TAPI-1
- Product Name
- TAPI-1
- CAS No.
- 171235-71-5
- Chemical Name
- TAPI-1
- Synonyms
- TAP 1;CS-1499;(S,S)-TAPI-1;(2S,2S)-TAPI-1;TAPI-1 TFA Salt;2-aminoethyl Amide;TAPI-1 trifluoroacetate;TNF-α Protease Inhibitor-1;TNF-Α PROTEASE INHIBITOR-1 (TAPI-1);N-(R)-[2-(Hydroxyaminocarbonyl)methyl]-4-methylpentanoyl-L-naphthylalanyl-L-alanine
- CBNumber
- CB22729657
- Molecular Formula
- C26H37N5O5
- Formula Weight
- 499.6
- MOL File
- 171235-71-5.mol
TAPI-1 Property
- 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)
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- 579051
- Product name
- TAPI-1 - CAS 171235-71-5 - Calbiochem<br />TAPI-1, CAS 171235-71-5, is a structural analog of TAPI-0 with similar in vitro efficacy for the inhibition of MMPs and TACE. Blocks the shedding of several cell surface proteins.
- Packaging
- 1mg
- Price
- $475
- Updated
- 2024/03/01
- Product number
- 18505
- Product name
- TAPI-1
- Purity
- ≥98%
- Packaging
- 500μg
- Price
- $149
- Updated
- 2024/03/01
- Product number
- 18505
- Product name
- TAPI-1
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $253
- Updated
- 2024/03/01
- Product number
- 18505
- Product name
- TAPI-1
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $894
- Updated
- 2024/03/01
- Product number
- 493389
- Product name
- TAP1
- Packaging
- 100ul
- Price
- $529
- Updated
- 2021/12/16
TAPI-1 Chemical Properties,Usage,Production
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
Raw materials
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