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Naroparcil

Catalog No. T68002   CAS 120819-70-7

Naroparcil, an orally available thioglycoside analog of 4-methylumbelliferyl β-D-xyloside, showed antithrombotic effects in the Wessler sludge model of venous thrombosis (jugular vein).Naroparcil enhanced the formation of the thrombin/heparin cofactor II complex, induced dermatophyte sulfate-like substances in plasma from treated rabbits appearance, but reduced the formation of thrombin/antithrombin III complexes in plasma incubated with (125I)-human alpha-thrombin.

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Naroparcil Chemical Structure
Naroparcil, CAS 120819-70-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 310.00
5 mg In stock $ 757.00
10 mg In stock $ 1,060.00
25 mg In stock $ 1,580.00
50 mg In stock $ 2,130.00
100 mg In stock $ 2,870.00
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Purity: 98.81%
ee: 100%
Purity: 98.11%
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Biological Description
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Description Naroparcil, an orally available thioglycoside analog of 4-methylumbelliferyl β-D-xyloside, showed antithrombotic effects in the Wessler sludge model of venous thrombosis (jugular vein).Naroparcil enhanced the formation of the thrombin/heparin cofactor II complex, induced dermatophyte sulfate-like substances in plasma from treated rabbits appearance, but reduced the formation of thrombin/antithrombin III complexes in plasma incubated with (125I)-human alpha-thrombin.
In vivo Naroparcil attenuated thrombus development in a Wessler stasis model of venous thrombosis (jugular vein) employing bovine factor Xa as a thrombogenic stimulus giving ED50 values of 21.9 mg/kg and 36.0 mg/kg after respectively i.v. and p.o.. Venous antithrombotic activity was maximal 2-3 h after i.v. administration and 4-8 h after oral administration. Four hours after the oral administration of maximal antithrombotic (Wessler model, factor Xa) doses (100 and 400 mg/kg), naroparcil had no significant effect on bleeding time. In platelet-poor plasma obtained from animals treated 4 h previously with various doses (25 to 400 mg/kg) of naroparcil, there was no detectable anti-factor Xa nor antithrombin activity. Similarly, naroparcil had no effect on APTT nor on thrombin time. A sensitized thrombin time (to about 35 s) was modestly but significantly increased following oral administration of the compound at 400 mg/kg. However, thrombin generation by the intrinsic pathway was reduced in a dose-related manner, with maximal reduction being 65% at 400 mg/kg. The same dose of naroparcil enhanced the formation of thrombin/heparin cofactor II complexes at the expense of thrombin/antithrombin III complexes in plasma incubated with (125I)-human alpha-thrombin and induced the appearance of dermatan sulfate-like material in the plasma of treated rabbits, as measured by a heparin cofactor II-mediated thrombin inhibition assay.[1]
Molecular Weight 387.47
Formula C19H17NO4S2
CAS No. 120819-70-7

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

Naroparcil 120819-70-7 Proteases/Proteasome Thrombin inhibitor inhibit

 

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