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ACT 335827

Catalog No.GC16336

Orexin receptor 1 antagonist,potent and selective

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ACT 335827 Chemical Structure

Cas No.: 1354039-86-3

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10mg
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Sample solution is provided at 25 µL, 10mM.

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Background

ACT 335827 is a potent and selective antagonist of OXR-1 with IC50 values of 120 and 2300 nM for OXR-1 and OXR-2, respectively [1].

Orexin receptor 1 (OXR-1) is a G-protein coupled receptor for neuropeptide orexin-A and regulates feeding behaviour. OXR-1 is expressed in the hypothalamus.

ACT 335827 is a potent and selective OXR-1 antagonist with Kb values of 41 and 560 nM for OXR-1 and OXR-2, respectively [1].

In the fear-potentiated startle rats, ACT-335827 (300 mg/kg) inhibited fear-induced startle reactions. Also, ACT-335827 (300 mg/kg) significantly reduced stress-induced tachycardia and hyperthermia. In the rat polydipsia model, ACT-335827 (300 mg/kg) inhibited compulsive drinking behavior [1]. In rats exposed to novelty stress, ACT-335827 (100 mg/kg) reduced the tachycardic and pressor by 48% and 32%, respectively [2]. In a diet-induced obesity(DIO) rat model, ACT-335827 increased the level of high-density lipoprotein and water intake. Also, it slightly increased body weight, which suggested that inhibition of OXR-1 had minimal impact in this model [3].

References:
[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.

Chemical Properties

Cas No. 1354039-86-3 SDF
Chemical Name (R,Z)-2-((S)-1-(3,4-dimethoxybenzyl)-6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-N-isopropyl-2-phenylacetimidic acid
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
Formula C31H38N2O5 M.Wt 518.64
Solubility <51.86mg/ml in DMSO; <51.86mg/ml in ethanol Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.9281 mL 9.6406 mL 19.2812 mL
5 mM 0.3856 mL 1.9281 mL 3.8562 mL
10 mM 0.1928 mL 0.9641 mL 1.9281 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 25 reference(s) in Google Scholar.)

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