JNJ-47965567 | B2972

JNJ-47965567 is a potent and selective antagonist of the purinergic receptor P2X subtype 7 (P2X7), a ligand-gated ion channel. Activation of P2X receptors by BzATP induces calcium flux. JNJ-47965567 attenuates Bz-ATP induced calcium flux in 1321N1 astrocytoma cells transfected with the recombinant P2X7 proteins with pIC₅₀ values of 8.3, 7.5 and 7.2 for human, mouse and rat receptors respectively. JNJ-47965567 (30 mg/kg for 5 days) significantly reduces spontaneous seizures in epileptic mice even after treatment is stopped.

JNJ-47965567 is a potent and selective antagonist of the purinergic receptor P2X subtype 7 (P2X7), a ligand-gated ion channel. Activation of P2X receptors by BzATP induces calcium flux. JNJ-47965567 attenuates Bz-ATP induced calcium flux in 1321N1 astrocytoma cells transfected with the recombinant P2X7 proteins with pIC₅₀ values of 8.3, 7.5 and 7.2 for human, mouse and rat receptors respectively. JNJ-47965567 (30 mg/kg for 5 days) significantly reduces spontaneous seizures in epileptic mice even after treatment is stopped.

B2972 | JNJ-47965567 DataSheet

Alternate Name/Synonyms: N-[[4-(4-phenylpiperazin-1-yl)oxan-4-yl]methyl]-2-phenylsulfanylpyridine-3-carboxamide; N-((4-(4-phenylpiperazin-1-yl)tetrahydro-2H-pyran-4-yl)methyl)-2-(phenylthio)nicotinamide; 2-(Phenylthio)-N-[[tetrahydro-4-(4-phenyl-1-piperazinyl)-2H-pyran-4-yl]methyl]-3-pyridinecarboxamide; P2X Antagonist III

Appearance: Solid

Formulation:

CAS Number: 1428327-31-4

Structure Available?: True

Peptide sequence:

Salt Form: false

Molecular Formula: C₂₈H₃₂N₄O₂S

Molecular Weight: 488.64

Cell-Permeable?: True

Purity: 98%

Solubilities: ~30 mg/ml in DMSO and DMF in 0, ~12.5 mg/ml in in Ethanol

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: A selective P2X7 antagonist

MDL Number:

PubChem CID: 66553218

SMILES: C1COCCC1(CNC(=O)C2=C(N=CC=C2)SC3=CC=CC=C3)N4CCN(CC4)C5=CC=CC=C5

InChi: InChI=1S/C28H32N4O2S/c33-26(25-12-7-15-29-27(25)35-24-10-5-2-6-11-24)30-22-28(13-20-34-21-14-28)32-18-16-31(17-19-32)23-8-3-1-4-9-23/h1-12,15H,13-14,16-22H2,(H,30,33)

InChi Key: XREFXUCWSYMIOG-UHFFFAOYSA-N