L-lysyl-L-glutaminyl-L-methionyl -L-alanyl-L-valyl-L-lysyl-L-lysyl-L-tyrosyl-L-leucyl-L-alanyl-L-alanyl-L-valyl- ADENYLATE CYCLASE ACTIVATING PEPTIDE-27 L-Histidyl-L-seryl-L-α-aspartylglycyl-L-isoleucyl-L-phenylalanyl-L-threonyl-L-α-aspartyl-L-seryl-L-tyrosyl-L-seryl-L-arginyl-L-tyrosyl-L-arginyl-L-lysyl-L-glutaminyl-L-methionyl-L-alanyl-L-val yl-L-lysyl-L-lysyl-L-tyrosyl-L-leucyl-L-alanyl-L-alanyl-L-valyl-L-leucinamide Talopram hydrochloride PACAP (1-27), human, ovine, rat

Description	PACAP (1-27), human, ovine, rat, the N-terminal fragment of PACAP-38, is a potent PACAP receptor antagonist with IC50s of 3, 2, and 5 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2.
Related Catalog	Signaling Pathways >> Others >> Others Research Areas >> Metabolic Disease Research Areas >> Neurological Disease Peptides
Target	IC50: 3 nM (rat PAC1), 2 nM (rat VPAC1), 5 nM (human VPAC2)[1]
In Vitro	The PACAP type I and II receptors recognize PACAP-27 and PACAP-38 with an equal high affinity[1]. PACAP(1-27) exhibits a distinct and much higher susceptibility to VIP-amino acid substitutions, compared to PACAP (1-38). Positions 4 and 5 seem to be most important for receptor binding of PACAP (1-27), whereas position 13 is identified to be crucial for maximal affinity of PACAP (1-38)[2].
In Vivo	PACAP (1-27) produces significant bronchodilatation and rapid onset of sustained action and without pronounced cardiovascular side effects. This peptide may have therapeutic potential as a bronchodilator[3]. PACAP(1-27) (0.005-5 μg) increases the basal insulin secretion by about 15 folds in a dose-dependent manner. Local infusion of either glucose (5%) or PACAP(1-27) (0.05 μg) results in a significant increase in the basal insulin output to about 300 μUx per min per g. PACAP(1-27) directly enhances the glucose-evoked insulin secretion in the endocrine pancreas in anesthetized dogs. The study suggests that PACAP may play a local facilitating role in insulin secretion in response to glucose loading[4].
Animal Admin	Guinea-pigs[3] PACAP-27 (0.045 to 4.5 nmol/kg/min), salbutamol (0.045 to 4.5 nmol/kg/min) or sterile saline is given i.v. (1.0 mL) via an infusion pump, starting 5 min before and continuing 10 min after airway challenge[3]. Dogs[4] Four dogs (28.4±1.8 kg) receive PACAP (1-27) with four different concentrations of 0.01, 0.1, 1.0 and 10 µg/mL, or 0.00318, 0.0318, 0.318 and 3.18 µM, respectively. Each solution is locally infused at a rate of 0.5 mL/min for precisely 1 min. A total dose delivered to the pancreas during each infusion is therefore 0.005, 0.05, 0.5 and 5 µg. The dead volume of the pancreatic arterial catheter (0.5 mL) is taken into account in relation to the infusion rate. After taking the initial control sample, simultaneously from the SPD vein and the aorta, saline is infused for 1 min and samples are obtained 1, 3 and 5 min after the onset of infusion. This procedure is repeated every 15 min for the doses of PACAP (1-27). The sample obtained at 15 min after the onset of each infusion served as control for the subsequent intervention[4].
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. [4]. Yamaguchi N, et al. Pituitary adenylate cyclase activating polypeptide enhances glucose-evoked insulin secretion in the canine pancreas in vivo. JOP. 2001 Sep;2(5):306-16.

Density	1.5±0.1 g/cm3
Molecular Formula	C₁₄₂H₂₂₄N₄₀O₃₉S
Molecular Weight	3147.608
Exact Mass	3145.649414
PSA	1340.85000
LogP	-3.65
Appearance	solid \| white
Index of Refraction	1.657
Storage condition	−20°C

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