Apoptosis
Aminopeptidase
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Product name : KML29
Item : C2501
Price : 200mg, $1250;500mg, $2090; 1g $2995; 2g, $4395
contact : Send inquiry to: info@acesobio.com
CAS : 1380424-42-9
Molecular Weight : 549.42
Formula : C₂₄H₂₁F₆NO₇
Storage : at -20°C
Additional information : We offer significant discount for bulky quantity order.
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| Details: |
Description of:KML29
KML-29(CAS: 1380424-42-9)is monoacylglycerol lipase inhibitor and an O-hexafluoroisopropyl carbamate analog of JZL 184. KML-29 potently and selectively inhibits MAGL (IC50s = 15, 43, and 5.9 nM in mouse, rat, and human brain proteomes, respectively). KML29 with gabapentin synergistically produces analgesia in mice. Quality control data: Quality control by 1H-NMR, 13C-NMR, HPLC and LCMS. Product will be shipped with supporting analytical data. REFERENCES1: Crowe MS, Wilson CD, Leishman E, Prather PL, Bradshaw HB, Banks ML, Kinsey SG. The monoacylglycerol lipase inhibitor KML29 with gabapentin synergistically produces analgesia in mice. Br J Pharmacol. 2017 Dec;174(23):4523-4539. doi: 10.1111/bph.14055. Epub 2017 Nov 20. PubMed PMID: 28963716; PubMed Central PMCID: PMC5715597. 2: Pasquarelli N, Porazik C, Bayer H, Buck E, Schildknecht S, Weydt P, Witting A, Ferger B. Contrasting effects of selective MAGL and FAAH inhibition on dopamine depletion and GDNF expression in a chronic MPTP mouse model of Parkinson's disease. Neurochem Int. 2017 Nov;110:14-24. doi: 10.1016/j.neuint.2017.08.003. Epub 2017 Aug 5. PubMed PMID: 28826718. 3: Pasquarelli N, Engelskirchen M, Hanselmann J, Endres S, Porazik C, Bayer H, Buck E, Karsak M, Weydt P, Ferger B, Witting A. Evaluation of monoacylglycerol lipase as a therapeutic target in a transgenic mouse model of ALS. Neuropharmacology. 2017 Sep 15;124:157-169. doi: 10.1016/j.neuropharm.2017.03.037. Epub 2017 Mar 31. PubMed PMID: 28373073. 4: Morena M, Leitl KD, Vecchiarelli HA, Gray JM, Campolongo P, Hill MN. Emotional arousal state influences the ability of amygdalar endocannabinoid signaling to modulate anxiety. Neuropharmacology. 2016 Dec;111:59-69. doi: 10.1016/j.neuropharm.2016.08.020. Epub 2016 Aug 20. PubMed PMID: 27553121. 5: Miller S, Leishman E, Hu SS, Elghouche A, Daily L, Murataeva N, Bradshaw H, Straiker A. Harnessing the Endocannabinoid 2-Arachidonoylglycerol to Lower Intraocular Pressure in a Murine Model. Invest Ophthalmol Vis Sci. 2016 Jun 1;57(7):3287-96. doi: 10.1167/iovs.16-19356. PubMed PMID: 27333182; PubMed Central PMCID: PMC4961057. 6: Subbanna S, Psychoyos D, Xie S, Basavarajappa BS. Postnatal ethanol exposure alters levels of 2-arachidonylglycerol-metabolizing enzymes and pharmacological inhibition of monoacylglycerol lipase does not cause neurodegeneration in neonatal mice. J Neurochem. 2015 Jul;134(2):276-87. doi: 10.1111/jnc.13120. Epub 2015 Apr 30. PubMed PMID: 25857698; PubMed Central PMCID: PMC4490952. 7: Pasquarelli N, Porazik C, Hanselmann J, Weydt P, Ferger B, Witting A. Comparative biochemical characterization of the monoacylglycerol lipase inhibitor KML29 in brain, spinal cord, liver, spleen, fat and muscle tissue. Neuropharmacology. 2015 Apr;91:148-56. doi: 10.1016/j.neuropharm.2014.12.001. Epub 2014 Dec 12. PubMed PMID: 25497453. 8: Ignatowska-Jankowska BM, Ghosh S, Crowe MS, Kinsey SG, Niphakis MJ, Abdullah RA, Tao Q, O' Neal ST, Walentiny DM, Wiley JL, Cravatt BF, Lichtman AH. In vivo characterization of the highly selective monoacylglycerol lipase inhibitor KML29: antinociceptive activity without cannabimimetic side effects. Br J Pharmacol. 2014 Mar;171(6):1392-407. doi: 10.1111/bph.12298. PubMed PMID: 23848221; PubMed Central PMCID: PMC3954480. |
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