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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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G610690-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $922.90 | |
G610690-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $4,000.90 |
Synonyms | GSK-1521498|1007573-18-3|GSK1521498|GSK1521498 (free base)|W0UTB622GK|GSK1521498 free base|[1,1'-Biphenyl]-4-methanamine, N-(2,3-dihydro-1H-inden-2-yl)-3,5-difluoro-3'-(1H-1,2,4-triazol-5-yl)-|1007573-18-3 (free base)|N-((3,5-Difluoro-3'-(1H-1,2,4-triazol |
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Grade | Moligand™ |
Action Type | ANTAGONIST |
Mechanism of action | Mu opioid receptor antagonist |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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INCHI | InChI=1S/C24H20F2N4/c25-22-11-19(15-6-3-7-18(8-15)24-28-14-29-30-24)12-23(26)21(22)13-27-20-9-16-4-1-2-5-17(16)10-20/h1-8,11-12,14,20,27H,9-10,13H2,(H,28,29,30) |
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InChi Key | WIEDUMBCZQRGSY-UHFFFAOYSA-N |
Canonical SMILES | Fc1cc(cc(c1CNC1Cc2c(C1)cccc2)F)c1cccc(c1)c1ncn[nH]1 |
Isomeric SMILES | C1C(CC2=CC=CC=C21)NCC3=C(C=C(C=C3F)C4=CC(=CC=C4)C5=NC=NN5)F |
PubChem CID | 24737629 |
PubChem CID | 24737629 |
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GPCRdb Ligand | GSK1521498 |
Enter Lot Number to search for COA:
1. Rabiner EA, Beaver J, Makwana A, Searle G, Long C, Nathan PJ, Newbould RD, Howard J, Miller SR, Bush MA et al.. (2011) Pharmacological differentiation of opioid receptor antagonists by molecular and functional imaging of target occupancy and food reward-related brain activation in humans.. Mol Psychiatry, 16 (8): (826-35, 785). [PMID:21502953] |
2. Nathan PJ, O'Neill BV, Bush MA, Koch A, Tao WX, Maltby K, Napolitano A, Brooke AC, Skeggs AL, Herman CS et al.. (2012) Opioid receptor modulation of hedonic taste preference and food intake: a single-dose safety, pharmacokinetic, and pharmacodynamic investigation with GSK1521498, a novel μ-opioid receptor inverse agonist.. J Clin Pharmacol, 52 (4): (464-74). [PMID:21610207] |
3. Ignar DM, Goetz AS, Noble KN, Carballo LH, Stroup AE, Fisher JC, Boucheron JA, Brainard TA, Larkin AL, Epperly AH et al.. (2011) Regulation of ingestive behaviors in the rat by GSK1521498, a novel micro-opioid receptor-selective inverse agonist.. J Pharmacol Exp Ther, 339 (1): (24-34). [PMID:21712426] |
4. Nathan PJ, Bush MA, Tao WX, Koch A, Davies KM, Maltby K, O'Neill BV, Napolitano A, Skeggs AL, Brooke AC et al.. (2012) Multiple-dose safety, pharmacokinetics, and pharmacodynamics of the μ-opioid receptor inverse agonist GSK1521498.. J Clin Pharmacol, 52 (10): (1456-67). [PMID:22162534] |
5. Ziauddeen H, Chamberlain SR, Nathan PJ, Koch A, Maltby K, Bush M, Tao WX, Napolitano A, Skeggs AL, Brooke AC et al.. (2013) Effects of the mu-opioid receptor antagonist GSK1521498 on hedonic and consummatory eating behaviour: a proof of mechanism study in binge-eating obese subjects.. Mol Psychiatry, 18 (12): (1287-93). [PMID:23147384] |
6. Kelly E, Mundell SJ, Sava A, Roth AL, Felici A, Maltby K, Nathan PJ, Bullmore ET, Henderson G. (2015) The opioid receptor pharmacology of GSK1521498 compared to other ligands with differential effects on compulsive reward-related behaviours.. Psychopharmacology (Berl.), 232 (1): (305-14). [PMID:24973897] |
7. Ziauddeen H, Nestor LJ, Subramaniam N, Dodds C, Nathan PJ, Miller SR, Sarai BK, Maltby K, Fernando D, Warren L et al.. (2016) Opioid Antagonists and the A118G Polymorphism in the μ-Opioid Receptor Gene: Effects of GSK1521498 and Naltrexone in Healthy Drinkers Stratified by OPRM1 Genotype.. Neuropsychopharmacology, 41 (11): (2647-57). [PMID:27109624] |
8. Giuliano C, Goodlett CR, Economidou D, García-Pardo MP, Belin D, Robbins TW, Bullmore ET, Everitt BJ. (2015) The Novel μ-Opioid Receptor Antagonist GSK1521498 Decreases Both Alcohol Seeking and Drinking: Evidence from a New Preclinical Model of Alcohol Seeking.. Neuropsychopharmacology, 40 (13): (2981-92). [PMID:26044906] |
9. Ripley TL, Sanchez-Roige S, Bullmore ET, Mugnaini M, Maltby K, Miller SR, Wille DR, Nathan P, Stephens DN. (2015) The novel mu-opioid antagonist, GSK1521498, reduces ethanol consumption in C57BL/6J mice.. Psychopharmacology (Berl.), 232 (18): (3431-41). [PMID:26141191] |