ACT-335827
- CAS No.
- 1354039-86-3
- Chemical Name:
- ACT-335827
- Synonyms
- ACT-335827;ACT 335827; ACT335827;ACT-335827,CID 54765113;(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;(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)-
- CBNumber:
- CB23038493
- Molecular Formula:
- C31H38N2O5
- Molecular Weight:
- 518.65
- MDL Number:
- MFCD27991288
- MOL File:
- 1354039-86-3.mol
ACT-335827 price More Price(6)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Tocris | 4983 | ACT335827 ≥98%(HPLC) | 1354039-86-3 | 10 | $368 | 2021-12-16 | Buy |
| Tocris | 4983 | ACT335827 ≥98%(HPLC) | 1354039-86-3 | 50 | $1488 | 2021-12-16 | Buy |
| TRC | A305310 | ACT335827 | 1354039-86-3 | 2.5mg | $415 | 2021-12-16 | Buy |
| Usbiological | 254537 | ACT 335827 | 1354039-86-3 | 10mg | $631 | 2021-12-16 | Buy |
| ApexBio Technology | B5787 | ACT335827 | 1354039-86-3 | 10mg | $534 | 2021-12-16 | Buy |
ACT-335827 Chemical Properties,Uses,Production
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
Raw materials
Preparation Products
ACT-335827 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| AdooQ BioScience, LLC | +1 (866) 930-6790 | info@adooq.com | United States | 2784 | 58 |
| Jinan Yaoyan Pharmaceutical Co., Ltd. | jnyaoyan@163.com | China | 3069 | 58 | |
| Nanjing Meihao Pharmaceutical Technology Co., Ltd. | meitaochem@126.com | meitaochem@126.com | China | 19105 | 58 |
| BOC Sciences | -- | info@bocsci.com | USA | 0 | 65 |
| Absin Bioscience Inc. | 021-38015121 15000105423 | chenjw@absin.cn | China | 24734 | 58 |
| Changzhou Furuisi Biotechnology Co., Ltd | 0519-85524369 | 3477467573@qq.com | China | 8618 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24017 | 58 |
| Nantong QuanYi Biotechnology Co., Ltd | 0513-66337626 18051384581 | sales@chemhifuture.com | China | 4249 | 58 |
| United States Biological | -- | sales@advtechind.com | United States | 6106 | 58 |