LY-2940094 tartrate (Synonyms: LY-2940094; LY2940094; LY 2940094 ) |
| Catalog No.GC19464 |
Le tartrate LY2940094 (BTRX-246040) est un antagoniste des récepteurs du peptide N/OFQ (NOP) puissant, pénétrant dans le cerveau, sélectif et disponible par voie orale avec une affinité élevée (Ki \u003d 0,105 nM) et une puissance antagoniste (Kb \u003d 0,166 nM).
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Synonymes | LY-2940094; LY2940094; LY 2940094 | ||
| Chemical Name | (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 | ||
| Formula | C6H29ClF2N4O8S | M.Wt | 631.0448 |
| Solubility | DMSO : 41.67 mg/mL (86.64 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5847 mL | 7.9234 mL | 15.8467 mL |
| 5 mM | 316.9 μL | 1.5847 mL | 3.1693 mL |
| 10 mM | 158.5 μL | 792.3 μL | 1.5847 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)
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