WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 530650
Description: JNJ-42253432 is a potent and selective central nervous system-penetrant P2X7 antagonist. JNJ-42253432 occupied the brain P2X7 channel with an ED50 of 0.3 mg/kg, corresponding to a mean plasma concentration of 42 ng/ml. JNJ-42253432 blocked the release of IL-1β induced by Bz-ATP in freely moving rat brain. At higher doses/exposure, JNJ-42253432 also increased serotonin levels in the rat brain, which is due to antagonism of the serotonin transporter (SERT) resulting in an ED50 of 10 mg/kg for SERT occupancy. JNJ-42253432 reduced electroencephalography spectral power in the α-1 band in a dose-dependent manner; the compound also attenuated amphetamine-induced hyperactivity. JNJ-42253432 significantly increased both overall social interaction and social preference, an effect that was independent of stress induced by foot-shock.
MedKoo Cat#: 530650
Chemical Formula: C28H38N4O
Exact Mass: 446.3046
Molecular Weight: 446.639
Elemental Analysis: C, 75.30; H, 8.58; N, 12.54; O, 3.58
This product is not in stock, which may be available by custom synthesis.
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Synonym: JNJ-42253432; JNJ 42253432; JNJ42253432.
IUPAC/Chemical Name: 2-methyl-N-([1-(4-phenylpiperazin-1-yl)cyclohexyl]methyl)-1,2,3,4-tetrahydroisoquinoline-5-carboxamide
InChi Key: DIKKTLPJDURHSW-UHFFFAOYSA-N
InChi Code: InChI=1S/C28H38N4O/c1-30-16-13-25-23(21-30)9-8-12-26(25)27(33)29-22-28(14-6-3-7-15-28)32-19-17-31(18-20-32)24-10-4-2-5-11-24/h2,4-5,8-12H,3,6-7,13-22H2,1H3,(H,29,33)
SMILES Code: O=C(C1=CC=CC2=C1CCN(C)C2)NCC3(N4CCN(C5=CC=CC=C5)CC4)CCCCC3
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 446.639 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|