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Catalog: | HY-109142 |
Brand: | MCE |
CAS: | 1422500-60-4 |
MDL | - |
---|---|
Molecular Weight | 439.53 |
Molecular Formula | C22H25N5O3S |
SMILES | NC1(COC1)CNC2=NC(N(CC3)CC4=CC=CC=C4S3(=O)=O)=NC5=C2C=C(C)C=C5 |
Ziresovir shows different efficacy in Wild Type (WT) and Mutant Strains RSV with EC
50
/EC
90
values (μM) of 0.003/0.005 (WT), 2.1/10.0 (D486N), and >10/>10 (D489A), respectively
[1]
.
RO-0529 (100 nM; 4 d) inhibits RSV F protein-induced cell–cell fusion process, and suppresses the syncytia formation induced by the RSV F protein
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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) | AUC 0-24h (p.o.) (ng·h/mL) | CL (mL/min/kg) | T 1/2 (i.v.) (h) | V ss (L/kg) | F (%) |
2 mg/kg (iv) or 10 mg/kg (po) | 906 | 58 | 1.2 | 3.9 | 32 |
Dose (mg/kg) | AUC 0-24h (p.o.) (μg·h/L) | tissue/lasma AUC 0-24h ratio (μg·h/L) | T 1/2 (h) | T max (h) | C max (μg/L) |
plasma | 8,380 | 1 | 1.02 | 0.25 | 5090 |
lung | 72,400 | 8.6 | 3.31 | 1 | 22700 |
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
NCT Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT03699202 | Ark Biosciences Inc. |
Respiratory Syncytial Virus Infections
|
March 29, 2019 | Phase 2 |
NCT04231968 | Ark Biosciences Inc.|Shanghai Ark Biopharmaceutical Co., Ltd. |
Respiratory Syncytial Virus Infections
|
September 23, 2020 | Phase 3 |
NCT04788017 | Ark Biosciences Inc. |
Healthy Subjects
|
March 24, 2021 | Phase 1 |
NCT03400995 | Ark Biosciences Inc. |
Healthy
|
January 5, 2018 | Phase 1 |
NCT02460016 | Ark Biosciences Inc. |
Respiratory Syncytial Virus Infections
|
August 28, 2015 | Phase 1 |
NCT03322800 | Ark Biosciences Inc. |
Healthy
|
October 23, 2017 | Phase 1 |
NCT02297594 | Ark Biosciences Inc. |
Respiratory Syncytial Virus Infections
|
October 2014 | Phase 1 |
NCT02654171 | Ark Biosciences Inc.|Ark Biosciences Pty Ltd. |
RESPIRATORY SYNCYTIAL VIRUS INFECTIONS
|
May 27, 2016 | Phase 2 |
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : 125 mg/mL ( 284.39 mM ; Need ultrasonic)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 2.2752 mL | 11.3758 mL | 22.7516 mL |
5 mM | 0.4550 mL | 2.2752 mL | 4.5503 mL |
10 mM | 0.2275 mL | 1.1376 mL | 2.2752 mL |
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