JNJ-40411813

• CAS: 1127498-03-6
• Catalog Number: ACM1127498036
• Category: Others
• Molecular Weight: 344.88
• Molecular Formula: C20H25ClN2O
• Description: JNJ-40411813, also known as ADX71149, is a positive allosteric modulator of the mGlu2 receptor. JNJ-40411813 acts as a PAM at the cloned mGlu2 receptor: EC50 = 147 ± 42 nmol/L in a [(35)S]GTPγS binding assay with human metabotropic glutamate type 2 (hmGlu2) CHO cells and EC50 = 64 ± 29 nmol/L in a Ca(2+) mobilization assay with hmGlu2 G α16 cotransfected HEK293 cells. JNJ-40411813 displaced [(3)H]JNJ-40068782 and [(3)H]JNJ-46281222 (mGlu2 receptor PAMs), while it failed to displace [(3)H]LY341495 (a competitive mGlu2/3 receptor antagonist). JNJ-40411813 is an interesting candidate to explore the therapeutic potential of mGlu2 PAMs, in in vivo rodents experiments as well as in clinical studies.
• Synonyms: JNJ-40411813; JNJ 40411813; JNJ40411813; ADX71149; ADX 71149; ADX-71149
• IUPAC Name: 1-butyl-3-chloro-4-(4-phenyl-1-piperidinyl)-(1H)-pyridone
• Canonical SMILES: ClC1=C(N2CCC(C3=CC=CC=C3)CC2)C=CN(CCCC)C1=O
• InChI: InChI=1S/C20H25ClN2O/c1-2-3-12-23-15-11-18(19(21)20(23)24)22-13-9-17(10-14-22)16-7-5-4-6-8-16/h4-8,11,15,17H,2-3,9-10,12-14H2,1H3
• InChI Key: HYOGJHCDLQSAHX-UHFFFAOYSA-N
• Solubility: Soluble in DMSO
• Appearance: Solid powder
• Shelf Life: >2 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Biological Target: JNJ-40411813 (ADX-71149) is a novel positive allosteric modulator of the metabotropic Glutamate 2 receptor (mGlu2R) with EC50 of 147 nM.
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 69.65; H, 7.31; Cl, 10.28; N, 8.12; O, 4.64
• Exact Mass: 344.1655
• HS Tariff Code: 2934.99.9001
• In Vitro Activity: JNJ-40411813 acts as a PAM at the cloned mGlu2 receptor: EC50 = 147 ± 42 nmol/L in a [(35)S]GTPγS binding assay with human metabotropic glutamate type 2 (hmGlu2) CHO cells and EC50 = 64 ± 29 nmol/L in a Ca(2+) mobilization assay with hmGlu2 G α16 cotransfected HEK293 cells.; Reference: Pharmacol Res Perspect. 2015 Feb;3(1):e00096. https://pubmed.ncbi.nlm.nih.gov/25692015/
• In Vivo Activity: In mice, JNJ-40411813, JNJ-42153605, and LY404039 inhibited spontaneous locomotion and phencyclidine- and scopolamine-induced but not d-amphetamine-induced hyperlocomotion; the 5HT2A antagonist ritanserin inhibited only spontaneous locomotion and phencyclidine-induced hyperlocomotion.; Reference: Pharmacol Res Perspect. 2015 Mar;3(2):e00097. https://pubmed.ncbi.nlm.nih.gov/25692027/
• Shipping: 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.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).