[CAS NO. 1353625-73-6] Presatovir

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PRODUCTS SPECIFICATIONS [1353625-73-6]

Catalog

HY-16727

Brand

MCE

CAS

1353625-73-6

DESCRIPTION [1353625-73-6]

Overview

MDL	-
Molecular Weight	532.06
Molecular Formula	C24H30ClN7O3S
SMILES	O=C(C(C=C(Cl)C=C1)=C1NS(C)(=O)=O)N(CCCC2)[C@@H]2C3=NN4C(N=C(N5CC[C@H](N)C5)C(C)=C4)=C3

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

3 Publications Citing Use of MCE

Summary

Presatovir (GS-5806) is an orally bioavailable RSV fusion inhibitor with a mean EC ₅₀ value of 0.43 nM ^[1] .

IC50 & Target

EC50: 0.43 nM (RSV) ^[1]

In Vitro

Presatovir is a novel, orally bioavailable RSV fusion inhibitor discovered following a lead optimization campaign on a hit originated from a phenotypic RSV antiviral high-throughput screen. Presatovir exhibits potent activity against a wide range of RSV A and B clinical isolates with a mean EC ₅₀ value of 0.43 nM ^[1] . GS-5806 inhibits pre to post triggered conformational changes of RSV F protein, suggesting a possible mechanism for antiviral activity ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Presatovir demonstrates dose-dependent (0-30 mg/kg) antiviral efficacy in a cotton rat model of RSV infection. Oral bioavailability in preclinical species ranges from 46 to 100%, with penetration of the compound into the lung tissue demonstrated in Sprague-Dawley rats. Multidose oral treatment of Presatovir appears safe in adults, and in healthy human volunteers experimentally infected with RSV, a potent antiviral effect and reduction in disease severity is observed in the high dose group. A group treated with a lower dose of Presatovir allows for a PK-PD relationship to be established to help guide future dose selections ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02254408	Gilead Sciences	Respiratory Syncytial Virus	January 23, 2015	Phase 2
NCT01801293	Gilead Sciences	RSV Infection	March 2013	Phase 1
NCT01797419	Gilead Sciences	Respiratory Syncytial Virus Infections	May 2013	Phase 1
NCT02254421	Gilead Sciences	Respiratory Syncytial Virus Infection	January 31, 2015	Phase 2
NCT02534350	Gilead Sciences	Respiratory Syncytial Virus (RSV)	December 31, 2015	Phase 2
NCT02135614	Gilead Sciences	Respiratory Syncytial Virus Infection	June 9, 2014	Phase 2
NCT01756482	Gilead Sciences	Respiratory Syncytial Virus Infections	November 2012	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 : 6 mg/mL ( 11.28 mM ; Need ultrasonic and warming)

H ₂ O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8795 mL	9.3974 mL	18.7949 mL
5 mM	0.3759 mL	1.8795 mL	3.7590 mL
10 mM	0.1879 mL	0.9397 mL	1.8795 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: ≥ 0.6 mg/mL (1.13 mM); Clear solution
2.

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

Solubility: ≥ 0.6 mg/mL (1.13 mM); Clear solution
3.

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

Solubility: ≥ 0.6 mg/mL (1.13 mM); Clear solution
4.

Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

Solubility: ≥ 0.48 mg/mL (0.90 mM); Clear solution
5.

Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)

Solubility: ≥ 0.48 mg/mL (0.90 mM); Clear solution

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