产品类型 |
多肽 |
CAS |
No.127317-03-7 |
单字母序列 |
HSDGIFTDSYSRYRKQMAVKKYLAAVL-NH2 |
三字母序列 |
His-Ser-Asp-Gly-Ile-Phe-Thr-Asp-Ser-Tyr-Ser-Arg-Tyr-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys-Tyr-Leu-Ala-Ala-Val-Leu-NH2 |
别名 |
PACAP 1-27 |
分子式 |
C142H224N40O39S1 |
分子量 |
3147.66 |
纯度 |
≥95% |
外观(性状) |
冻干粉;Lyophilized powder |
溶解性 |
DMSO:100 mg/mL; *超声助溶; |
盐体系 |
TFA盐;Trifluoroacetate salt |
来源 |
合成;Synthetic |
储存条件 |
Store at -20℃,2 years.(Avoid freeze/thaw cycles) |
背景说明 |
PACAP (1-27), human, ovine, rat (PACAP 1-27) 是 PACAP-38 的 N-末端片段,是一种有效的 PACAP 受体拮抗剂,对大鼠 PAC1,大鼠 VPAC1 和人 VPAC2 的 IC50 值分别为 3 nM,2 nM 和 5 nM。 |
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 prevented 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. |
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 Kd 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. |
参考文献 |
[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]. Sch fer 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. |
研究领域 |
神经科学研究 |
规格 |
1mg 5mg 10mg |
单位 |
瓶 |
分类属性 |
目录肽 |