KT203 (Synonyms: ML-296) |
| Catalog No.GC13763 |
KT203 es un inhibidor potente y selectivo del dominio α/β-hidrolasa que contiene 6 (ABHD6), con una IC50 de 0,31 nM en células Neuro2A.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1402612-64-9
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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.
| Cas No. | 1402612-64-9 | SDF | |
| Sinónimos | ML-296 | ||
| Chemical Name | 4'-[1-[[2-(phenylmethyl)-1-piperidinyl]carbonyl]-1H-1,2,3-triazol-4-yl]-[1,1'-biphenyl]-3-carboxylic acid | ||
| Canonical SMILES | O=C(N1N=NC(C2=CC=C(C3=CC=CC(C(O)=O)=C3)C=C2)=C1)N4C(CC5=CC=CC=C5)CCCC4 | ||
| Formula | C28H26N4O3 | M.Wt | 466.5 |
| Solubility | ≤10mg/ml in DMSO;10mg/ml in dimethyl formamide | 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. |
||
| 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 | 2.1436 mL | 10.7181 mL | 21.4362 mL |
| 5 mM | 0.4287 mL | 2.1436 mL | 4.2872 mL |
| 10 mM | 0.2144 mL | 1.0718 mL | 2.1436 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *