Description
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 . 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 . 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 . In rats exposed to novelty stress, ACT-335827 (100 mg/kg) reduced the tachycardic and pressor by 48% and 32%, respectively . 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 .
Product information
CAS Number: 1354039-86-3
Molecular Weight: 518.64
Formula: C31H38N2O5
Chemical Name: (Z,2R)-2-[(1S)-1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl]-2-phenyl-N-(propan-2-yl)ethanimidic acid
Smiles: CC(C)/N=C(\O)/[C@@H](C1=CC=CC=C1)N1CCC2=CC(OC)=C(C=C2[C@@H]1CC1C=CC(OC)=C(C=1)OC)OC
InChiKey: HXHOBPVRRPCTLG-SETSBSEESA-N
InChi: InChI=1S/C31H38N2O5/c1-20(2)32-31(34)30(22-10-8-7-9-11-22)33-15-14-23-18-28(37-5)29(38-6)19-24(23)25(33)16-21-12-13-26(35-3)27(17-21)36-4/h7-13,17-20,25,30H,14-16H2,1-6H3,(H,32,34)/t25-,30+/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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