PACAP (1-27), human, ovine, rat TFA
(Synonyms: PACAP 1-27 TFA) 目录号 : GC38596PACAP (1-27), human, ovine, rat TFA (PACAP 1-27 TFA) 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。
Sample solution is provided at 25 µL, 10mM.
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 IC50s of 3 nM, 2 nM and 5 nM for rat PAC1, rat VPAC1 and human VPAC2, respectively[1].
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[2].
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].
[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.
Cas No. | SDF | ||
别名 | PACAP 1-27 TFA | ||
分子式 | C144H225F3N40O41S | 分子量 | 3261.68 |
溶解度 | Water: 100 mg/mL (30.66 mM) | 储存条件 | Store at -20°C |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
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1 mg | 5 mg | 10 mg | |
1 mM | 0.3066 mL | 1.533 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 |
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给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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