Lorglumide (sodium salt)
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.
Lorglumide (sodium salt) is the first nonpeptidic, selective and potent inhibitor of the CCK-A receptor [1][2][3][4] .
Cholecystokinin (CCK) is a peptide hormone that plays important roles in the physiological regulation of pancreatic enzyme secretion, induction of pancreatic growth, smooth muscle contraction in the gall bladder and stomach, and modulation of feeding and behavior [1][2][3].
Lorglumide (CR1409) is the first nonpeptidic, selective and potent inhibitor of the CCK-A receptor. Lorglumide inhibited CCK A receptor and CCK B receptor with IC50 values of 50 nM and 3 μM, respectively [4]. In the guinea-pig isolated ileum, Lorglumide (0.06-2.1 μM) antagonized longitudinal muscle responses to ceruletide (a CCK-related decapeptide) and CCK-octapeptide (CCK-8) in a concentration dependent and competitive manner. Lorglumide (0.2-0.4 μM) also blocked contractions of the circular muscle induced by ceruletide [2].
In mice, CR1409 completely abolished the trophic effects of exogenous CCK and significantly inhibited the effects of chronic camostate feeding. CR1409 reduced pancreatic weight, DNA and protein content [3].
References:
[1]. Makovec F, Peris W, Revel L, et al. Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives. J Med Chem. 1992 Jan;35(1):28-38.
[2]. Barthó L, Holzer P, Lembeck F, et al. Evaluation of a new and potent cholecystokinin antagonist on motor responses of the guinea-pig intestine. Br J Pharmacol. 1987 Apr;90(4):753-61.
[3]. Niederau C, Liddle RA, Williams JA, et al. Pancreatic growth: interaction of exogenous cholecystokinin, a protease inhibitor, and a cholecystokinin receptor antagonist in mice. Gut. 1987;28 Suppl:63-9.
[4]. Scarpignato C, Varga G, Dobronyi I, et al. Effect of a new potent CCK antagonist, lorglumide, on caerulein- and bombesin-induced pancreatic secretion and growth in the rat. Br J Pharmacol. 1989 Mar;96(3):661-9.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 481.4 |
Cas No. | 1021868-76-7 |
Formula | C22H31Cl2N2O4·Na |
Solubility | ≤1mg/ml in ethanol;1mg/ml in DMSO;1mg/ml in dimethyl formamide |
Chemical Name | 4-[(3,4-dichlorobenzoyl)amino]-5-(dipentylamino)-5-oxo-pentanoic acid, monosodium salt |
SDF | Download SDF |
Canonical SMILES | ClC1=C(Cl)C=CC(C(NC(C(N(CCCCC)CCCCC)=O)CCC([O-])=O)=O)=C1.[Na] |
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。 |