KML29
CAS No. 1380424-42-9
KML29( KML-29 | KML29 | KML 29 )
Catalog No. M17269 CAS No. 1380424-42-9
KML29 is highly selective and effective monoacylglycerol lipase (MAGL) inhibitor.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 43 | In Stock |
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| 10MG | 73 | In Stock |
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| 25MG | 158 | In Stock |
|
| 50MG | 231 | In Stock |
|
| 100MG | 341 | In Stock |
|
| 500MG | 803 | In Stock |
|
| 1G | Get Quote | In Stock |
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Biological Information
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Product NameKML29
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NoteResearch use only, not for human use.
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Brief DescriptionKML29 is highly selective and effective monoacylglycerol lipase (MAGL) inhibitor.
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DescriptionKML29 is highly selective and effective monoacylglycerol lipase (MAGL) inhibitor. It has effective inhibition of human/mouse/rat MAGL (IC50: 5.9/15/43 nM). It has not inhibitory for FAAH (IC50 > 50 μM). It also effectively and selectively blocks hydrolysis of 2-arachidonoylglycerol (2-AG) in mice (IC50: 2.5 nM, 2-AG; >50 μM, AEA).
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In VitroKML29 dose-dependently elevates brain 2-AG level up to10-fold without alteration in brain levels of anandamide, palmitoylethanolamide, and oleoylethanolamide.KML29 is a potent inhibitor of 2-AG hydrolysis, but did not affect AEA hydrolysis at any concentration tested.
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In VivoKML29 enhibits antinociceptive activity without cannabimimetic side effects.KML29 (20 mg/kg) has a significant but modest protective effectagainst LPS-induced fever. Animal Model:C57Bl/6 mice.Dosage:1-40 mg/kg. Administration:P.O. single dose.Result:Selectively inhibited MAGL in mice.Animal Model:Wistar albino male rats.Dosage:20 mg/kg (+LPS E. coli O111:B4 (250 μg/kg, sc)).Administration:SC.Result:Administration of KML29 simultaneously with LPS E. coli O111:B4 significantly decreased ?T (with 5% type 1 error, 1.7 fold) compared to saline+LPS E. coli O111:B4. Administration of KML29 simultaneously with LPS E. coli O111:B4 resulted in decreased plateau phase of fever compared to LPS E. E. coli O111:B4+saline administration.
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SynonymsKML-29 | KML29 | KML 29
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PathwayNeuroscience
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TargetGluR
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RecptorMAGL
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Research AreaNeurological Disease
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Indication——
Chemical Information
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CAS Number1380424-42-9
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Formula Weight549.42
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Molecular FormulaC24H21F6NO7
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Purity>98% (HPLC)
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SolubilityDMSO : 50 mg/mL. 91.01 mM; H2O : < 0.1 mg/mL
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SMILESO=C(OC(C(F)(F)F)C(F)(F)F)N1CCC(C(c2ccc3OCOc3c2)(O)c2cc3OCOc3cc2)CC1
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Chemical Name1,1,1,3,3,3-hexafluoropropan-2-yl 4-(bis(benzo[d][1,3]dioxol-5-yl)(hydroxy)methyl)piperidine-1-carboxylate
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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GYKI 52466 dihydroch...
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Basimglurant
Basimglurant is a potent, selective and orally available modulator of mGlu5 negative allosteric(Kd of 1.1 nM). In competition binding experiments on human recombinant mGlu5, Basimglurant (RG7090) fully displaces [3H]-MPEP with a Ki of 35.6 nM and [3H]-ABP688 with a Ki of 1.4 nM. In HEK293 cells stably expressing human mGlu5, Basimglurant (RG7090) inhibits quisqualate induced Ca2+ mobilization with an IC50 of 7.0 nM and [3H]-inositolphosphate accumulation (IC50 of 5.9 nM).
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