MI-1851
Based on 1 Customer Validation
MI-1851 is a potent furin inhibitor. MI-1851 prevents the proteolytic processing of the S protein of SARS-CoV-2 by endogenous flavoprotease in HEK293 cells. MI-185 has antiviral activity.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 95.92%
- CAS. Nr.: 2417283-44-2
- Formel: C34H53N15O6
- Molecular Weight:767.88
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Speicherung:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Vero 76 | CC50 |
>50 μM
Compound: 8
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Cytotoxicity against african green monkey Vero 76 cells by Cell Titer Glo assay
Cytotoxicity against african green monkey Vero 76 cells by Cell Titer Glo assay
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[PMID: 33732412] |
MI-1851 (0-100 μM, 2h, 24 h) does not affect PHH cells viability, and extracellular hydrogen peroxide production even at 100 μM but reduces CYP3A4 isoenzyme activity in PHH cells in a dose-dependent manner[1].
MI-1851 (10-50 μM, 72 h) strongly inhibits the spread of SARS-CoV-2 and its proliferation in Calu-3 cells even at a low dose of 10 μM, which reduces the virus titer by 30 to 190-fold[2].
MI-1851 (compound 8) (0.5-16 μM, 48 h) inhibits DENV-2 and WNV replication with the EC50 values of 1.50 μM and 1.46 μM, respectively in huh-7 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[3]
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Dosage:2.5 mg/kg
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Administration:Intravenous injection; once
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Result:The pharmacokinetic parameters of MI-1851 (compound 8)
Parameter MI-1851 (compound 8) t1/2 1.6 h total body clearance 273 mL/(h•kg) Cmax 3156 ng/mL
Chemical Information
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CAS. Nr. 2417283-44-2
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Appearance Solid
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Molecular Weight 767.88
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Formel C34H53N15O6
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Color White to off-white
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SMILES
NC(NCC1=CC=C(C=C1)CC(N[C@H](C(N[C@H](C(N[C@H](C(NCC2=CC=C(C=C2)C(N)=N)=O)CCONC(N)=N)=O)C(C)(C)C)=O)CCONC(N)=N)=O)=N
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
DMSO : 125 mg/mL (162.79 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Reinheit & Dokumentation
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Data Sheet (271 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]. Erzsébet Pászti-Gere, et al. In vitro characterization of the furin inhibitor MI-1851: Albumin binding, interaction with cytochrome P450 enzymes and cytotoxicity. Biomed Pharmacother. 2022 Jul;151:113124. [Content Brief]
[2]. Dorothea Bestle, et al. TMPRSS2 and furin are both essential for proteolytic activation of SARS-CoV-2 in human airway cells. Life Sci Alliance. 2020 Jul 23;3(9):e202000786. [Content Brief]
[3]. Thuy Van Lam van, et al. The Basicity Makes the Difference: Improved Canavanine-Derived Inhibitors of the Proprotein Convertase Furin. ACS Med Chem Lett. 2021 Feb 9;12(3):426-432. [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 (sealed storage, away from moisture). 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 | 1.3023 mL | 6.5114 mL | 13.0229 mL | 32.5572 mL |
| 5 mM | 0.2605 mL | 1.3023 mL | 2.6046 mL | 6.5114 mL | |
| 10 mM | 0.1302 mL | 0.6511 mL | 1.3023 mL | 3.2557 mL | |
| 15 mM | 0.0868 mL | 0.4341 mL | 0.8682 mL | 2.1705 mL | |
| 20 mM | 0.0651 mL | 0.3256 mL | 0.6511 mL | 1.6279 mL | |
| 25 mM | 0.0521 mL | 0.2605 mL | 0.5209 mL | 1.3023 mL | |
| 30 mM | 0.0434 mL | 0.2170 mL | 0.4341 mL | 1.0852 mL | |
| 40 mM | 0.0326 mL | 0.1628 mL | 0.3256 mL | 0.8139 mL | |
| 50 mM | 0.0260 mL | 0.1302 mL | 0.2605 mL | 0.6511 mL | |
| 60 mM | 0.0217 mL | 0.1085 mL | 0.2170 mL | 0.5426 mL | |
| 80 mM | 0.0163 mL | 0.0814 mL | 0.1628 mL | 0.4070 mL | |
| 100 mM | 0.0130 mL | 0.0651 mL | 0.1302 mL | 0.3256 mL |
MI-1851 Related Classifications
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