SR 48692
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.
SR 48692对HT-29细胞的Ki值为8.6 nM。
SR 48692是一种非肽类神经降压素的拮抗剂。
神经降压素是一种十三肽,分布于中枢和外周神经系统。神经降压素具有广泛的生物学活性,在大脑中显示出神经递质/神经调质双重功能,在外周组织中起着激素/细胞介质作用。
体外:在小鼠大脑与HT-29细胞中,SR 48692抑制[3H]-神经降压素或[125I]-神经降压素结合细胞膜。在HT-29细胞中,SR 48692还拮抗神经降压素诱导的细胞内钙离子动员,与以往研究结果一致。此外,在大鼠小脑切片中,SR 48692呈剂量依赖性地抑制cGMP水平增加[1]。
体内:在大鼠脑内,具有全身性作用的神经降压素活性肽EI用于诱导中脑边缘多巴胺更新,而SR 48692能拮抗多巴胺更新率。然而,SR 48692不能拮抗EI诱导的小鼠体温下降以及自发活动减少[1]。
临床试验:在临床试验中,SR 48692用于研究内源性神经降压素对食管下段括约肌功能的影响。结果表明,SR 48692对人食管运动无影响[2]。
参考文献:
[1] Pugsley TA, Akunne HC, Whetzel SZ, Demattos S, Corbin AE, Wiley JN, Wustrow DJ, Wise LD, Heffner TG. Differential effects of the nonpeptide neurotensin antagonist, SR 48692, on the pharmacological effects of neurotensin agonists. Peptides. 1995;16(1):37-44.
[2] Zerbib F, Piche T, Charles F, Galmiche JP, Bruley des Varannes S. SR 48692, a specific neurotensin receptor antagonist, has no effect on oesophageal motility in humans. Aliment Pharmacol Ther. 2004 Apr 15;19(8):931-9.
Physical Appearance | White solid |
Storage | Store at -20°C |
M.Wt | 587.07 |
Cas No. | 146362-70-1 |
Formula | C32H31ClN4O5 |
Solubility | Soluble in DMSO |
Chemical Name | (1R,2R,3R,5S,7S)-2-(1-(7-chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)-1H-pyrazole-3-carboxamido)adamantane-2-carboxylic acid |
SDF | Download SDF |
Canonical SMILES | ClC1=CC=C2C(N3N=C(C=C3C(C(OC)=CC=C4)=C4OC)C(N[C@]5(C(O)=O)[C@H]6C[C@H]7C[C@H]5C[C@H](C7)C6)=O)=CC=NC2=C1 |
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。 |