ACT-462206
- CAS No.
- 1361321-96-1
- Chemical Name:
- ACT-462206
- Synonyms
- ACT-462206;ACT 462206,ACT462206;ACT-462206 >=98% (HPLC);ACT-462206, 10 mM in DMSO;(2S)-N-(3,5-DIMETHYLPHENYL)-1-(4-METHOXYPHENYL)SULFONYLPYRROLIDINE-2-CARBOXAMIDE;(2S)-N-(3,5-Dimethylphenyl)-1-[(4-methoxyphenyl)sulfonyl]-2-pyrrolidinecarboxamide;2-Pyrrolidinecarboxamide, N-(3,5-dimethylphenyl)-1-[(4-methoxyphenyl)sulfonyl]-, (2S)-
- CBNumber:
- CB53167703
- Molecular Formula:
- C20H24N2O4S
- Molecular Weight:
- 388.48
- MDL Number:
- MFCD28502270
- MOL File:
- 1361321-96-1.mol
| Density | 1.285±0.06 g/cm3(Predicted) |
|---|---|
| storage temp. | Store at -20°C |
| solubility | Soluble in DMSO |
| pka | 14.27±0.70(Predicted) |
| form | Solid |
| color | White to off-white |
| FDA UNII | 64ONO62P28 |
| UNSPSC Code | 51111800 |
| NACRES | NA.77 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302 |
| Precautionary statements | P301+P312+P330 |
ACT-462206 price More Price(4)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Tocris | 5319 | ACT462206 ≥99%(HPLC) | 1361321-96-1 | 10 | $219 | 2021-12-16 | Buy |
| Tocris | 5319 | ACT462206 ≥99%(HPLC) | 1361321-96-1 | 50 | $815 | 2021-12-16 | Buy |
| TRC | A305313 | ACT462206 | 1361321-96-1 | 2.5mg | $220 | 2021-12-16 | Buy |
| Usbiological | 254538 | ACT 462206 | 1361321-96-1 | 10mg | $495 | 2021-12-16 | Buy |
ACT-462206 Chemical Properties,Uses,Production
Uses
ACT-462206 is a potent and selective dual orexin receptor antagonist (DORA) that inhibits the stimulating effects of the orexin peptides at both the orexin 1 and 2 receptors. It decreases wakefulness and increases non-rapid eye movement (non-REM) and REM sleep while maintaining natural sleep architectures in some animal models while showing anxiolytic-like properties without affecting cognition and motor function in others.
Biological Activity
ACT-462206 is a orally active, brain penetrant, potent and selective dual orexin1/2 receptor antagonist (DORA). ACT-462206 decreases wakefulness, decreases sleep latency, and increases sleep efficacy in rats and dogs.', 'ACT-462206 is a proline sulphonamide with the potential to tre at insomnia. On absorption, its displays asthenia, blurred vision, and fatigue as adverse events.
in vivo
ACT-462206 (compound 24) (100 mg/kg; p.o.; sampling at 3 h) can go cross blood brain barrier, with concentrations are 2267 ng/mL and 1219 ng/g in plasma and brain, respectively in male Wistar rats[1].
ACT-462206 (10-300 mg/kg; p.o.; single dose) shows sleep-promoting effects in male Wistar rats and in male Beagle dogs, with decreasing wakefulness and increasing non-rapid eye movement (non-REM) and REM sleep[1].
ACT-462206 (100, 300 mg/kg; p.o.; single dose) exerts anxiolytic-like effects, decreases the fear-potentiated startle reflexes in response to a sudden loud noise in rats, reduces the socialstress-induced increases of locomotion, body temperature, and heart rate[1].
Pharmacokinetics in different species[1]
| Route | Dose (mg/kg) | AUC (ng h/mL) | CL (mL/min/kg) | Vss (L/kg) | t1/2 (h) | cmax (ng/mL) | tmax (h) | F1/2 (%) | |
| rat | i.v. | 1 | 586 | 29 | 1.8 | 1.9 | / | / | / |
| p.o. | 10 | 2310 | / | / | / | 1600 | 0.5 | 39 | |
| dog | i.v. | 1 | 1490 | 11 | 1.4 | 1.7 | / | / | / |
| p.o. | 3 | 2750 | / | / | / | 426 | 0.5 | 52 |
| Animal Model: | Male Wistar rats[1] |
| Dosage: | 0, 10, 30, 100, 300 mg/kg |
| Administration: | Oral gavage; single dose |
| Result: | Decreased the latency to the first persistent episode of non-REM sleep (60 s) and the first persistent episode of REM sleep (30 s). Dose-dependently decreased total wake time and behavioral home cage activity (one-way ANOVA; p <0.001), while increasing REM and non-REM sleep times. |
IC 50
OX2; OX1
storage
Store at +4°C
ACT-462206 Preparation Products And Raw materials
ACT-462206 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32159 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 57505 | 58 | |
| HangZhou YuHao Chemical Technology Co., Ltd. | 0571-82693216 | info@yuhaochemical.com | China | 2028 | 58 |
| Shanghai JiYi Biotechnology Co. Ltd. | 13621943973 | sales@shjiyipharmatech.com | China | 1166 | 55 |
| Shanghai YuanYe Biotechnology Co., Ltd. | 021-61312847; 18021002903 | 3008007409@qq.com | China | 71829 | 60 |
| MQ (shanghai) Pharmaceuticals Co., Ltd. | 13761635123 | 1014988033@qq.com | China | 4966 | 55 |
| Jinan Yaoyan Pharmaceutical Co., Ltd. | jnyaoyan@163.com | China | 3069 | 58 | |
| Angel Pharmatech, Ltd. | 17317130613 | 3358272972@qq.com | China | 3260 | 58 |
| Shanghai Hongye Biotechnology Co. Ltd | 400-9205774 | sales@glpbio.cn | China | 6777 | 58 |
| Nanjing Meihao Pharmaceutical Technology Co., Ltd. | meitaochem@126.com | meitaochem@126.com | China | 19103 | 58 |