ACT 335827 |
Catalog No.GC16336 |
Orexin receptor 1 antagonist,potent and selective
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1354039-86-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
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. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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