UK‑396082

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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 522553

CAS#: 400044-47-5

Description: UK‑396082 is an activated thrombin activatable fibrinolysis inhibitor. UK‑396082 (TAFIa Ki = 10 nM, selectivity TAFIa/CPN > 1000) exhibited antithrombotic efficacy in a rabbit model of venous thrombosis, yet had no effect on surgical bleeding in the rabbit. UK‑396082 exhibited an excellent preclinical and clinical pharmacokinetic profile, characterized by paracellular absorption, low clearance, and a low volume of distribution, fully consistent with its physicochemical properties of low molecular weight (MW = 239) and high hydrophilicity (log D = -2.8). UK-396,082 has potential as a novel TAFIa inhibitor for the treatment of thrombosis and other fibrin-dependent diseases in humans.


Price and Availability

Size Price Shipping out time Quantity
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Pricing updated 2020-10-31. Prices are subject to change without notice.

UK‑396082 is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 522553
Name: UK‑396082
CAS#: 400044-47-5
Chemical Formula: C12H21N3O2
Exact Mass: 239.1634
Molecular Weight: 239.319
Elemental Analysis: C, 60.23; H, 8.85; N, 17.56; O, 13.37


Synonym: UK‑396082; UK396082; UK 396082; UK‑396,082; UK396,082; UK 396,082

IUPAC/Chemical Name: (S)-5-amino-2-((1-propyl-1H-imidazol-4-yl)methyl)pentanoic acid

InChi Key: OTDGPKRCQXSTPV-JTQLQIEISA-N

InChi Code: InChI=1S/C12H21N3O2/c1-2-6-15-8-11(14-9-15)7-10(12(16)17)4-3-5-13/h8-10H,2-7,13H2,1H3,(H,16,17)/t10-/m0/s1

SMILES Code: CCCN1C=C(N=C1)C[C@H](CCCN)C(=O)O


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


References

1: Atkinson JM, Pullen N, Da Silva-Lodge M, Williams L, Johnson TS. Inhibition of Thrombin-Activated Fibrinolysis Inhibitor Increases Survival in Experimental Kidney Fibrosis. J Am Soc Nephrol. 2015 Aug;26(8):1925-37. doi: 10.1681/ASN.2014030303. Epub 2014 Nov 19. PubMed PMID: 25411467; PubMed Central PMCID: PMC4520161.

2: Atkinson JM, Pullen N, Johnson TS. An inhibitor of thrombin activated fibrinolysis inhibitor (TAFI) can reduce extracellular matrix accumulation in an in vitro model of glucose induced ECM expansion. Matrix Biol. 2013 Jun 24;32(5):277-87. doi: 10.1016/j.matbio.2013.01.006. Epub 2013 Jan 29. PubMed PMID: 23369837.

3: Owen DR, Bull DJ, Bunnage ME, Glossop MS, Maguire RJ, Strang RS. Oxygenated analogues of UK-396082 as inhibitors of activated thrombin activatable fibrinolysis inhibitor. Bioorg Med Chem Lett. 2010 Jan 1;20(1):92-6. doi:10.1016/j.bmcl.2009.11.029. Epub 2009 Nov 13. PubMed PMID: 19954973.

4: Bunnage ME, Blagg J, Steele J, Owen DR, Allerton C, McElroy AB, Miller D, Ringer T, Butcher K, Beaumont K, Evans K, Gray AJ, Holland SJ, Feeder N, Moore RS, Brown DG. Discovery of potent & selective inhibitors of activated thrombin-activatable fibrinolysis inhibitor for the treatment of thrombosis. J Med Chem. 2007 Nov 29;50(24):6095-103. Epub 2007 Nov 9. PubMed PMID: 17990866.