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| Product Name: | TAPI-1 | | Synonyms: | N1-((S)-1-((S)-1-(2-aminoethylamino)-1-oxopropan-2-ylamino)-3-(naphthalen-2-yl)-1-oxopropan-2-yl)-N4-hydroxy-2-isobutylsuccinamide;N-[2-[2-(Hydroxyamino)-2-oxoethyl]-4-methyl-1-oxopentyl]-3-(2-naphthalenyl)-L-alanyl-N-(2-aminoethyl)-L-alaninamide;N-[2-[2-(Hydroxyamino)-2-oxoethyl]-4-methyl-1-oxopentyl]-3-(2-naphthalenyl)-L-alanyl-N-(2-aminoethyl)-L-alaninamide TAPI-1;TAPI-1 trifluoroacetate;TNF-Α PROTEASE INHIBITOR-1 (TAPI-1);2-aminoethyl Amide;N-(R)-[2-(Hydroxyaminocarbonyl)methyl]-4-methylpentanoyl-L-naphthylalanyl-L-alanine;N-(R)-[2-(HYDROXYAMINOCARBONYL)METHYL]-4-METHYLPENTANOYL-L-NAPHTHYLALANYL-L-ALANINE; 2-AMINOETHYL AMIDE; TNF-Α PROTEASE INHIBITOR-1 | | CAS: | 171235-71-5 | | MF: | C26H37N5O5 | | MW: | 499.6 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 171235-71-5.mol |  |
| | TAPI-1 Chemical Properties |
| density | 1?+-.0.06 g/cm3(Predicted) | | storage temp. | -20C | | solubility | ≥24.98 mg/mL in DMSO; ≥15.77 mg/mL in EtOH with ultrasonic; ≥18.1 mg/mL in H2O | | form | White solid | | pka | 9.17±0.20(Predicted) |
| | TAPI-1 Usage And Synthesis |
| Uses | 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. | | General Description | 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). | | Biological Activity | 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 | | references | [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 Preparation Products And Raw materials |
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