[CAS NO. 1902114-15-1] PC786

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PRODUCTS SPECIFICATIONS [1902114-15-1]

Catalog

HY-102038

Brand

MCE

CAS

1902114-15-1

DESCRIPTION [1902114-15-1]

Overview

MDL	-
Molecular Weight	715.83
Molecular Formula	C41H38FN5O4S
SMILES	O=C(C(S1)=CC2=C1C3=CC=CC=C3N(C(C4=CC=C(NC(C5=CC(C)=CN=C5N6CC7(CCOCC7)C6)=O)C=C4)=O)CC2)NC8=C(C)C=CC=C8F

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

Summary

PC786 is an inhaled respiratory syncytial virus ( RSV ) L protein polymerase inhibitor. PC786 demonstrates potent antiviral activity against RSV-A ( IC ₅₀ <0.09 to 0.71 nM) and RSV-B ( IC ₅₀ , 1.3 to 50.6 nM) ^[1] .

In Vitro

PC786 demonstrates a potent and selective antiviral activity against laboratory-adapted or clinical isolates of RSV-A (IC ₅₀ <0.09 to 0.71 nM) and RSV-B (IC ₅₀ , 1.3 to 50.6 nM), which are determined by inhibition of cytopathic effects in HEp-2 cells without causing detectable cytotoxicity. PC786 inhibits RSV A2 activity, exhibiting an IC ₅₀ and IC ₉₀ of 0.50±0.0014 nM and 0.63±0.035 nM, respectively. PC786 inhibits RSV B WST activity, exhibiting an IC ₅₀ and IC ₉₀ of 27.3±0.77 nM and 57.1±3.87 nM, respectively. PC786 exhibits potent inhibition of cytopathic effect (CPE) induced by known RSV A clinical isolates (IC ₅₀ , 0.14 to 3.2 nM). PC786 also exhibits potent inhibition of CPE induced by various low-passage-number clinical isolates of RSV A (IC ₅₀ , 0.42 nM [median]) and RSV B (IC ₅₀ , 17.5 nM [median]) ^[1] .

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

In Vivo

Once-daily treatment with PC786, on days-1 to 3, by either intratracheal (i.t.) or intranasal (i.n.) administration, is found to inhibit viral loads in the lungs of RSV A2-infected BALB/c mice. The viral load is below the level of detection when the drug is given at 2 mg/mL (40 μg/mouse [approximately 1.6 mg/kg of body weight] for i.t. treatment, or 80 μg/mouse [approximately 3.2 mg/kg] for i.n. treatment) ^[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
NCT03236233	Pulmocide Ltd	Respiratory Syncytial Virus (RSV)	June 21, 2017	Phase 1
NCT03715023	Pulmocide Ltd	Respiratory Syncytial Virus Infections	November 5, 2018	Phase 2
NCT03382431	Pulmocide Ltd	Respiratory Syncytial Virus Infections	November 14, 2017	Phase 1\|Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 130 mg/mL ( 181.61 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.3970 mL	6.9849 mL	13.9698 mL
5 mM	0.2794 mL	1.3970 mL	2.7940 mL
10 mM	0.1397 mL	0.6985 mL	1.3970 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: 3.25 mg/mL (4.54 mM); Suspended solution; Need ultrasonic
2.

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

Solubility: 3.25 mg/mL (4.54 mM); Suspended solution; Need ultrasonic
3.

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

Solubility: ≥ 3.25 mg/mL (4.54 mM); Clear solution

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

References

[1] Coates M, et al. Preclinical Characterization of PC786, an Inhaled Small-Molecule Respiratory Syncytial Virus L Protein Polymerase Inhibitor. Antimicrob Agents Chemother. 2017 Aug 24;61(9). pii: e00737-17.