GSK 366
Based on 1 Customer Validation
GSK 366 is a type II kynurenine-3-monooxygenase (KMO) inhibitor with IC50 values of 2.3 nM and 0.7 nM for human KMO and P. fluorescens-KMO (Pf-KMO). GSK 366 binds to KMO’s substrate site, prevents productive NADPH association, substrate binding, and FAD hydroperoxy species formation. GSK 366 does not stimulate hydrogen peroxide (H2O2) production and reduces H2O2 levels. GSK 366 can be used for the researches of inflammation and neurological disease, such as acute pancreatitis multiple organ dysfunction syndrome and Alzheimer’s disease.
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- Purity: 98.17%
- CAS No.: 1953157-39-5
- 화학식: C17H16ClN3O4
- 분자량:361.78
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
IC50: 2.3 nM (human KMO), 0.7 nM (Pf-KMO)[1]
GSK366 potently inhibits purified Pf-KMO with an IC50 of 0.7 nM[1].
GSK366 potently inhibits human KMO from Sf9 cell membranes with an IC50 of 2.3 nM and an estimated Ki of ~12 pM[1].
GSK366 (5 nM; 0-400 min) exhibits slow association kinetics with human KMO from Sf9 cell membranes and exhibits very slow dissociation kinetics[1].
GSK366 (0.0001-100 μM; 15 min) does not stimulate hydrogen peroxide production in Pf-KMO or human KMO from Sf9 cell membranes, and reduces basal hydrogen peroxide levels in human KMO[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1953157-39-5
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Appearance Solid
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분자량 361.78
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화학식 C17H16ClN3O4
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Color Light yellow to yellow
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SMILES
O=C(O)CCC1=NOC2=C1C=C(Cl)C(O[C@@H](C3=NN=C(C)C=C3)C)=C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
DMSO : 250 mg/mL (691.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.75 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.75 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.7641 mL | 13.8206 mL | 27.6411 mL | 69.1028 mL |
| 5 mM | 0.5528 mL | 2.7641 mL | 5.5282 mL | 13.8206 mL | |
| 10 mM | 0.2764 mL | 1.3821 mL | 2.7641 mL | 6.9103 mL | |
| 15 mM | 0.1843 mL | 0.9214 mL | 1.8427 mL | 4.6069 mL | |
| 20 mM | 0.1382 mL | 0.6910 mL | 1.3821 mL | 3.4551 mL | |
| 25 mM | 0.1106 mL | 0.5528 mL | 1.1056 mL | 2.7641 mL | |
| 30 mM | 0.0921 mL | 0.4607 mL | 0.9214 mL | 2.3034 mL | |
| 40 mM | 0.0691 mL | 0.3455 mL | 0.6910 mL | 1.7276 mL | |
| 50 mM | 0.0553 mL | 0.2764 mL | 0.5528 mL | 1.3821 mL | |
| 60 mM | 0.0461 mL | 0.2303 mL | 0.4607 mL | 1.1517 mL | |
| 80 mM | 0.0346 mL | 0.1728 mL | 0.3455 mL | 0.8638 mL | |
| 100 mM | 0.0276 mL | 0.1382 mL | 0.2764 mL | 0.6910 mL |
GSK 366 Related Classifications
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