2. GPCR/G Protein Immunology/Inflammation Apoptosis NF-κB MAPK/ERK Pathway
  3. Leukotriene Receptor Interleukin Related Apoptosis IRAK NF-κB p38 MAPK NOD-like Receptor (NLR) Caspase
  4. 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.

For research use only. We do not sell to patients.

BLT1-IN-1

BLT1-IN-1 Chemical Structure

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BLT1-IN-1 Related Antibodies

Top Publications Citing Use of Products

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LTB4 LTC4/CysLT2 LTD4/CysLT1 LTE4

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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IRAK1 IRAK3 IRAK4

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

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NLRP3 NLRP1 NOD1 NOD2

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

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[1].

IC50 & Target[1]

NLRP3

 

IL-1β

 

IL-6

 

In Vitro

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.

BLT1-IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: LPS-stimulated RAW264.7 cells
Concentration: 5 nM, 10 nM, 20 nM
Incubation Time: 24 h (after 30 min LPS pre-treatment)
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.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-∞ MRT0-∞ CL Bioavailability
Rat[1] 5 mg/kg i.v. 0.74 h / 3083.30 ng/mL 733.60 ng·h/mL 1.58 h 6.82 L/h/kg /
Rat[1] 20 mg/kg p.o. 1.34 h 2.00 h 711.70 ng/mL 2504.40 ng·h/mL 4.52 h 7.98 L/h/kg 85.30 %
In Vivo

BLT1-IN-1 (5-20 mg/kg; oral gavage; once daily for 8 consecutive days) dose-dependently alleviates LPS-induced acute lung injury in mice[1].
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.

Animal Model: C57BL/6 (male and female, 8−10 weeks, 22.0 ± 1.0 g, ALI induced by intratracheal instillation of LPS)[1]
Dosage: 5 mg/kg; 10 mg/kg; 20 mg/kg
Administration: intragastric; once daily for 7 days, plus a single dose 6 hours post-LPS
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.
Animal Model: C57BL/6 (male and female, 8−10 weeks, 22.0 ± 1.0 g, sepsis induced by intraperitoneal injection of LPS)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: intragastric; once daily for 7 days
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.
Molecular Weight

686.67

Formula

C38H33F3N2O7
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BLT1-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BLT1-IN-1Leukotriene ReceptorInterleukin RelatedApoptosisIRAKNF-κBp38 MAPKNOD-like Receptor (NLR)CaspaseILInterleukin-1 receptor associated kinaseIL-1R associated kinaseNuclear factor-κBNuclear factor-kappaBSer277acute lung injuryAla274BLT1His94Arg156Ser278BLT2Met101sepsisInhibitorinhibitorinhibit

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