| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
KML-29 is monoacylglycerol lipase inhibitor and an O-hexafluoroisopropyl carbamate analogue 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.
| ln Vitro |
KML29 dose-dependently raises brain 2-AG levels up to ten times without changing anandamide, palmitoylethanolamide, or oleoylethanolamide levels in the brain [2]. KML29 is a strong inhibitor of the hydrolysis of 2-AG, whereas it has no effect on the hydrolysis of AEA at any tested concentration [2].
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| ln Vivo |
KML29 prevents the analgesic effect without causing adverse effects similar to cannabis [3]. The preventive effect of KML29 (20 mg/kg) against fever produced by LPS is considerable but moderate [3].
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| Animal Protocol |
Animal/Disease Models: C57Bl/6 mice[2].
Doses: 1-40 mg/kg. Route of Administration: PO single dose. Experimental Results: Selective inhibition of MAGL in mice. Animal/Disease Models: Wistar albino male rat [2]. Doses: 20 mg/kg (+LPS E. coli O111:B4 (250 µg/kg, SC)). Management: SC. Experimental Results: Simultaneous administration of KML29 and LPS E. coli O111:B4 Dramatically diminished ΔT (Type 1 error 5%, 1.7-fold) compared to saline + LPS E. coli O111:B4. Coadministration of KML29 with LPS E. coli O111:B4 resulted in a reduction in the fever plateau compared with administration of LPS EE E. coli O111:B4 + saline. |
| References |
[1]. Natsuo Ueda, et al. Discrimination between two endocannabinoids. Chem Biol. 2012 May 25;19(5):545-7.
[2]. Jae Won Chang, et al. Highly selective inhibitors of monoacylglycerol lipase bearing a reactive group that is bioisosteric with endocannabinoid substrates. Chem Biol. 2012 May 25;19(5):579-88. [3]. B M Ignatowska-Jankowska, et al. 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. |
| Molecular Formula |
C24H21F6NO7
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|---|---|
| Molecular Weight |
549.4224
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| Exact Mass |
549.1222
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| CAS # |
1380424-42-9
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| Related CAS # |
1380424-42-9
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| SMILES |
FC(C([H])(C(F)(F)F)OC(N1C([H])([H])C([H])([H])C([H])(C([H])([H])C1([H])[H])C(C1C([H])=C([H])C2=C(C=1[H])OC([H])([H])O2)(C1C([H])=C([H])C2=C(C=1[H])OC([H])([H])O2)O[H])=O)(F)F
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| InChi Key |
SXHQLPHDBLTFPM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H21F6NO7/c25-23(26,27)20(24(28,29)30)38-21(32)31-7-5-13(6-8-31)22(33,14-1-3-16-18(9-14)36-11-34-16)15-2-4-17-19(10-15)37-12-35-17/h1-4,9-10,13,20,33H,5-8,11-12H2 SMILES
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| Chemical Name |
1,1,1,3,3,3-hexafluoropropan-2-yl 4-(bis(benzo[d][1,3]dioxol-5-yl)(hydroxy)methyl)piperidine-1-carboxylate
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| Synonyms |
KML-29 KML29 KML 29.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~91.01 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.55 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.55 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8201 mL | 9.1005 mL | 18.2010 mL | |
| 5 mM | 0.3640 mL | 1.8201 mL | 3.6402 mL | |
| 10 mM | 0.1820 mL | 0.9101 mL | 1.8201 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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