ChemicalBook > CAS DataBase List > N-[(3-aminooxetan-3-yl)methyl]-2-(1,1-dioxido-2,3-dihydro-1,4-benzothiazepin-4(5H)-yl)-6-methylquinazolin-4-amine

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
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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
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0086934
Product name
Ziresovir
Purity
99.86%
Packaging
5mg
Price
$350
Updated
2021/12/16
ChemScene
Product number
CS-0086934
Product name
Ziresovir
Purity
99.86%
Packaging
10mg
Price
$550
Updated
2021/12/16
ChemScene
Product number
CS-0086934
Product name
Ziresovir
Purity
99.86%
Packaging
25mg
Price
$990
Updated
2021/12/16
ChemScene
Product number
CS-0086934
Product name
Ziresovir
Purity
99.86%
Packaging
50mg
Price
$1650
Updated
2021/12/16
ChemScene
Product number
CS-0086934
Product name
Ziresovir
Purity
99.86%
Packaging
100mg
Price
$2250
Updated
2021/12/16
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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 bioavailability?with 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)906581.23.932
Pharmacokinetics of Ziresovir in CD-1 Mice[1]
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)
plasma8,38011.020.255090
lung72,4008.63.31122700
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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N-[(3-aminooxetan-3-yl)methyl]-2-(1,1-dioxido-2,3-dihydro-1,4-benzothiazepin-4(5H)-yl)-6-methylquinazolin-4-amine Suppliers

China 27 United States 2 Global 29
Shanghai Balmxy Pharmaceutical Co., Ltd
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1422500-60-4, N-[(3-aminooxetan-3-yl)methyl]-2-(1,1-dioxido-2,3-dihydro-1,4-benzothiazepin-4(5H)-yl)-6-methylquinazolin-4-amineRelated Search:


  • N-[(3-aminooxetan-3-yl)methyl]-2-(1,1-dioxido-2,3-dihydro-1,4-benzothiazepin-4(5H)-yl)-6-methylquinazolin-4-amine
  • Ziresovir
  • 4-(4-(((3-Aminooxetan-3-yl)methyl)amino)-6-methylquinazolin-2-yl)-2,3,4,5-tetrahydrobenzo[f][1,4]thiazepine 1,1-dioxide
  • AK0529
  • RO-0529
  • 4-Quinazolinamine, N-[(3-amino-3-oxetanyl)methyl]-2-(2,3-dihydro-1,1-dioxido-1,4-benzothiazepin-4(5H)-yl)-6-methyl-
  • Sialyllactose Impurity 22
  • RO-0529(AK0529) Ziresovir
  • 1422500-60-4