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TAPI-1 ADAM17 Inhibitor

Name: TAPI-1
Brand: Selleck Chemicals
SKU: S7434
Availability: InStock
Rating: 5 (25 reviews)

Cat.No.S7434

(S,S)-TAPI-1 is an isomer of TAPI-1. TAPI-1 is an ADAM17/TACE inhibitor, which blocks shedding of cytokine receptors. TAPI-1 is also an inhibitor of Matrix Metalloproteinase (MMP).

Chemical Structure

Molecular Weight: 499.60

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Quality Control

Batch: Purity: 99.35%

99.35

Related Targets	Bcl-2 Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras
Featured Inhibitors	Y-27632 Dihydrochloride SB431542 CHIR-99021 (Laduviglusib) RMC-7977 RMC-6236 (Daraxonrasib) MRTX1133 MG132 Z-VAD-FMK VT3989 IAG933

Solubility

In vitro
Batch:

DMSO : 99 mg/mL (198.15 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 99 mg/mL

Ethanol : 99 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.950mg/ml (9.91mM)	Taking the 1 mL working solution as an example, add 50 μL of 99 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	499.60	Formula	C₂₆H₃₇N₅O₅	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	171235-71-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C)CC(CC(=O)NO)C(=O)NC(CC1=CC2=CC=CC=C2C=C1)C(=O)NC(C)C(=O)NCCN

Mechanism of Action

Targets/IC₅₀/Ki	ADAM17/TACE MMP
In vitro	TAPI-1 prevents unstimulated and PMA-induced release of the soluble forms of TNF-alpha, p60 TNFR, and IL-6R from the monocytic cell line, THP-1, and from human peripheral blood monocytes. TAPI also inhibits LPS-induced shedding of the p60 TNFR and TNF-alpha from monocytes. TAPI-1 inhibits TACE-dependent constitutive release of co-transfected APP(695). TAPI-1 attenuates Ang II-induced EGFR transactivation and cell proliferation in human HSC line LI90. TAPI-1 with the EGFR inhibitor AG1478 exhibits deactivated AREG/EGFR/ERK signaling pathway and reduces pro-inflammatory cytokines release in pSS salivary gland-derived epithelial cells.
In vivo	TAPI-1 is an ADAM17/TACE inhibitor, which blocks shedding of cytokine receptors
References	[1] https://pubmed.ncbi.nlm.nih.gov/7594530/ [2] https://pubmed.ncbi.nlm.nih.gov/11463349/ [3] https://pubmed.ncbi.nlm.nih.gov/24412389/ [4] https://pubmed.ncbi.nlm.nih.gov/24664458/ [5] https://pubmed.ncbi.nlm.nih.gov/31822434/ [6] https://pubmed.ncbi.nlm.nih.gov/31154904/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-EGFR(Y1068) / EGFR / p-AKT / AKT / p-ERK / ERK		31426531

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Handling Instructions

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