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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
PACAP-1-38
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
137061-48-4
- 规格：
5mg/1mg/500μg
| 规格： | 5mg | 产品价格： | ￥4790.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥1590.0 |
| 规格： | 500μg | 产品价格： | ￥1190.0 |
H-Gly-Gly-Pro-OH 是由 3 个氨基酸构成的多肽。
| 基本信息 | |
| CAS | No.137061-48-4 |
| 英文名称 | PACAP-1-38 |
| 别名 | PituitaryAdenylateCyclaseActivatingPolypeptide38 |
| 分子式 | C203H331N63O53S |
| 分子量 | 4534.26 |
| 溶解性 | Soluble in Water |
| 纯度 | ≥96% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00081800 |
| SMILES | --- |
| 靶点 | PACAP receptor |
| 通路 | Others |
| 背景说明 | H-Gly-Gly-Pro-OH 是由 3 个氨基酸构成的多肽。 |
| 生物活性 | PACAP (1-38), human, ovine, rat is a neuropeptide with 38 amino acid residues. PACAP (1-38) binds to PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2 with IC50s of 4 nM, 2 nM, and 1 nM, respectively.[1-4] |
| IC50 | 4nM(PACAP type I receptor);2nM(PACAP type II receptor VIP1);1nM(PACAP type II receptor VIP2)[1] |
| In Vitro | PACAP(1-38)，human，ovine，rat is a fragment of pituitary adenylate cyclase activating polypeptide[1]. PACAP(1-38)shows high affinity for PACAP specific(PAC1)receptor in membranes from various tissues including the endocrine pancreas[2]. In vitro，PACAP(1-38)relaxes guinea-pig and rabbit tracheal smooth muscle precontracted by histamine and by acetylcholine. PACAP(1-38)also increases adenosine 3':5'-cyclic monophosphate(cyclic AMP)in tracheal smooth muscle，providing a possible mechanism for the relaxant effect of PACAP(1-38)[3]. |
| 细胞实验 | PACAP(1-38)alone in sham animals does not result in changes in any of the retinal layers. PACAP(1-38)dissolved in solutio ophthalmica cum benzalkonio leads to significant protection in the retina in bilateral common carotid artery occlusion(BCCAO)-lesioned retinas; retinas treated with PACAP(1-38)eye drops have preserved structure compared to control retinas. OLM-ILM(outer limiting membrane-inner limiting membrane)distance is reduced by 49.7%(p<0.001)in BCCAO retinas compared to sham controls，but it is only 40.6%(p<0.001)in the eyes treated with PACAP(1-38)eye drops. A protection to a similar degree is found in the inner nuclear layer(INL)(BCCAO: 38.5%，PACAP(1-38): 30.5%; p<0.001)，and inner plexiform layer(IPL)(BCCAO: 64.8%，PACAP(1-38): 38.2%; p<0.05)，while no statistically significant attenuation of the damage is observed in the outer nuclear layer(ONL)(BCCAO: 36.5%，PACAP(1-38): 37.7%)or outer plexiform layer(OPL)(BCCAO: 53.0%，PACAP(1-38): 48.2%). The number of cells in the ganglion cell layer(GCL)is significantly decreased after BCCAO by 52.4%(p<0.05)and is significantly ameliorated by PACAP(1-38)eye drops(decreased by 25.9%; p<0.05)[4]. |
| 动物实验 | Wistar rats(n=20:n=12 for histological analysis，n=8 for immunohistochemical analysis)weighing 250-300 are fed and watered ad libitum，under light/dark cycles of 12/12 h. Directly after the operation within 1 min，the right eye is treated with PACAP(1-38)eye drops(1 μg/drop). The vehicle used is benzalkonium-chloride in a concentration of 0.005%，as it is the most effective vehicle to achieve neuroprotection with PACAP1-27 eye drops. The left eye serves as a control，treated only with the vehicle. A group of animals serve as the sham-operated group that undergo anesthesia and all steps of the surgical procedure except ligation of the carotid arteries. Rats are treated twice a day with one drop，for 5 consecutive days[4]. |
| 数据来源文献 | [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]. Yamaguchi N. Pituitary adenylate cyclase activating polypeptide enhances glucose-evoked insulin secretion in the canine pancreas in vivo. JOP. 2001 Sep;2(5):306-16. [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. [4]. Werling D， et al. Passage through the Ocular Barriers and Beneficial Effects in Retinal Ischemia of Topical Application of PACAP (1-38) in Rodents. Int J Mol Sci. 2017 Mar 21;18(3). pii: E675. |
| 单位 | 瓶 |
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2 是一种用以表示竞争性拮抗剂作用强度的指标，其意义是能使激动剂提高到原来的 2 倍时，可产生与原来浓度相同效应所需的拮抗剂克分子浓度的负对数 (-log(B)) 。 PA2 的值越大说明拮抗剂的作用越强。 pA2 是拮抗参数 (antagonism parameter) ：当有一定浓度的拮抗药存在时，激动剂增加 2 倍时才能达到原来效应，此时拮抗药的负对数即拮抗参数， pA2 = -log[I] = -logKI 3 、药物作用
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