BLT1-IN-1
BLT1-IN-1 is an orally active and selective BLT1 inhibitor with an IC50 of 8.7 nM and a Kd of 121 nM. BLT1-IN-1 exerts protective effects against acute lung injury and sepsis in in vivo models. BLT1-IN-1 can be used in research related to acute lung injury and sepsis.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C38H33F3N2O7
- Molecular Weight:686.67
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Biologische Aktivität
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NLRP3 |
IL-1β |
IL-6 |
BLT1-IN-1 (compound VI-8) (5-20 nM; 24 h) dose-dependently inhibits NO production in LPS (HY-D1056)-stimulated RAW264.7 cells[1].
BLT1-IN-1 (5-20 nM; 24 h) dose-dependently inhibits the activation of IRAK4/NF-κB, MAPK and NLRP3 inflammasome pathways, as well as the expression of proinflammatory cytokines (IL-1β, TNF-α, IL-6) in LPS-induced RAW264.7 cells[1].
BLT1-IN-1 (5-20 nM; 24 h) protects MLE-12 cells against LPS-induced injury in a dose-dependent manner, as evidenced by restored cell viability, reduced apoptosis, and regulated expression of apoptotic proteins[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LPS-stimulated RAW264.7 cells
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Concentration:5 nM, 10 nM, 20 nM
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Incubation Time:24 h (after 30 min LPS pre-treatment)
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Result:Reduced LPS-induced phosphorylation of IRAK4 and NF-κB p65 in a dose-dependent manner.
Decreased protein levels of NLRP3 inflammasome components (NLRP3, ASC, cleaved caspase-1) in a dose-dependent manner without affecting total protein levels of IRAK4, p65, p38, ERK1/2, or JNK.
Reduced phosphorylation of p38, ERK1/2, and JNK in a dose-dependent manner.
BLT1-IN-1 (10-20 mg/kg; oral gavage; once daily for 7 consecutive days) improves the survival rate of mice and alleviates sepsis-induced lung injury and inflammatory response[1].
BLT1-IN-1 (500 mg/kg; p.o.; single administration) is well tolerated in male and female C57BL/6 mice, with no acute toxicity observed[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 (male and female, 8−10 weeks, 22.0 ± 1.0 g, ALI induced by intratracheal instillation of LPS)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:intragastric; once daily for 7 days, plus a single dose 6 hours post-LPS
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Result:Reduced lung wet-to-dry weight ratio dose-dependently, with the 20 mg/kg dose showing the most significant reduction.
Decreased LPS-induced lung tissue damage (including interstitial thickening, alveolar collapse, alveolar fusion) and lung injury scores dose-dependently, and decreased LPS-induced upregulation of RAGE protein levels in lung tissue.
Reversed LPS-induced ventilatory dysfunction dose-dependently: increased minute volume (MV), peak expiratory flow (PEF), and the ratio of expiratory flow at 50% of tidal volume to peak expiratory flow (Rpef), while decreasing expiratory time (Te) and enhanced pause (Penh).
Reduced total inflammatory cell counts (lymphocytes, neutrophils, macrophages) in blood dose-dependently, and reduced macrophage accumulation in lung tissues.
Decreased protein levels of pro-inflammatory cytokines IL-6, TNF-α, and IL-1β in lung tissues and BALF dose-dependently, with the 20 mg/kg dose showing the highest efficacy.
Reversed LPS-induced increases in p-IRAK4 expression and nuclear accumulation of NF-κB p65 in lung tissues.
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Animal Model:C57BL/6 (male and female, 8−10 weeks, 22.0 ± 1.0 g, sepsis induced by intraperitoneal injection of LPS)[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:intragastric; once daily for 7 days
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Result:Improved the survival rate of sepsis-induced mice significantly compared to the LPS model group.
Reduced the lung wet-to-dry weight ratio in sepsis-induced mice.
Attenuated LPS-induced changes in peripheral blood cell counts, reducing the increase in immune cells and the decrease in platelets.
Reduced protein levels of pro-inflammatory cytokines IL-6, TNF-α, and IL-1β in lung tissues significantly.
Alleviated LPS-induced histopathological changes in lung tissue and reduced immune cell infiltration.
Chemical Information
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Molecular Weight 686.67
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Formel C38H33F3N2O7
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SMILES
O=C1C=C(OC2=C(C(OCCCCCCOC3=CC=C(C=C3)/C(N)=N/O)=CC(O)=C21)/C=C/C(C4=CC=C(C(F)(F)F)C=C4)=O)C5=CC=CC=C5
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
BLT1-IN-1 Related Classifications
HY-181809 Related Classifications
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