Toggle Nav

KT203

Catalog No.
C3518
ABHD6 inhibitor
Grouped product items
SizePriceStock Qty
5mg
$99.00
Ship with 5-10 days
10mg
$183.00
Ship with 5-10 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

IC50: < 5 nM

KT203 is an ABHD6 inhibitor.

ABHD6, a unique and highly conserved enzyme in mammals, is prominently expressed in brain, liver, kidney, and brown adipose tissue based on global gene expression analysis and activitybased protein profiling (ABPP).

In vitro: The in-vitro potency of KT203 was studied and it was found that KT203 was able to potently inhibit ABHD6 as measured by gelbased competitive ABPP and 2-AG hydrolysis assays. Moreover, the in-situ potency was then measured by treating Neuro2A cells with varying concentrations of KT203 for 4 h and the results showed that KT203 inhibited ABHD6 with IC50 values in the subnanomolar range [1].

In vivo: In a previous animal study, mice were treated intraperitoneally with KT203 at various doses (0.1-1 mg/kg) for 4 h. Results showed that KT203 had near-complete blockade of ABHD6 in the liver at the highest dose tested. At lower doses, KT203 showed about 80% inhibition of ABHD6 in the liver. Notably, KT203 exhibited impressive selectivity in the mouse liver even at higher doses, showing little cross-reactivity against the numerous carboxylesterase enzymes that are common off-targets of mechanism-based SH inhibitors in rodents. In addition, KT203 showed good selectivity against other brain and liver SHs as judged by gelbased ABPP, suggesting a single major off-target, carboxylesterase-1 (CES1) [1].

Clinical trial: Up to now, KT203 is still in the preclinical development stage.

Reference:
[1] Hsu KL, Tsuboi K, Chang JW, Whitby LR, Speers AE, Pugh H, Cravatt BF.  Discovery and optimization of piperidyl-1,2,3-triazole ureas as potent, selective, and in vivo-active inhibitors of α/β-hydrolase domain containing 6 (ABHD6). J Med Chem. 2013 Nov 14;56(21):8270-9.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt466.5
Cas No.1402612-64-9
FormulaC28H26N4O3
SynonymsML-296
Solubility≤10mg/ml in DMSO;10mg/ml in dimethyl formamide
Chemical Name4'-[1-[[2-(phenylmethyl)-1-piperidinyl]carbonyl]-1H-1,2,3-triazol-4-yl]-[1,1'-biphenyl]-3-carboxylic acid
SDFDownload SDF
Canonical SMILESO=C(N1N=NC(C2=CC=C(C3=CC=CC(C(O)=O)=C3)C=C2)=C1)N4C(CC5=CC=CC=C5)CCCC4
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37°C and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

KT203