Pralnacasan
Based on 1 publication(s) in Google Scholar
Pralnacasan (VX-740) is a potent, selective, non-peptide and orally active interleukin-1β converting enzyme (ICE, caspase 1) inhibitor with a Ki of 1.4 nM. Pralnacasan inhibits proinflammatory cytokines IL-18, IL-1β , and IFN-γ. Pralnacasan has the potential for osteoarthritis and rheumatoid arthritis treatment.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.83%
- CAS. Nr.: 192755-52-5
- Formel: C26H29N5O7
- Molecular Weight:523.54
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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
Publications Citing Use of MedChemExpress (MCE) Pralnacasan
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Biologische Aktivität
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Interleukin-1β converting enzyme 1.4 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| THP-1 | IC50 |
120 nM
Compound: 3
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Inhibition of 1 ug/mL LPS-induced IL1-beta production in human monocytic cells after 4 hrs
Inhibition of 1 ug/mL LPS-induced IL1-beta production in human monocytic cells after 4 hrs
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[PMID: 16046125] |
| THP-1 | IC50 |
190 nM
Compound: 2, pralnacasan
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Inhibition of IL1-beta secretion in human THP1 cells
Inhibition of IL1-beta secretion in human THP1 cells
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[PMID: 16782334] |
| THP-1 | IC50 |
190 nM
Compound: 3
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Inhibition of LPS-induced ILbeta1 release in human THP1 cells
Inhibition of LPS-induced ILbeta1 release in human THP1 cells
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[PMID: 16870441] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Balb/c mice induced with collagenase[1]
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Dosage:0 mg/kg, 12.5 mg/kg, 25 mg/kg and 50 mg/kg
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Administration:Oral gavage; twice a day; for 6 weeks
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Result:Significantly ameliorated the histopathological damage of the medial knee joint compartments.
Chemical Information
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CAS. Nr. 192755-52-5
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Appearance Solid
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Molecular Weight 523.54
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Formel C26H29N5O7
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Color White to off-white
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SMILES
O=C([C@@H]1CCCN2N1C([C@@H](NC(C3=NC=CC4=C3C=CC=C4)=O)CCC2=O)=O)N[C@@H](C5)[C@H](OCC)OC5=O
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Synonyms
VX-740; HMR 3480
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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
Publications (1)
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Journal Impact Factor
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Most Recent
Lösungsmittel & Löslichkeit
DMSO : 220 mg/mL (420.22 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)
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: ≥ 5.5 mg/mL (10.51 mM); Clear solution
This protocol yields a clear solution of ≥ 5.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 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: ≥ 5.5 mg/mL (10.51 mM); Clear solution
This protocol yields a clear solution of ≥ 5.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (55.0 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.
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Rudolphi K, et al. Pralnacasan, an inhibitor of interleukin-1beta converting enzyme, reduces joint damage in two murine models of osteoarthritis. Osteoarthritis Cartilage. 2003 Oct;11(10):738-46. [Content Brief]
[2]. Loher F, et al. The interleukin-1 beta-converting enzyme inhibitor pralnacasan reduces dextran sulfate sodium-induced murine colitis and T helper 1 T-cell activation. J Pharmacol Exp Ther. 2004 Feb;308(2):583-90. [Content Brief]
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 | 1.9101 mL | 9.5504 mL | 19.1007 mL | 47.7518 mL |
| 5 mM | 0.3820 mL | 1.9101 mL | 3.8201 mL | 9.5504 mL | |
| 10 mM | 0.1910 mL | 0.9550 mL | 1.9101 mL | 4.7752 mL | |
| 15 mM | 0.1273 mL | 0.6367 mL | 1.2734 mL | 3.1835 mL | |
| 20 mM | 0.0955 mL | 0.4775 mL | 0.9550 mL | 2.3876 mL | |
| 25 mM | 0.0764 mL | 0.3820 mL | 0.7640 mL | 1.9101 mL | |
| 30 mM | 0.0637 mL | 0.3183 mL | 0.6367 mL | 1.5917 mL | |
| 40 mM | 0.0478 mL | 0.2388 mL | 0.4775 mL | 1.1938 mL | |
| 50 mM | 0.0382 mL | 0.1910 mL | 0.3820 mL | 0.9550 mL | |
| 60 mM | 0.0318 mL | 0.1592 mL | 0.3183 mL | 0.7959 mL | |
| 80 mM | 0.0239 mL | 0.1194 mL | 0.2388 mL | 0.5969 mL | |
| 100 mM | 0.0191 mL | 0.0955 mL | 0.1910 mL | 0.4775 mL |
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