NA-184
Based on 1 publication(s) in Google Scholar
NA-184 is a selective and brain-penetrant calpain-2 inhibitor with an IC50 of 134 nM for mouse calpain-2. NA-184 has weak inhibitory activity on calpain-1 (IC50 of 2826 nM). NA-184 does not exhibit significant inhibition on a variety of other cysteine-, serine- or metallo-proteases. NA-184 shows significant neuroprotection and can be used for the study of traumatic brain injury (TBI).
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- Pureza : 99.66%
- No. CAS: 2688119-39-1
- Fòrmula: C27H35ClN4O5
- Peso molecular:531.04
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) NA-184
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Actividad biológica
Descripciòn
In Vitro
NA-184 selectively inhibits calpain-2 with Ki values of 50 nM (human calpain-2) and 309 nM (human calpain-1)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
Parmacokinetics
| Species | Dose | Route | T1/2 | Clearance (CL) | Vd | AUC |
|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.v. | 5.15 h | 480.8 mL/h/kg | 3.56 L/kg | 20800 ng·h/mL |
In Vivo
NA-184 (1 mg/kg; i.p.; once (mice), twice (rat)) inhibits TBI-induced calpain-2 activation and cell death in mice and rats, both male and females[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl/6 mice (3-month-old, 25-30 g) and Sprague-Dawley rats (males and females; six-seven-month-old) bearing controlled cortical impact (CCI)[1]
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Dosage:1 mg/kg
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Administration:i.p.; once (mice), twice (rat)
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Result:Had no effect on calpain-1 activity but resulted in 50%-70% inhibition of calpain-2 activity in both male and female mice and rats.
Chemical Information
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No. CAS 2688119-39-1
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Appearance Solid
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Peso molecular 531.04
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Fòrmula C27H35ClN4O5
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Color White to off-white
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SMILES
ClC1=CC=CC(CNC(C(C(CC)NC([C@H](CC(C)C)NC(NCC2=CC=CC=C2)=O)=O)=O)=O)=C1OC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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ACS Sens
A Sensitive Green-Red FRET Sensor for Calpain-1 Utilizing Heterodimeric Fluorescent Proteins from Distinct Evolutionary Origins. [Abstract]2026 Mar 27;11(3):1891-1907. PMID: 41837894
Solvente y solubilidad
In Vitro:
DMSO : ≥ 100 mg/mL (188.31 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Pureza y Documentación
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Ficha de datos (270 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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Instrucciones de manejo (2659 KB)
Referencias
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8831 mL | 9.4155 mL | 18.8310 mL | 47.0774 mL |
| 5 mM | 0.3766 mL | 1.8831 mL | 3.7662 mL | 9.4155 mL | |
| 10 mM | 0.1883 mL | 0.9415 mL | 1.8831 mL | 4.7077 mL | |
| 15 mM | 0.1255 mL | 0.6277 mL | 1.2554 mL | 3.1385 mL | |
| 20 mM | 0.0942 mL | 0.4708 mL | 0.9415 mL | 2.3539 mL | |
| 25 mM | 0.0753 mL | 0.3766 mL | 0.7532 mL | 1.8831 mL | |
| 30 mM | 0.0628 mL | 0.3138 mL | 0.6277 mL | 1.5692 mL | |
| 40 mM | 0.0471 mL | 0.2354 mL | 0.4708 mL | 1.1769 mL | |
| 50 mM | 0.0377 mL | 0.1883 mL | 0.3766 mL | 0.9415 mL | |
| 60 mM | 0.0314 mL | 0.1569 mL | 0.3138 mL | 0.7846 mL | |
| 80 mM | 0.0235 mL | 0.1177 mL | 0.2354 mL | 0.5885 mL | |
| 100 mM | 0.0188 mL | 0.0942 mL | 0.1883 mL | 0.4708 mL |
NA-184 Related Classifications
HY-155482 Related Classifications
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