Name: TAPI-1
Price: 936.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    TAPI-1 is an inhibitor of tumour necrosis factor with IC50 value of 8.09 μM [1].TAPI-1 is an inhibitor of TACE/ADAM17 which catalyzes the cleavage of full-length APP to the soluble N-terminal fragment (sAPPα). The release of sAPPα has been reported to be a receptor-coupled process increased by the stimulation of muscarinic receptors. In HEK293 cells, treatment of TAPI-1 resulted in an inhibition of increased sAPPα which was induced by the expressing of M3 subtype. The IC50 values of TAPI-1 in the inhibition of M3-increased sAPPα and constitutive release of sAPPα were 3.61 μM and 8.09 μM, respectively. Besides APP, TAPI-1 was also found to have inhibitory effects on the release of TNF-α, IL6R, TNFRI and TNFRII with IC50 values of 50-100, 5-10, 5-10 and 25-50 mM, respectively [1, 2].
    
    [1] Slack B, Ma L, Seah C. Constitutive shedding of the amyloid precursor protein ectodomain is up-regulated by tumour necrosis factor-α converting enzyme. Biochem. J, 2001, 357: 787-794.
    [2] Hooper N, Karran E, Turner A. Membrane protein secretases. Biochem. J, 1997, 321: 265-279.
- Properties
  - Alternative Name
    
    N1-((R)-1-(((R)-1-((2-aminoethyl)amino)-1-oxopropan-2-yl)amino)-3-(naphthalen-2-yl)-1-oxopropan-2-yl)-N4-hydroxy-2-isobutylsuccinamide
    
    CAS Number
    
    171235-71-5
    
    Molecular Formula
    
    C26H37N5O5
    
    Molecular Weight
    
    499.6
    
    Appearance
    
    A solid
    
    Purity
    
    99.49%
    
    Solubility
    
    ≥24.98 mg/mL in DMSO; ≥15.77 mg/mL in EtOH with ultrasonic; ≥18.1 mg/mL in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Zhang Y, Wang Y, et al. "Angiotensin Ⅱ deteriorates advanced atherosclerosis by promoting MerTK cleavage and impairing efferocytosis through AT1R/ROS/p38MAPK/ADAM17 pathway." Am J Physiol Cell Physiol. 2019 Aug 7. PMID:31390228
    2. Zhou J, Sun J, et al. "MicroRNA-145 overexpression attenuates apoptosis and increases matrix synthesis in nucleus pulposus cells." Life Sci. 2019 Mar 15;221:274-283. PMID:30797016
    3. Ellis-Connell AL, Balgeman AJ, et al. "ALT-803 transiently reduces SIV replication in the absence of antiretroviral treatment." J Virol. 2017 Nov 8. pii: JVI.01748-17. PMID:29118125

TAPI-1

TAPI-1

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