| 产品详情 |
PACAP (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。
|
| 生物活性 |
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 IC 50 s of 3 nM, 2 nM and 5 nM for rat PAC1, rat VPAC1 and human VPAC2, respectively.
|
| 性状 |
Solid
|
| IC50 & Target[1][2] |
IC50: 3 nM (rat PAC1), 2 nM (rat VPAC1), 5 nM (human VPAC2)
|
| 体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
|
| 体内研究(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 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. has not independently confirmed the accuracy of the
|
| 运输条件 |
Room temperature in continental US; may vary elsewhere.
|
| 储存方式 |
Sealed storage, away from moisture and light, under nitrogenPowder -80°C 2 years;-20°C 1 ye
|
| SequenceShortening |
HSDGIFTDSYSRYRKQMAVKKYLAAVL-NH2
|
| Sequence |
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
|
| 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.
|