| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
ABHD6 (α/β-hydrolase domain-containing protein 6). ABHD6 is a serine hydrolase that hydrolyzes the endocannabinoid 2-arachidonoylglycerol (2-AG). KT185 is a selective ABHD6 inhibitor. The compound is orally bioavailable and brain-penetrant.
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|---|---|
| ln Vitro |
KT185 inhibits ABHD6 with an IC50 of 0.21 nM in a competitive activity-based protein profiling assay using Neuro2A membranes. It shows exceptional potency. By blocking ABHD6 activity, KT185 enhances endocannabinoid signaling through elevated 2-AG levels.
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| ln Vivo |
KT185 is an orally bioavailable and brain-penetrant ABHD6 inhibitor. It has potential for studying neuroinflammation, pain modulation, and metabolic regulation in vivo. Detailed in vivo activity data in animal models has not been extensively reported in the available literature.
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| Enzyme Assay |
ABHD6 activity-based protein profiling (ABPP) assay: Neuro2A cell membranes are incubated with varying concentrations of KT185 and a fluorescent activity-based probe (e.g., fluorophosphonate-rhodamine or a serine hydrolase-directed probe) that labels active ABHD6. The reaction is carried out at room temperature for 30-60 min. Proteins are separated by SDS-PAGE and fluorescently labeled ABHD6 is detected by in-gel fluorescence scanning. IC50 values are calculated from competition curves.
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| Cell Assay |
2-AG hydrolysis assay: Recombinant ABHD6 or cell lysates containing ABHD6 are incubated with varying concentrations of KT185 and 2-AG substrate in assay buffer at 37°C for 30-60 min. The reaction is terminated, and the amount of arachidonic acid or glycerol released is measured by LC-MS/MS or a coupled enzyme assay. IC50 values are calculated.
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| Animal Protocol |
No in vivo animal experimental protocols have been published for KT185 in the available literature. In vivo studies would typically involve mouse models of neuroinflammation, pain, or metabolic disorders, where KT185 would be administered orally (due to its oral bioavailability and brain penetration), followed by measurement of 2-AG levels, behavioral endpoints, and biochemical markers.
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| ADME/Pharmacokinetics |
KT185 is orally bioavailable and brain-penetrant. It shows exceptional potency with an IC50 of 0.21 nM. Comprehensive PK parameters such as half-life, Cmax, AUC, and plasma protein binding have been characterized in preclinical studies. The compound has a molecular weight of 519.64 g/mol.
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| Toxicity/Toxicokinetics |
No detailed toxicity data has been published in the available literature. KT185 is for research use only. Standard laboratory safety practices should be followed when handling this compound. As an ABHD6 inhibitor that enhances endocannabinoid signaling, potential effects on neurological and metabolic functions should be considered.
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| References | |
| Additional Infomation |
KT185 is an orally bioavailable, brain-penetrant, and selective ABHD6 inhibitor with an IC50 of 0.21 nM. It enhances endocannabinoid signaling by elevating 2-AG levels. The compound is a research tool for studying neuroinflammation, pain modulation, and metabolic regulation. No clinical trials or approved上市 status have been reported.
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| Molecular Formula |
C32H33N5O2
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|---|---|
| Molecular Weight |
519.63672709465
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| Exact Mass |
519.263
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| CAS # |
1472640-86-0
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| PubChem CID |
53364498
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| Appearance |
White to off-white solid powder
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| LogP |
5.5
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
39
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| Complexity |
817
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C(C2C=CC=CC=2)N(C(=O)N2C=C(C3C=CC(C4C=C(C(=O)N5CCCCC5)C=CC=4)=CC=3)N=N2)CCC1
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| InChi Key |
SGQNTNACVSWXMA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H33N5O2/c38-31(35-19-6-2-7-20-35)28-13-9-12-27(22-28)24-15-17-25(18-16-24)29-23-37(34-33-29)32(39)36-21-8-5-14-30(36)26-10-3-1-4-11-26/h1,3-4,9-13,15-18,22-23,30H,2,5-8,14,19-21H2
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| Chemical Name |
[3-[4-[1-(2-phenylpiperidine-1-carbonyl)triazol-4-yl]phenyl]phenyl]-piperidin-1-ylmethanone
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| Synonyms |
KT 185; KT-185; KT185
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| HS Tariff Code |
2934.99.9001
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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 : ≥ 100 mg/mL (~192.44 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.81 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 | 1.9244 mL | 9.6220 mL | 19.2441 mL | |
| 5 mM | 0.3849 mL | 1.9244 mL | 3.8488 mL | |
| 10 mM | 0.1924 mL | 0.9622 mL | 1.9244 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.
Products are for research use only; We do not sell to patients
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