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TAPI-1

Cat. No. M3634
TAPI-1 Structure
Size Price Availability Quantity
1mg USD 200  USD200 In stock
5mg USD 730  USD730 In stock
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Quality Control & Documentation
Biological Activity

TAPI blocks the spontaneous and PMA-induced release of TNF-alpha from transfected cells. TAPI-1, an inhibitor of ADAMs, reduced constitutive and muscarinic receptor-stimulated sAPP alpha release in HEK-293 cells stably expressing M3 muscarinic receptors. 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.

Protocol (for reference only)
Cell Experiment
Cell lines LI90 cells
Preparation method Seeding five thousand cells into each well of 96-well plates and assessing their viability by CellTiter-Glo Luminescent Cell Viability assay. Upon serum deprivation for 24 h, tresting the cells with Ang II for 60 h with and without pretreatment with each inhibitor and antagonist. Then addint The assay substrates to each well on the plate and using a luminometer to evaluate the samples
Concentrations 20 μM
Incubation time 60 hours
Animal Experiment
Animal models
Formulation
Dosages
Administration
Chemical Information
Molecular Weight 499.60
Formula C26H37N5O5
CAS Number 171235-71-5
Solubility (25°C) DMSO ≥ 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Slack BE, et al. Biochem J. Constitutive shedding of the amyloid precursor protein ectodomain is up-regulated by tumour necrosis factor-alpha converting enzyme.

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