LY-2940094 tartrate
(Synonyms: LY-2940094; LY2940094; LY 2940094 ) 目录号 : GC19464
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)。
Cas No.:1307245-87-9
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 1307245-87-9 | SDF | |
| 别名 | LY-2940094; LY2940094; LY 2940094 | ||
| 化学名 | (2-(4-((2'-chloro-4',4'-difluoro-4',5'-dihydrospiro[piperidine-4,7'-thieno[2,3-c]pyran]-1-yl)methyl)-3-methyl-1H-pyrazol-1-yl)pyridin-3-yl)methanol (2R,3R)-2,3-dihydroxysuccinate | ||
| Canonical SMILES | OCC1=CC=CN=C1N2N=C(C)C(CN3CCC4(C5=C(C=C(Cl)S5)C(F)(F)CO4)CC3)=C2.O=C(O)[C@H](O)[C@@H](O)C(O)=O | ||
| 分子式 | C6H29ClF2N4O8S | 分子量 | 631.0448 |
| 溶解度 | DMSO : 41.67 mg/mL (86.64 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5847 mL | 7.9234 mL | 15.8467 mL |
| 5 mM | 0.3169 mL | 1.5847 mL | 3.1693 mL |
| 10 mM | 0.1585 mL | 0.7923 mL | 1.5847 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet