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TAPI-1 is a structural analog of TAPI-0, which shares similar in vitro efficacy for the inhibition of matrix metalloproteinases (MMPs) and TACE (TNF-α convertase; ADAM17). It is characterized by its enhanced stability in serum compared to TAPI-0. TAPI-1 effectively blocks the shedding of various cell surface proteins, including TNF-α, IL-6 receptor, and p60 and p80 TNF receptors. It also inhibits the constitutive and muscarinic receptor-stimulated release of sAPPa in HEK-293 cells expressing muscarinic receptors and the TACE-dependent constitutive release of co-transfected APP(695).

171235-71-5

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171235-71-5 Usage

Uses

Used in Pharmaceutical Industry:
TAPI-1 is used as an inhibitor for [application type] due to its ability to block the shedding of cell surface proteins and inhibit the release of sAPPa and APP(695). Its enhanced stability in serum makes it a promising candidate for the development of therapeutic agents targeting MMPs and TACE.
Used in Research Applications:
In the field of research, TAPI-1 is used as a research tool for studying the roles of MMPs and TACE in various biological processes. Its ability to inhibit the shedding of cell surface proteins and the release of sAPPa and APP(695) makes it a valuable asset for understanding the underlying mechanisms of these proteins and their involvement in disease progression.
Used in Drug Development:
TAPI-1 is used as a lead compound in the development of new drugs targeting MMPs and TACE. Its stability in serum and efficacy in inhibiting the shedding of cell surface proteins make it a potential candidate for the creation of novel therapeutic agents for various diseases, including those involving inflammation and tissue remodeling.

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.

Check Digit Verification of cas no

The CAS Registry Mumber 171235-71-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,7,1,2,3 and 5 respectively; the second part has 2 digits, 7 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 171235-71:
(8*1)+(7*7)+(6*1)+(5*2)+(4*3)+(3*5)+(2*7)+(1*1)=115
115 % 10 = 5
So 171235-71-5 is a valid CAS Registry Number.

171235-71-5SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 19, 2017

Revision Date: Aug 19, 2017

1.Identification

1.1 GHS Product identifier

Product name L-?Alaninamide, N-?[2-?[2-?(hydroxyamino)?-?2-?oxoethyl]?-?4-?methyl-?1-?oxopentyl]?-?3-?(2-?naphthalenyl)?-?L-?alanyl-?N-?(2-?aminoethyl)?- (9CI)

1.2 Other means of identification

Product number -
Other names -

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

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More Details:171235-71-5 SDS

171235-71-5Upstream product

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