N-[(3-aminooxetan-3-yl)methyl]-2-(1,1-dioxido-2,3-dihydro-1,4-benzothiazepin-4(5H)-yl)-6-methylquinazolin-4-amine
- Product Name
- N-[(3-aminooxetan-3-yl)methyl]-2-(1,1-dioxido-2,3-dihydro-1,4-benzothiazepin-4(5H)-yl)-6-methylquinazolin-4-amine
- CAS No.
- 1422500-60-4
- Chemical Name
- N-[(3-aminooxetan-3-yl)methyl]-2-(1,1-dioxido-2,3-dihydro-1,4-benzothiazepin-4(5H)-yl)-6-methylquinazolin-4-amine
- Synonyms
- AK0529;RO-0529;Ziresovir;RO-0529(AK0529) Ziresovir;Sialyllactose Impurity 22;N-[(3-aminooxetan-3-yl)methyl]-2-(1,1-dioxido-2,3-dihydro-1,4-benzothiazepin-4(5H)-yl)-6-methylquinazolin-4-amine;4-Quinazolinamine, N-[(3-amino-3-oxetanyl)methyl]-2-(2,3-dihydro-1,1-dioxido-1,4-benzothiazepin-4(5H)-yl)-6-methyl-;4-(4-(((3-Aminooxetan-3-yl)methyl)amino)-6-methylquinazolin-2-yl)-2,3,4,5-tetrahydrobenzo[f][1,4]thiazepine 1,1-dioxide
- CBNumber
- CB33147253
- Molecular Formula
- C22H25N5O3S
- Formula Weight
- 439.53
- MOL File
- 1422500-60-4.mol
N-[(3-aminooxetan-3-yl)methyl]-2-(1,1-dioxido-2,3-dihydro-1,4-benzothiazepin-4(5H)-yl)-6-methylquinazolin-4-amine Property
- Boiling point:
- 745.4±70.0 °C(Predicted)
- Density
- 1.390±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 125 mg/mL (284.39 mM)
- form
- Solid
- pka
- 7.70±0.20(Predicted)
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- CS-0086934
- Product name
- Ziresovir
- Purity
- 99.86%
- Packaging
- 5mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-0086934
- Product name
- Ziresovir
- Purity
- 99.86%
- Packaging
- 10mg
- Price
- $550
- Updated
- 2021/12/16
- Product number
- CS-0086934
- Product name
- Ziresovir
- Purity
- 99.86%
- Packaging
- 25mg
- Price
- $990
- Updated
- 2021/12/16
- Product number
- CS-0086934
- Product name
- Ziresovir
- Purity
- 99.86%
- Packaging
- 50mg
- Price
- $1650
- Updated
- 2021/12/16
- Product number
- CS-0086934
- Product name
- Ziresovir
- Purity
- 99.86%
- Packaging
- 100mg
- Price
- $2250
- Updated
- 2021/12/16
N-[(3-aminooxetan-3-yl)methyl]-2-(1,1-dioxido-2,3-dihydro-1,4-benzothiazepin-4(5H)-yl)-6-methylquinazolin-4-amine Chemical Properties,Usage,Production
Uses
Ziresovir (AK0529;RO-0529) is a potent, selective, and orally bioavailable respiratory syncytial virus (RSV) fusion (F) protein (RSV F) protein inhibitor. Ziresovir shows anti-RSV activity (EC50=3 nM) and highlights pharmacokinetics in animal species[1].
in vivo
Ziresovir (12.5 mg/kg, 50 mg/kg; p.o.; twice daily; 4 d) results reduction of RSV titer in mouse lung[1].
Ziresovir (10 mg/kg; p.o.; single dose) exhibits good oral exposure and bioavailabilitywith F(%) of 32% in male Wistar-Han rats[1].
Ziresovir (150 mg/kg; p.o.; single dose) demonstrates a high tissue distribution to lung than plasma in CD-1 Mice[1].
Pharmacokinetics of Ziresovir in male Wistar-Han rats[1]
| Dose (mg/kg) | AUC0-24h(p.o.) (ng·h/mL) | CL (mL/min/kg) | T1/2(i.v.) (h) | Vss (L/kg) | F (%) |
| 2 mg/kg (iv) or 10 mg/kg (po) | 906 | 58 | 1.2 | 3.9 | 32 |
| Dose (mg/kg) | AUC0-24h(p.o.) (μg·h/L) | tissue/lasma AUC0-24h ratio (μg·h/L) | T1/2 (h) | Tmax (h) | Cmax (μg/L) |
| plasma | 8,380 | 1 | 1.02 | 0.25 | 5090 |
| lung | 72,400 | 8.6 | 3.31 | 1 | 22700 |
| Animal Model: | Female BALB/c mice infected by RSV[1] |
| Dosage: | 12.5 mg/kg, 50 mg/kg |
| Administration: | Oral gavage; twice daily; 4 days |
| Result: | Resulted >1 log unit of viral titer reduction in the lung of infected mice at the dose level as low as 12.5 mg/kg. Reduced viral titer to 1.9 log units compared to vehicle at 50 mg/kg dose. |
References
[1] Zheng X, et al. Discovery of Ziresovir as a Potent, Selective, and Orally Bioavailable Respiratory Syncytial Virus Fusion Protein Inhibitor. J Med Chem. 2019 Jul 11;62(13):6003-6014. DOI:10.1021/acs.jmedchem.9b00654
N-[(3-aminooxetan-3-yl)methyl]-2-(1,1-dioxido-2,3-dihydro-1,4-benzothiazepin-4(5H)-yl)-6-methylquinazolin-4-amine Preparation Products And Raw materials
Raw materials
Preparation Products
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