ZT-1a
Based on 3 publication(s) in Google Scholar
ZT-1a is a potent, non-ATP-competitive and selective SPAK inhibitor. ZT-1a inhibits SPAK activity with IC50s of 44.3, 35.0, 46.7 μM at ATP concentrations of 0.01, 0.1 and 1 mM, respectively.
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- Pureté: 99.83%
- CAS No.: 212135-62-1
- Formule: C22H15Cl3N2O2
- Masse moléculaire:445.73
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ZT-1a
More
Activité biologique
SPAK[1]
ZT-1a inhibits Na-K-2Cl cotransporter (NKCC1) and stimulates K-Cl cotransporters (KCCs) by decreasing their SPS1-related proline/alanine-rich kinase (SPAK)-dependent phosphorylation[1].
ZT-1a inhibits phosphorylation of NKCC1 p-Thr203/207/212 by 72±5.2% at 1 μM ZT-1a and phosphorylation of KCC sites 1/2 by 65-77% at 3 μM in HEK-293 cells[1].
SPAK phosphorylation at Ser373 is inhibited by 70±3.8% inhibition at 3-10 μM ZT-1a[1].
ZT-1a (10 μM) inhibits NKCC1 but stimulates KCC3 activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Naive mice[1]
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Dosage:10, 30, 50, and 100 mg/kg
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Administration:Intraperitoneal (i.p.) administration
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Result:Inhibited SPAK-dependent cation-Cl- cotransporters (CCC) phosphorylation in vivo.
Chemical Information
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CAS No. 212135-62-1
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Appearance Solid
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Masse moléculaire 445.73
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Formule C22H15Cl3N2O2
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Color White to off-white
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SMILES
O=C(NC1=CC(Cl)=C(C(C2=CC=C(Cl)C=C2)C#N)C=C1C)C3=CC(Cl)=CC=C3O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Biosci Trends
Suppression of STK39 weakens the MASLD/MASH process by protecting the intestinal barrier. [Abstract]2024 Jul 9;18(3):289-302. PMID: 38925962 -
bioRxiv
2025 Feb 27:2025.02.27.640596. PMID: 40060460 -
Solvant et solubilité
DMSO : 100 mg/mL (224.35 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 (4.67 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 (4.67 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.
Pureté et documentation
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Fiche technique (276 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)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 2.2435 mL | 11.2176 mL | 22.4351 mL | 56.0878 mL |
| 5 mM | 0.4487 mL | 2.2435 mL | 4.4870 mL | 11.2176 mL | |
| 10 mM | 0.2244 mL | 1.1218 mL | 2.2435 mL | 5.6088 mL | |
| 15 mM | 0.1496 mL | 0.7478 mL | 1.4957 mL | 3.7392 mL | |
| 20 mM | 0.1122 mL | 0.5609 mL | 1.1218 mL | 2.8044 mL | |
| 25 mM | 0.0897 mL | 0.4487 mL | 0.8974 mL | 2.2435 mL | |
| 30 mM | 0.0748 mL | 0.3739 mL | 0.7478 mL | 1.8696 mL | |
| 40 mM | 0.0561 mL | 0.2804 mL | 0.5609 mL | 1.4022 mL | |
| 50 mM | 0.0449 mL | 0.2244 mL | 0.4487 mL | 1.1218 mL | |
| 60 mM | 0.0374 mL | 0.1870 mL | 0.3739 mL | 0.9348 mL | |
| 80 mM | 0.0280 mL | 0.1402 mL | 0.2804 mL | 0.7011 mL | |
| 100 mM | 0.0224 mL | 0.1122 mL | 0.2244 mL | 0.5609 mL |
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