Virstatin
Based on 1 Customer Validation
Virstatin is an orally effective Vibrio cholerae virulence inhibitor. Virstatin blocks the expression of downstream virulence genes, such as cholera toxin (ctx) and toxin-coregulated pilus (tcpA), at the post-transcriptional level by inhibiting the dimerization of the transcriptional activator ToxT. Virstatin inhibits Vibrio cholerae-induced expression of COX-2 and iNOS, and exerts bactericidal effects at high concentrations. Virstatin can be used for research on cholera.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.00%
- CAS. Nr.: 88909-96-0
- Formel: C16H13NO4
- Molecular Weight:283.28
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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
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[2]|
COX-2 |
iNOS |
In Vitro
Virstatin (50 µM) does not inhibit the growth of V. cholerae O395 or C6706, with MBCs of 600 and 1200 µM, respectively[1].
Virstatin (50 µM; overnight) blocks the inhibition of cholera toxin (CT) and TcpA expression in V. cholerae O395 and C6706, with MICs for inhibiting CT expression of 3 and 40 µM, respectively[1].
Virstatin (50 μM; 30 min) prevents functional TCP assembly and completely inhibits CTX-Km phage transduction in V. cholerae 0395 cells[1].
Virstatin (50 µM; overnight) inhibits ctx transcription downstream of toxT in V. cholerae O395 and inhibits tcp/ctx locus genes in O395 and C6706, without affecting toxRS, tcpPH, or toxT transcript levels[1].
Virstatin (10-60 μM) inhibits wild-type ToxT-induced β-galactosidase activity in E. coli DTH3060 cells, but has no effect on the mutant ToxT_L113P[1].
Virstatin (0.1-1 mM; 1 h-overnight) exhibits toxicity in V. cholerae C6706 cells by reducing cell viability at a concentration of 1 mM[3].
Virstatin (100 μM; overnight) inhibits CT expression driven by ToxT_EPI in V. cholerae O395ΔtoxT cells, but has no effect on ToxT_ENV and ToxT_L113P[4].
Virstatin (10-50 μM; overnight) inhibits ToxT_EPI dimerization in E. coli KDZif1ZΔtolC cells[4].
Virstatin (50 μM; 18 h) inhibits CT/TcpA expression in classical V. cholerae O395 (toxT-SY), YJB001 (toxT-SF), 569B (toxT-AY), EJK003 (toxT-SF), and EJK017 (toxT-AY), but not in EJK008 (toxT-AY), EJK009 (toxT-AF), EJK011 (toxT-SY), and EJK012 (toxT-SF), with EJK007 (toxT-AF) showing only partial inhibition (TcpA at 50% of the positive control)[5].
Virstatin (50 µM; 8 h) in V. cholerae O395 inhibits virulence genes, including ctxA (-8.1) and tcpC (-11.6), and induces lipid A biosynthesis genes such as VC0212 (5.8)[6].
Virstatin (50 µM; 1 h) strongly inhibits virulence genes in V. cholerae C6706, including tcpA (-18.1), tcpS (-15.8), tcpQ (-14.2), ctxB (-12.6), and ctxA (-9.7)[6].
Virstatin (< 2 mM) exhibits minimal toxicity toward Hep2 epithelial cells[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:V. cholerae O395 and C6706
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Concentration:50 µM
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Incubation Time:overnight
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Result:Significantly inhibited the expression of cholera toxin (CT) .
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Cell Line:V. cholerae O395 and C6706
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Concentration:50 µM
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Incubation Time:overnight
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Result:Significantly inhibited the expression of toxin coregulated pilin (TcpA).
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Cell Line:V. cholerae C6706
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Concentration:0.1 mM, 1 mM
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Incubation Time:1 h, overnight
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Result:Severely attenuated bacterial growth and decreased viability by 6 logs at 1 mM, while showing no significant attenuation at 0.1 mM.
In Vivo
Virstatin (1 mg/mL at inoculation + 50 μg supplemented at 3 h post-infection; i.g.; two doses; 18-24 h) exhibits specific activity in inhibiting TCP-dependent bacterial colonization in a neonatal mouse model of oral Vibrio cholerae inoculation[4].
Virstatin (1.50 mg/mL; p.o.; single administration; 12 h) significantly reduces intestinal fluid secretion, intestinal barrier leakage, and COX-2 expression in a closed ileal loop diarrhea model induced by the Vibrio cholerae El Tor variant in outbred ICR mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR outbred (male; 6 weeks old; 30-35 g)[2]
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Dosage:1.50 mg/mL
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Administration:p.o.; single administration; 12 h
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Result:Significantly reduced EL-induced intestinal fluid secretion and prevented intestinal barrier leakage.
Suppressed EL-induced expression of COX-2 and iNOS in intestinal tissues.
Chemical Information
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CAS. Nr. 88909-96-0
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Appearance Solid
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Molecular Weight 283.28
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Formel C16H13NO4
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Color Light yellow to yellow
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SMILES
O=C(N(C1=O)CCCC(O)=O)C2=CC=CC3=CC=CC1=C23
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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 : 125 mg/mL (441.26 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)
Reinheit & Dokumentation
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Data Sheet (306 KB)
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SDS (758 KB)
- English - EN (758 KB)
- Français - FR (758 KB)
- Deutsch - DE (758 KB)
- Norwegian - NO (758 KB)
- Español - ES (758 KB)
- Swedish - SV (758 KB)
- Italian - IT (758 KB)
- Korean - KR (758 KB)
- Portuguese - PT (758 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.5301 mL | 17.6504 mL | 35.3008 mL | 88.2519 mL |
| 5 mM | 0.7060 mL | 3.5301 mL | 7.0602 mL | 17.6504 mL | |
| 10 mM | 0.3530 mL | 1.7650 mL | 3.5301 mL | 8.8252 mL | |
| 15 mM | 0.2353 mL | 1.1767 mL | 2.3534 mL | 5.8835 mL | |
| 20 mM | 0.1765 mL | 0.8825 mL | 1.7650 mL | 4.4126 mL | |
| 25 mM | 0.1412 mL | 0.7060 mL | 1.4120 mL | 3.5301 mL | |
| 30 mM | 0.1177 mL | 0.5883 mL | 1.1767 mL | 2.9417 mL | |
| 40 mM | 0.0883 mL | 0.4413 mL | 0.8825 mL | 2.2063 mL | |
| 50 mM | 0.0706 mL | 0.3530 mL | 0.7060 mL | 1.7650 mL | |
| 60 mM | 0.0588 mL | 0.2942 mL | 0.5883 mL | 1.4709 mL | |
| 80 mM | 0.0441 mL | 0.2206 mL | 0.4413 mL | 1.1031 mL | |
| 100 mM | 0.0353 mL | 0.1765 mL | 0.3530 mL | 0.8825 mL |
Virstatin Related Classifications
HY-127041 Related Classifications
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