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  • LY-2940094 tartrate
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LY-2940094 tartrate

LY2940094 (BTRX-246040) tartrate 是一种有效的、脑渗透性、选择性和可口服的 N/OFQ 肽 (NOP) 受体拮抗剂,具有高亲和力 (Ki\u003d0.105 nM) 和拮抗效力 (Kb\u003d0.166 nM)。

原价
¥1525-9062
价格
1220-7250
LY-2940094 tartrate的二维码

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  • 货号: ajci23170
  • CAS: 1307245-87-9
  • 别名: LY-2940094; LY2940094; LY 2940094
  • 分子式: C6H29ClF2N4O8S
  • 分子量: 631.0448
  • 纯度: >98%
  • 溶解度: DMSO : 41.67 mg/mL (86.64 mM)
  • 储存: Store at -20°C
  • 库存: 现货

Background

LY-2940094 is a nociceptin receptor antagonist potentially for the treatment of major depressive disorder and alcoholism.


Reference:
?1: Post A, Smart TS, Jackson K, Mann J, Mohs R, Rorick-Kehn L, Statnick M, Anton R, O'Malley SS, Wong CJ. Proof-of-Concept Study to Assess the Nociceptin Receptor Antagonist LY2940094 as a New Treatment for Alcohol Dependence. Alcohol Clin Exp Res. 2016 Sep;40(9):1935-44. doi: 10.1111/acer.13147. PubMed PMID: 27435979.
2: Witkin JM, Rorick-Kehn LM, Benvenga MJ, Adams BL, Gleason SD, Knitowski KM, Li X, Chaney S, Falcone JF, Smith JW, Foss J, Lloyd K, Catlow JT, McKinzie DL, Svensson KA, Barth VN, Toledo MA, Diaz N, Lafuente C, Jiménez A, Benito A, Pedregal C, Martínez-Grau MA, Post A, Ansonoff MA, Pintar JE, Statnick MA. Preclinical findings predicting efficacy and side-effect profile of LY2940094, an antagonist of nociceptin receptors. Pharmacol Res Perspect. 2016 Nov 7;4(6):e00275. doi: 10.1002/prp2.275. PubMed PMID: 28097008; PubMed Central PMCID: PMC5226289.
3: Statnick MA, Chen Y, Ansonoff M, Witkin JM, Rorick-Kehn L, Suter TM, Song M, Hu C, Lafuente C, Jiménez A, Benito A, Diaz N, Martínez-Grau MA, Toledo MA, Pintar JE. A Novel Nociceptin Receptor Antagonist LY2940094 Inhibits Excessive Feeding Behavior in Rodents: A Possible Mechanism for the Treatment of Binge Eating Disorder. J Pharmacol Exp Ther. 2016 Feb;356(2):493-502. doi: 10.1124/jpet.115.228221. PubMed PMID: 26659925.
4: Raddad E, Chappell A, Meyer J, Wilson A, Ruegg CE, Tauscher J, Statnick MA, Barth V, Zhang X, Verfaille SJ. Occupancy of Nociceptin/Orphanin FQ Peptide Receptors by the Antagonist LY2940094 in Rats and Healthy Human Subjects. Drug Metab Dispos. 2016 Sep;44(9):1536-42. doi: 10.1124/dmd.116.070359. PubMed PMID: 27353045.
5: Rorick-Kehn LM, Ciccocioppo R, Wong CJ, Witkin JM, Martinez-Grau MA, Stopponi S, Adams BL, Katner JS, Perry KW, Toledo MA, Diaz N, Lafuente C, Jiménez A, Benito A, Pedregal C, Weiss F, Statnick MA. A Novel, Orally Bioavailable Nociceptin Receptor Antagonist, LY2940094, Reduces Ethanol Self-Administration and Ethanol Seeking in Animal Models. Alcohol Clin Exp Res. 2016 May;40(5):945-54. doi: 10.1111/acer.13052. PubMed PMID: 27084498; PubMed Central PMCID: PMC4844902.
6: Post A, Smart TS, Krikke-Workel J, Dawson GR, Harmer CJ, Browning M, Jackson K, Kakar R, Mohs R, Statnick M, Wafford K, McCarthy A, Barth V, Witkin JM. A Selective Nociceptin Receptor Antagonist to Treat Depression: Evidence from Preclinical and Clinical Studies. Neuropsychopharmacology. 2016 Jun;41(7):1803-12. doi: 10.1038/npp.2015.348. PubMed PMID: 26585287; PubMed Central PMCID: PMC4869049.

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