KCC2 blocker 1
Based on 1 Customer Validation
KCC2 blocker 1 is an orally active and selective K+-Cl- cotransporter KCC2 blocker with an IC50 of 1 μM. KCC2 blocker 1 is a benzyl prolinate.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.08%
- CAS. Nr.: 1228439-36-8
- Formel: C22H25NO5S
- Molecular Weight:415.50
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
IC50: 1 μM (KCC2)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| MDCK | IC50 |
3 μM
Compound: 13
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Antagonist activity to dog NKCC1 transporter expressed in MDCK cells assessed as inhibition of Cl- free medium-stimulated Rb+ influx after 45 mins by atomic absorption spectroscopy
Antagonist activity to dog NKCC1 transporter expressed in MDCK cells assessed as inhibition of Cl- free medium-stimulated Rb+ influx after 45 mins by atomic absorption spectroscopy
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[PMID: 20299216] |
In Vitro
KCC2 blocker 1 (compound 13; 100 μM) inhibits NKCC1 with 35%.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats[1]
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Dosage:1 mg/kg or 6 mg/kg (Pharmacokinetic Analysis)
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Administration:IV (1 mg/kg) and PO (6 mg/kg)
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Result:Had a t1/2 of 0.3 hours, a CL of 26 mL/min/kg, a C max of 457 ng/mL and a AUC of 726 ng•h/mL.
Chemical Information
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CAS. Nr. 1228439-36-8
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Appearance Solid
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Molecular Weight 415.50
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Formel C22H25NO5S
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Color Light yellow to yellow
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SMILES
O=C(OCC1=CC=CC=C1)C2(CC3=CC=C(S(=O)(C)=O)C=C3)N(C(C)=O)CCC2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 250 mg/mL (601.68 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
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 (5.01 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 (5.01 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.
In Vivo Dissolution Calculator
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.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
Verweise
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.4067 mL | 12.0337 mL | 24.0674 mL | 60.1685 mL |
| 5 mM | 0.4813 mL | 2.4067 mL | 4.8135 mL | 12.0337 mL | |
| 10 mM | 0.2407 mL | 1.2034 mL | 2.4067 mL | 6.0168 mL | |
| 15 mM | 0.1604 mL | 0.8022 mL | 1.6045 mL | 4.0112 mL | |
| 20 mM | 0.1203 mL | 0.6017 mL | 1.2034 mL | 3.0084 mL | |
| 25 mM | 0.0963 mL | 0.4813 mL | 0.9627 mL | 2.4067 mL | |
| 30 mM | 0.0802 mL | 0.4011 mL | 0.8022 mL | 2.0056 mL | |
| 40 mM | 0.0602 mL | 0.3008 mL | 0.6017 mL | 1.5042 mL | |
| 50 mM | 0.0481 mL | 0.2407 mL | 0.4813 mL | 1.2034 mL | |
| 60 mM | 0.0401 mL | 0.2006 mL | 0.4011 mL | 1.0028 mL | |
| 80 mM | 0.0301 mL | 0.1504 mL | 0.3008 mL | 0.7521 mL | |
| 100 mM | 0.0241 mL | 0.1203 mL | 0.2407 mL | 0.6017 mL |
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