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Product Name:ACT-335827
CAS:1354039-86-3
Purity:98% Package:5mg;10mg;25mg;50mg;100mg;250mg;500mg;1g
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ACT-335827 manufacturers
- ACT 335827
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- $4600.00 / 50mg
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2024-10-24
- CAS:1354039-86-3
- Min. Order:
- Purity:
- Supply Ability: 10g
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| | ACT-335827 Basic information |
| Product Name: | ACT-335827 | | Synonyms: | ACT-335827;ACT 335827; ACT335827;(aR,1S)-1-[(3,4-Dimethoxyphenyl)methyl]-3,4-dihydro-6,7-dimethoxy-N-(1-methylethyl)-a-phenyl-2(1H)-isoquinolineacetamide;(2R)-2-[(1S)-1-[(3,4-dimethoxyphenyl)methyl]-6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl]-N-isopropyl-2-phenyl-acetamide;ACT-335827,CID 54765113;(2R)-2-[(1S)-1-[(3,4-DIMETHOXYPHENYL)METHYL]-6,7-DIMETHOXY-3,4-DIHYDRO-1H-ISOQUINOLIN-2-YL]-2-PHENYL-N-PROPAN-2-YLACETAMIDE;2(1H)-Isoquinolineacetamide, 1-[(3,4-dimethoxyphenyl)methyl]-3,4-dihydro-6,7-dimethoxy-N-(1-methylethyl)-α-phenyl-, (αR,1S)- | | CAS: | 1354039-86-3 | | MF: | C31H38N2O5 | | MW: | 518.65 | | EINECS: | | | Product Categories: | | | Mol File: | 1354039-86-3.mol |  |
| | ACT-335827 Chemical Properties |
| Boiling point | 664.0±55.0 °C(Predicted) | | density | 1.144±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | <51.86mg/ml in DMSO; <51.86mg/ml in ethanol | | form | solid | | pka | 14.75±0.46(Predicted) | | color | Off-white |
| | ACT-335827 Usage And Synthesis |
| Uses | ACT 335827 is an orally available, brain penetrant orexin receptor type 1 selective antagonist and elicits anxiolytic-like effects without promoting sleep. | | Biological Activity | 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]. | | Enzyme inhibitor | This brain-penetrant and orally available orexin receptor antagonist (FW = 518.64 g/mol; CAS 1354039-86-3; Soluble to 100 mM in DMSO, also known as (aR,1S)-1-[(3,4-Dimethoxyphenyl)methyl]-3,4-dihydro-6,7dimethoxy-N-(1-methylethyl)-a-phenyl-2(1H)-isoquinoline acetamide, elicits its anxiolytic effects in vivo by targeting OX1 (Ki = 41 nM) and OX2 (Ki = 560 nM) receptors. ACT-335827 decreases fear, compulsive behaviors, and autonomic stress reactions in rats. | | storage | Store at -20°C | | 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. |
| | ACT-335827 Preparation Products And Raw materials |
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