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LTB4 antagonist 3

Cat. No. M41854
LTB4 antagonist 3 Structure
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Biological Activity

LTB4 antagonist 3 is a leukotriene B4 (LTB4) antagonist with an IC50 value of 477 nM.

Chemical Information
Molecular Weight 485.53
Formula C29H27NO6
CAS Number 2929239-87-0
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Wei-Gang Tong et al. Biochem Biophys Res Commun. LTB4 stimulates growth of human pancreatic cancer cells via MAPK and PI-3 kinase pathways

[2] H J Showell et al. Br J Pharmacol. Characterization of the pharmacological profile of the potent LTB4 antagonist CP-105,696 on murine LTB4 receptors in vitro

[3] J C Boehm et al. J Med Chem. Synthesis and LTB4 receptor antagonist activities of the naturally occurring LTB4 receptor antagonist Leucettamine A and related analogues

[4] J S Sawyer et al. J Med Chem. Synthetic and structure/activity studies on acid-substituted 2-arylphenols: discovery of 2-[2-propyl-3-[3-[2-ethyl-4-(4-fluorophenyl)-5- hydroxyphenoxy]-propoxy]phenoxy]benzoic acid, a high-affinity leukotriene B4 receptor antagonist

[5] K Kishikawa et al. Prostaglandins. ONO-4057, a novel, orally active leukotriene B4 antagonist: effects on LTB4-induced neutrophil functions

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