[CAS NO. 1422500-60-4] Ziresovir

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PRODUCTS SPECIFICATIONS [1422500-60-4]

Catelog

HY-109142

Brand

MCE

CAS

1422500-60-4

DESCRIPTION [1422500-60-4]

Overview

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

For research use only. We do not sell to patients.

1 Publications Citing Use of MCE

[1]J Virol. 2021 Aug 11;JVI0120521.

Summary

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 ( EC ₅₀ =3 nM) and highlights pharmacokinetics in animal species ^[1] .

IC50 & Target

RSV F protein (respiratory syncytial virus fusion protein) ^[1] EC50: 3 nM (RSV F) ^[1]

In Vitro

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.

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)	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

Pharmacokinetics of Ziresovir in CD-1 Mice ^[1]

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.

Clinical Trial

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

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL ( 284.39 mM ; Need ultrasonic)

Preparing
Stock Solutions

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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (4.73 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (4.73 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (4.73 mM); Clear solution

* All of the co-solvents are available by MCE.

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.