TAPI-1 Struktur

TAPI-1

Bezeichnung:TAPI-1

CAS-Nr171235-71-5

Englisch Name:TAPI-1

CBNumberCB22729657

SummenformelC26H37N5O5

Molgewicht499.6

MOL-Datei171235-71-5.mol

TAPI-1 physikalisch-chemischer Eigenschaften

Dichte	1?+-.0.06 g/cm3(Predicted)
storage temp.	-20C
Löslichkeit	≥24.98 mg/mL in DMSO; ≥15.77 mg/mL in EtOH with ultrasonic; ≥18.1 mg/mL in H2O
Aggregatzustand	White solid
pka	9.17±0.20(Predicted)
Farbe	White to off-white

TAPI-1 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
TAPI-1 Trifluoroacetic Acid Salt is a TNF-a converting enzyme (TACE) inhibitor, which blocks shedding of cytokine receptors. It is a modulation of juxtamembrane cleavage (shedding) of angiotensin-converting enzyme by stalking glycosylation in relation to an alternative shedding protease.
Allgemeine Beschreibung
A structural analog of TAPI-0 (Cat. No. 579050) with similar in vitro efficacy for the inhibition of MMPs and TACE (TNF-α convertase; ADAM17). However, TAPI-1 is more stable in serum than TAPI-0. TAPI-1 Blocks the shedding of several cell surface proteins such as TNF-α, IL-6 receptor, and p60 and p80 TNF receptors. Inhibits constitutive (IC₅₀ = 8.09 μM) and muscarinic receptor-stimulated (IC₅₀ = 3.61 μM) sAPPa release in HEK-293 cells expressing muscarinic receptors. Also blocks the TACE-dependent constitutive release of co-transfected APP(695) (IC₅₀ = 920 nM).
Biologische Aktivität
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].
Biochem/physiol Actions
Primary TargetMMPs and TACE
Einzelnachweise
[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.

TAPI-1 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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