ACT 335827
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.
ACT 335827是OXR-1的有效选择性拮抗剂,对OXR-1和OXR-2的IC50值分别为120和2300 nM[1].
食欲素受体1(OR-1)是神经肽食欲素A的G蛋白偶联受体,调节摄食行为.OXR-1在下丘脑中表达.
ACT 335827是OXR-1的强效选择性拮抗剂,对OXR-1和OXR-2的Kb值分别为41和560 nM[1].
在恐惧增强惊吓老鼠中,300 mg/kg的ACT-335827抑制恐惧引起的惊吓反应.此外,300 mg/kg的ACT-335827显著减少应激诱导的心动过速和发热.在大鼠烦渴模型中,300 mg/kg的ACT-335827抑制强迫饮酒行为[1].在暴露于新颖性应激的大鼠中,100 mg/kg的ACT-335827分别减少48%和32%的心动过速和升压[2].在饮食诱导的肥胖(DIO)大鼠模型中,ACT-335827增加高密度脂蛋白的水平和水的摄入量.此外,ACT-335827略微增加体重,表明OXR-1抑制在该模型中具有最小的影响[3].
参考文献:
[1]. Steiner MA, Gatfield J, Brisbare-Roch C, et al. Discovery and characterization of ACT-335827, an orally available, brain penetrant orexin receptor type 1 selective antagonist. ChemMedChem, 2013, 8(6): 898-903.
[2]. Beig MI, Dampney BW, Carrive P. Both Ox1r and Ox2r orexin receptors contribute to the cardiovascular and locomotor components of the novelty stress response in the rat. Neuropharmacology, 2015, 89: 146-156.
[3]. Steiner MA, Sciarretta C, Pasquali A, et al. The selective orexin receptor 1 antagonist ACT-335827 in a rat model of diet-induced obesity associated with metabolic syndrome. Front Pharmacol, 2013, 4: 165.
Physical Appearance | Off-white solid |
Storage | Store at -20°C |
M.Wt | 518.64 |
Cas No. | 1354039-86-3 |
Formula | C31H38N2O5 |
Solubility | <51.86mg/ml in DMSO; <51.86mg/ml in ethanol |
Chemical Name | (R,Z)-2-((S)-1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-N-isopropyl-2-phenylacetimidic acid |
SDF | Download SDF |
Canonical SMILES | CC(/N=C(O)/[C@@](N1CCC2=CC(OC)=C(OC)C=C2[C@]1([H])CC3=CC(OC)=C(OC)C=C3)([H])C4=CC=CC=C4)C |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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