UK‑396082 | CAS#400044-47-5 | Thrombin Activatable Fibrinolysis Inhibitor

MedKoo Cat#: 522553 | Name: UK‑396082

Description:

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

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.

Chemical Structure

UK‑396082

CAS#400044-47-5

Theoretical Analysis

MedKoo Cat#: 522553

Name: UK‑396082

CAS#: 400044-47-5

Chemical Formula: C12H21N3O2

Exact Mass: 239.1634

Molecular Weight: 239.32

Elemental Analysis: C, 60.23; H, 8.85; N, 17.56; O, 13.37

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

No Data

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

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

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 239.32 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

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.