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Terutroban

Cat. No. M3951
Terutroban Structure
Synonym:

S-18886

Size Price Availability Quantity
10mM*1mL USD 90  USD90 In stock
10mg USD 80  USD80 In stock
50mg USD 350  USD350 In stock
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Quality Control & Documentation
Biological Activity

Terutroban significantly protected retinal vascularity from ischaemia in experimental diabetes, and this result could be attributed not only to its antiplatelet/antithrombotic activities but also to its vascular properties.TP-receptor blockade with terutroban decreases portal pressure in cirrhosis.This effect is due to decreased hepatic resistance, which in CCl4 -cirrhotic rats was linked to decreased hepatic fibrosis, but not in BDL rats, in which the main mediator appeared to be an enhanced eNOS-dependent vasodilatation, which was not liver-selective, as it was associated with decreased arterial pressure. The potential use of terutroban for portal hypertension requires further investigation.

Chemical Information
Molecular Weight 407.92
Formula C20H22ClNO4S
CAS Number 165538-40-9
Form Solid
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] De La Cruz JP, et al. Diabetes Metab Res Rev. Effects of terutroban, a thromboxane/prostaglandin endoperoxide receptor antagonist, on retinal vascularity in diabetic rats.

[2] Rosado E, et al. Diabetes Metab Res Rev. Terutroban, a TP-receptor antagonist, reduces portal pressure in cirrhotic rats.

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