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(R)-TAPI-2

Cat. No. M30492
(R)-TAPI-2 Structure
Synonym:

(R)-TNF Protease Inhibitor 2

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Biological Activity

(R)-TAPI-2 is the isomer of TAPI-2. TAPI-2 (TNF Protease Inhibitor 2) is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC50 of 20 μM for MMP. TAPI-2 blocks the entry of infectious SARS-CoV.

Chemical Information
Molecular Weight 415.53
Formula C19H37N5O5
CAS Number 689284-12-6
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Nadège Poncet, et al. Cell Signal. Epidermal growth factor receptor transactivation is implicated in IL-6-induced proliferation and ERK1/2 activation in non-transformed prostate epithelial cells

[2] Cécile Delarasse, et al. J Biol Chem. The purinergic receptor P2X7 triggers alpha-secretase-dependent processing of the amyloid precursor protein

[3] Qiongman Kong, et al. J Neurochem. Interleukin-1beta enhances nucleotide-induced and alpha-secretase-dependent amyloid precursor protein processing in rat primary cortical neurons via up-regulation of the P2Y(2) receptor

[4] Marcia L Moss, et al. Anal Biochem. Fluorescent substrates for the proteinases ADAM17, ADAM10, ADAM8, and ADAM12 useful for high-throughput inhibitor screening

[5] Jean M Camden, et al. J Biol Chem. P2Y2 nucleotide receptors enhance alpha-secretase-dependent amyloid precursor protein processing

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Keywords: (R)-TAPI-2, (R)-TNF Protease Inhibitor 2 supplier, inhibitors, activators

 
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