JNJ-46281222

JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positive allosteric modulator) with nanomolar affinity (Kd = 1.7 nM) and a high modulatory potency (pEC50 = 7.71).

Product information

CAS Number: 1254980-38-5

Molecular Weight: 414.47

Formula: C23H25F3N4

Chemical Name: 1-{[3-(cyclopropylmethyl)-8-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridin-7-yl]methyl}-4-phenylpiperidine

Smiles: FC(F)(F)C1C2=NN=C(CC3CC3)N2C=CC=1CN1CCC(CC1)C1C=CC=CC=1

InChiKey: LYDKDODJIBQNLK-UHFFFAOYSA-N

InChi: InChI=1S/C23H25F3N4/c24-23(25,26)21-19(10-13-30-20(14-16-6-7-16)27-28-22(21)30)15-29-11-8-18(9-12-29)17-4-2-1-3-5-17/h1-5,10,13,16,18H,6-9,11-12,14-15H2

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 62.5 mg/mL (150.79 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

JNJ‐4628122 binds to the selected mGlu2 receptor mutants is significantly decreased by approximately 10‐fold compared with WT, in transfected mGlu2 WT and mutant receptors in CHO‐K1 cells, mutations F643A and N735D are selected.

References:

1. Doornbos ML,et al. Molecular mechanism of positive allosteric modulation of the metabotropic glutamate receptor 2 by JNJ-46281222.Br J Pharmacol. 2016 Feb;173(3):588-600.

Products are for research use only. Not for human use.