[CAS NO. 1627902-21-9] JNJ-54175446

Name: JNJ-54175446
Brand: Arctom Scientific
SKU: AS941522

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PRODUCTS SPECIFICATIONS [1627902-21-9]

Distributor

Catalog

AS941522

Brand

Arctom Scientific

CAS

1627902-21-9

DESCRIPTION [1627902-21-9]

Overview

MDL	MFCD31556312
Molecular Weight	440.78
Molecular Formula	C18H13ClF4N6O
SMILES	ClC1=C(C=CC=C1C(N2CCC3=C(N=NN3C4=NC=C(F)C=N4)[C@H]2C)=O)C(F)(F)F

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

Summary

JNJ-54175446 is a potent and selective brain penetrant P2X7 receptor antagonist, with pIC ₅₀ s of 8.46 and 8.81 for hP2X7 receptor and rP2X7 receptor, respectively.

IC50 & Target

pIC50: 8.46 (hP2X7 receptor), 8.81 (rP2X7 receptor) ^[1]

In Vitro

JNJ-54175446 (Compound 14) is a potent and selective brain penetrant P2X7 antagonist, with pIC ₅₀ s of 8.46 and 8.81 for hP2X7 and rP2X7, respectively. JNJ-54175446 shows less potent activity against mouse, dog and Macaque P2X7 (pIC ₅₀ , 7.8, 7.9 and 8.1, respectively) ^[1] .

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

In Vivo

JNJ-54175446 shows dose-dependent occupancy with the ED ₅₀ of 0.46 mg/kg, corresponding to plasma EC ₅₀ of 105 ng/mL ^[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
NCT02933762	Janssen Research & Development, LLC	Healthy	September 2016	Phase 1
NCT03088644	Janssen-Cilag International NV	Healthy	March 24, 2017	Phase 1
NCT02930694	Janssen Research & Development, LLC	Healthy	October 2016	Phase 1
NCT04116606	CCTU-Core\|Janssen Pharmaceuticals\|Cambridgeshire and Peterborough NHS Foundation Trust	Depressive Disorder, Major\|Inflammation	September 12, 2019	Phase 2
NCT03058419	Janssen Research & Development, LLC	Healthy	March 14, 2017	Phase 1
NCT02475148	Janssen-Cilag International NV	Healthy	June 2015	Phase 1
NCT02515955	Janssen-Cilag International NV	Healthy	August 2015	Phase 1

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 : 62.5 mg/mL ( 141.79 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2687 mL	11.3435 mL	22.6871 mL
5 mM	0.4537 mL	2.2687 mL	4.5374 mL
10 mM	0.2269 mL	1.1344 mL	2.2687 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 (4.72 mM); Clear solution
2.

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

Solubility: ≥ 2.08 mg/mL (4.72 mM); Clear solution
3.

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

Solubility: ≥ 2.08 mg/mL (4.72 mM); Clear solution

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

References

[1] Letavic MA, et al. 4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate. Send to