KT172 |
| Katalog-Nr.GC45491 |
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1402612-56-9
Sample solution is provided at 25 µL, 10mM.
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KT172 is a non-selective inhibitor of diacylglycerol lipase α (DAGLα) and DAGLβ.1 It inhibits DAGL-mediated hydrolysis of 1-stearoyl-2-arachidonoylglycerol in HEK293T cell membranes expressing recombinant DAGLα or DAGLβ (IC50s = 140 and 60 nM, respectively). KT172 also inhibits α/β-hydrolase 6 (ABHD6; IC50 = 5 nM) and weakly inhibits monoacylglycerol lipase (MAGL; IC50 = 5,000 nM) in a panel of 47 mouse serine hydrolases. It restores nicotine-stimulated GABA release in isolated ventral tegmental area (VTA) dopamine neurons from rats chronically exposed to nicotine when used at a concentration of 1 μM.2 KT172 decreases production of 2-arachidonoyl glycerol and subsequently reduces arachidonic acid , prostaglandin E2 , and PGD2 in thioglycolate-stimulated peritoneal macrophages when administered at a dose of 5 mg/kg in mice.1
References
1. Hsu, K.L., Tsuboi, K., Adibekian, A., et al. DAGLβ inhibition perturbs a lipid network involved in macrophage inflammatory responses. Nature Chemical Biology 8(12), 999-1007 (2012).
2. Buczynski, M.W., Herman, M.A., Hsu, K.L., et al. Diacylglycerol lipase disinhibits VTA dopamine neurons during chronic nicotine exposure. Proc. Natl. Acad. Sci. U.S.A. 113(4), 1086-1091 (2016).
| Cas No. | 1402612-56-9 | SDF | |
| Canonical SMILES | O=C(N1N=NC(C2=CC=C(C3=C(OC)C=CC=C3)C=C2)=C1)N4C(CC5=CC=CC=C5)CCCC4 | ||
| Formula | C28H28N4O2 | M.Wt | 452.6 |
| Löslichkeit | DMF: 5mg/mL,DMSO: 10mg/mL,DMSO:PBS (pH 7.2) (1:2): 0.25mg/mL | 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. |
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| 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 | 2.2095 mL | 11.0473 mL | 22.0946 mL |
| 5 mM | 0.4419 mL | 2.2095 mL | 4.4189 mL |
| 10 mM | 0.2209 mL | 1.1047 mL | 2.2095 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 28 reference(s) in Google Scholar.)
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