JNJ-8003

Cat. No.: HY-149648 Purity: 99.84%: Data Sheet
COA

SDS
Handling Instructions
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JNJ-8003 is a potent and orally active non-nucleoside RSV polymerase inhibitor with an IC₅₀ of 0.29 nM. JNJ-8003 targets the L protein polymerase complex of RSV (IC₅₀ = 0.67 nM), and blocks the transcription and replication of the viral genome by inhibiting the activity of RNA-dependent RNA polymerase (RdRp). JNJ-8003 displays subnanomolar activity in vitro as well as prominent efficacy in mice and a neonatal lamb models. JNJ-8003 can be used for the study of respiratory syncytial virus (RSV).

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

JNJ-8003 Chemical Structure

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Description

In Vitro

JNJ-8003 (5 μM) inhibits RVS RNA replication and transcription at the initiation and early elongation stage^[1].
JNJ-8003 exhibits significant anti-RSV activity at the cellular level (HeLa cells) with an EC₅₀ of 0.82 nM and shows cytotoxicity against Hela cells with a CC₅₀ of 27.7 μM^[2].

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

Parmacokinetics^[1]

Species	Dose	Route	Indicator	value
Dog	0.5 mg/kg	i.v.	CL	5.62 mL/min/kg
Dog	0.5 mg/kg	p.o.	C_max	249 ng/mL
Mice	10 mg/kg	p.o.	C_max	1727 ng/mL
Mice	2.5 mg/kg	i.v.	CL	10.6 mL/min/kg
Rat	1.25 mg/kg	i.v.	CL	8.03 mL/min/kg
Rat	5 mg/kg	p.o.	C_max	401 ng/mL
Dog	0.5 mg/kg	i.v.	T_1/2	4.25 h
Dog	0.5 mg/kg	p.o.	AUC_0-last	1200 ng·h/mL
Mice	10 mg/kg	p.o.	AUC_0-last	9578 ng·h/mL
Mice	2.5 mg/kg	i.v.	T_1/2	1.95 h
Rat	1.25 mg/kg	i.v.	T_1/2	3.15 h
Rat	5 mg/kg	p.o.	AUC_0-last	2097 ng·h/mL
Dog	0.5 mg/kg	i.v.	V_dss	1.49 L/kg
Dog	0.5 mg/kg	p.o.	F	81 %
Mice	10 mg/kg	p.o.	F	61 %
Mice	2.5 mg/kg	i.v.	V_dss	1.68 L/kg
Rat	1.25 mg/kg	i.v.	V_dss	1.04 L/kg
Rat	5 mg/kg	p.o.	F	20 %

In Vivo

JNJ-8003 (0.25-100 mg/kg, p.o., once daily for 4-5 days) shows outstanding Efficacy in RSV mouse and neonatal lamb models^[2].

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

Animal Model:	RSV-A2 infection model established in 6-8 week old female BALB/c mice (Janvier)^[2]
Dosage:	1, 4, 10, 40, 100 mg/kg
Administration:	Oral administration (p.o.), once daily for 4 days
Result:	Dose-dependently inhibited virus, with viral titers dropping below the detection limit at doses of 10 mg/kg and above.

Animal Model:	RSV M37 infection model established in lamb (from LambCure)^[2]
Dosage:	0.25, 1, 4 mg/kg
Administration:	Oral administration (p.o.), once daily for 5 days
Result:	Decreased the lung virus titer below the detection limit at 4 mg/kg. Completed resolution of lung inflammation and lesions (H&E scores returned to normal).

Molecular Weight

576.51

Formula

C₂₈H₂₅F₅N₄O₄

Appearance

Solid

Color

Off-white to light yellow

SMILES

CC(N=N1)=CC2=C1C(OC)=CC(C(NC[C@](C(F)(F)F)(O)C3=CC(C(C)(C)O)=C(F)C(C4=CC=C(F)C=C4)=N3)=O)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (216.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7346 mL	8.6729 mL	17.3458 mL
5 mM	0.3469 mL	1.7346 mL	3.4692 mL
10 mM	0.1735 mL	0.8673 mL	1.7346 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.84%

Select Batch:

Data Sheet (277 KB) SDS (251 KB)

COA (253 KB) HNMR (284 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Yu X, et al. Structural and mechanistic insights into the inhibition of respiratory syncytial virus polymerase by a non-nucleoside inhibitor. Commun Biol. 2023 Oct 21;6(1):1074. [Content Brief]

[2]. Grosse S, et al. Discovery of gem-Dimethyl-hydroxymethylpyridine Derivatives as Potent Non-nucleoside RSV Polymerase Inhibitors. J Med Chem. 2024 Aug 22;67(16):13723-13736. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7346 mL	8.6729 mL	17.3458 mL	43.3644 mL
	5 mM	0.3469 mL	1.7346 mL	3.4692 mL	8.6729 mL
	10 mM	0.1735 mL	0.8673 mL	1.7346 mL	4.3364 mL
	15 mM	0.1156 mL	0.5782 mL	1.1564 mL	2.8910 mL
	20 mM	0.0867 mL	0.4336 mL	0.8673 mL	2.1682 mL
	25 mM	0.0694 mL	0.3469 mL	0.6938 mL	1.7346 mL
	30 mM	0.0578 mL	0.2891 mL	0.5782 mL	1.4455 mL
	40 mM	0.0434 mL	0.2168 mL	0.4336 mL	1.0841 mL
	50 mM	0.0347 mL	0.1735 mL	0.3469 mL	0.8673 mL
	60 mM	0.0289 mL	0.1445 mL	0.2891 mL	0.7227 mL
	80 mM	0.0217 mL	0.1084 mL	0.2168 mL	0.5421 mL
	100 mM	0.0173 mL	0.0867 mL	0.1735 mL	0.4336 mL

JNJ-8003 Related Classifications

Infection

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JNJ-8003JNJ8003JNJ 8003RSVDNA/RNA SynthesisRespiratory syncytial virusRSV Polymerase InhibitorRespiratory syncytial virus polymeraseNon-nucleoside InhibitorInhibitorinhibitorinhibit

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JNJ-8003

JNJ-8003 Related Antibodies

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