标签归档：pacap

神经垂体素

发表于由

神经垂体素

货号：
IP3110

品牌：
Jinpan

神经垂体素

暂无详情
产品简介
有效期 2年
MDL MFCD00167418
别名 尿崩停；垂体后叶粉；垂体腺苷环化酶激活肽
英文名称 PACAP-1-27
CAS 127317-03-7
分子式 C142H224N40O39S
分子量 3147.61
储存条件 2-8°C
纯度 ≥98%
外观（性状） White Powder
单位 瓶
生物活性 PACAP (1-27), human, ovine, rat 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3，2和5 nM。[1-4]
IC50 3 nM (rat PAC1), 2 nM (rat VPAC1), 5 nM (human VPAC2)[1]
In Vitro PACAP I型和II型受体以相同的高亲和力识别PACAP-27和PACAP-38 [1]。与PACAP（1-38）相比，PACAP（1-27）对VIP-氨基酸取代具有明显且更高的易感性。位置4和5似乎对PACAP的受体结合最重要（1-27），而位置13被鉴定为对PACAP（1-38）的最大亲和力至关重要[2]。
In Vivo PACAP（1-27）产生显著的支气管扩张和持续作用的快速起效，并且没有明显的心血管副作用。该肽可能具有作为支气管扩张剂的治疗潜力[3]。 PACAP（1-27）（0.005-5μg）以剂量依赖性方式将基础胰岛素分泌增加约15倍。局部输注葡萄糖（5％）或PACAP（1-27）（0.05μg）导致基础胰岛素输出显著增加至约300μUx/ min / g。 PACAP（1-27）直接增强麻醉狗内分泌胰腺中葡萄糖诱发的胰岛素分泌。该研究表明，PACAP可能在胰岛素分泌中起到促进葡萄糖负荷的局部促进作用[4]。
SMILES CCC(C)C(C(=O)NC(CC1=CC=CC=C1)C(=O)NC(C(C)O)C(=O)NC(CC(=O)O)C(=O)NC(CO)C(=O)NC(CC2=CC=C(C=C2)O)C(=O)NC(CO)C(=O)NC(CCCNC(=N)N)C(=O)NC(CC3=CC=C(C=C3)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCCCN)C(=O)NC(CCC(=O)N)C(=O)NC(CCSC)C(=O)NC(C)C(=O)NC(C(C)C)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CC4=CC=C(C=C4)O)C(=O)NC(CC(C)C)C(=O)NC(C)C(=O)NC(C)C(=O)NC(C(C)C)C(=O)NC(CC(C)C)C(=O)N)NC(=O)CNC(=O)C(CC(=O)O)NC(=O)C(CO)NC(=O)C(CC5=CNC=N5)N
靶点 PACAP receptor
动物实验 豚鼠[3] PACAP-27（0.045至4.5 nmol / kg / min），沙丁胺醇（0.045至4.5 nmol / kg / min）或无菌生理盐水通过输液泵静脉注射（1.0 mL），开始于5分钟前气道激发后持续10分钟[3]。狗[4]四只狗（28.4±1.8 kg）接受PACAP（1-27），其中四种不同浓度分别为0.01,0.1,1.0和10μg/ mL，或0.00318,0.0318,0.318和3.18μM。每种溶液以0.5mL / min的速率局部注入，精确1分钟。因此，在每次输注期间递送至胰腺的总剂量为0.005,0.05,0.5和5μg。关于输注速率考虑胰腺动脉导管的死体积（0.5mL）。在从SPD静脉和主动脉同时取出初始对照样品后，输注盐水1分钟并在输注开始后1,3和5分钟获得样品。对于PACAP（1-27）的剂量，每15分钟重复该过程。在每次输注开始后15分钟获得的样品用作随后干预的对照[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]. 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.
规格 1mg

是有效的PACAP受体拮抗剂。

PACAP-1-38

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PACAP-1-38

货号：
IP3120

品牌：
Jinpan

PACAP-1-38

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产品简介
有效期 2年
别名 体腺苷酸环化酶-活化聚肽
英文名称 PACAP-1-38
CAS 137061-48-4
分子式 C203H331N63O53S
分子量 4534.26
储存条件 -20°C
纯度 ≥96%
外观（性状） White Powder
单位 瓶
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 4 nM (PACAP type I receptor); 2 nM (PACAP type II receptor VIP1); 1 nM (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].
In Vivo 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].
SMILES —
靶点 PACAP receptor
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.
规格 1mg

H-Gly-Gly-Pro-OH 是由 3 个氨基酸构成的多肽。

PACAP-6-38

发表于由

PACAP-6-38

货号：
IP3130

品牌：
Jinpan

PACAP-6-38

暂无详情
产品简介
有效期 2年
英文名称 PACAP-6-38
CAS 143748-18-9
分子式 C182H300N56O45S
分子量 4024.74
储存条件 -20°C
纯度 ≥98%
外观（性状） White Powder
单位 瓶
SMILES —
靶点 PACAP receptor
规格 1mg
His-Pro 是一种由组氨酰和脯氨酸组成的二肽。