A-71623
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
A-71623是CCKA受体的选择性激动剂，对豚鼠胰腺的IC50值为3.7 nM[1,2]。
CCKA受体属于大脑中胆囊收缩素（CCK）受体的亚型。CCK是一种神经肽，在整个中枢神经系统中广泛分布。CCK可以作为正常和异常脑中的神经递质。CCK受体在大脑以两种形式存在，CCK受体的另一亚型是CCKB亚型[1]。
在具有CCKB/胃泌素受体的NCI-H345细胞中，A-71623作用较弱，在钙的研究中作为部分激动剂[2]。在C6细胞中，A-71623对CCK结合位点的亲和力非常低，IC50值为1236 ± 81 nM[3]。A-71623作用于细胞，很难得到CCKA的响应结果。
在放射配体结合实验中，A-71623对于豚鼠胰腺CCKA的IC50值为3.7 nM，对大脑皮层CCKB的IC50值为4500 nM。数据表明，A-71623是一种激动剂，可以刺激胰淀粉酶的释放，这种刺激作用可以被CCKA拮抗剂L-364,718强效抑制。数据显示，A-71623可以作为完全激动剂刺激胰腺中磷酸肌醇的降解。在回肠中，A-71623也可以作为强效激动剂刺激CCKA受体。在豚鼠胃腺中，A-71623对于CCK-B/胃泌素受体的亲和力为11 μM。这一结果表明，A-71623是CCKA受体的一种强效选择性激动剂[2]。
参考文献：
[1]. Gracey DJ, Bell R, King DJ. Differential effects of the CCKA receptor ligands PD-140,548 and A-71623 on latent inhibition in the rat. Progress in Neuro-Psychopharmacology and Biological Psychiatry, 2002, 26(3): 497-504.
[2]. Lin CW, Shiosaki K, Miller TR, et al. Characterization of two novel cholecystokinin tetrapeptide (30-33) analogues, A-71623 and A-70874, that exhibit high potency and selectivity for cholecystokinin-A receptors. Molecular pharmacology, 1991, 39(3): 346-351.
[3]. Kaufmann R, Lindschau C, Scho T, et al. Type B cholecystokinin receptors on rat glioma C6 cells. Binding studies and measurement of intracellular calcium mobilization. Brain research, 1994, 639(1): 109-114.
| Physical Appearance | White lyophilised solid |
| Storage | Desiccate at -20°C |
| M.Wt | 840.97 |
| Cas No. | 130408-77-4 |
| Formula | C44H56N8O9 |
| Solubility | Soluble to 1 mg/ml in 20mM PBS buffer |
| Chemical Name | (6S,9S,12S)-6-((1H-indol-3-yl)methyl)-12-(((S)-1-amino-1-oxo-3-phenylpropan-2-yl)(methyl)carbamoyl)-2,2-dimethyl-4,7,10-trioxo-9-(4-(3-(o-tolyl)ureido)butyl)-3-oxa-5,8,11-triazatetradecan-14-oic acid |
| SDF | Download SDF |
| Canonical SMILES | O=C([C@H](CCCCNC(NC1=CC=CC=C1C)=O)NC([C@H](CC2=CNC3=CC=CC=C23)NC(OC(C)(C)C)=O)=O)N[C@@H](CC(O)=O)C(N(C)[C@H](C(N)=O)CC4=CC=CC=C4)=O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
化学结构
