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ICI 192605

Cat. No. M7855
ICI 192605 Structure
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Biological Activity

ICI 192605 is a potent thromboxane A2 receptor antagonist. It inhibits platelet aggregation and can reverse the effects of vasoconstrictors such as TXA2 or PGD2. ICI 192605 can reverse vasoconstriction induced by inhibition of NO production by L-NEMA, which leads to an increase in TXA2 release.

Chemical Information
Molecular Weight 402.87
Formula C22H23ClO5
CAS Number 117621-64-4
Solubility (25°C) DMSO: ≥20 mg/mL
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] Matthew M Hewitt, et al. Pharmacology of Bradykinin-Evoked Coughing in Guinea Pigs

[2] Luke J Janssen, et al. Involvement of TP and EP3 receptors in vasoconstrictor responses to isoprostanes in pulmonary vasculature

[3] N al Jarad, et al. Effects of a thromboxane receptor antagonist on prostaglandin D2 and histamine induced bronchoconstriction in man

[4] A G Brewster, et al. The synthesis of a novel thromboxane receptor antagonist 4(Z)-6-(2-o-chlorophenyl-4-o-hydroxyphenyl-1,3-dioxan-cis-5-yl) hexenoic acid ICI 192605

[5] G R Brown, et al. Improved synthetic routes to the novel thromboxane receptor antagonist ICI 192605: activity of synthetic 1,3-dioxane intermediates

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