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UK-396082

Chemical Structure : UK-396082

CAS No.: 400044-47-5

UK-396082 (UK 396,082;UK396082)

Catalog No.: PC-61820Not For Human Use, Lab Use Only.

UK-396082 is a potent and selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (activated TAFI.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

UK-396082 is a potent and selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (activated TAFI; TAFIa) with Ki of 10 nM; displays excellent selectivity over plasma carboxypeptidase N (>1,000-fold); exhibits antithrombotic efficacy in a rabbit model of venous thrombosis, yet has no effect on surgical bleeding in the rabbit; possesses excellent preclinical and clinical pharmacokinetic profile, and shows potential for the treatment of thrombosis and other fibrin-dependent diseases in humans.

Thrombosis

Phase 1 Discontinued

Physicochemical Properties

M.Wt 239.319
Formula C12H21N3O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-5-amino-2-((1-propyl-1H-imidazol-4-yl)methyl)pentanoic acid

References

1. Bunnage ME, et al. J Med Chem. 2007 Nov 29;50(24):6095-103.

2. Atkinson JM, et al. Matrix Biol. 2013 Jun 24;32(5):277-87.

3. Bridge K, et al. PLoS One. 2017 May 4;12(5):e0177117.

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