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Merck
CN

579051

TAPI-1

≥97% (HPLC), solid, MMP, TACE inhibitor, Calbiochem®

别名:

TAPI-1, N-(R)-[2-(Hydroxyaminocarbonyl)methyl]-4-methylpentanoyl-L-naphthylalanyl-L-alanine, 2-aminoethyl Amide, TNF-α Protease Inhibitor-1

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关于此项目

经验公式（希尔记法）:
C26H37N5O5
化学文摘社编号:
171235-71-5
分子量:
499.60
MDL number:
MFCD02684280
UNSPSC Code:
12352200
NACRES:
NA.77

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产品名称

TAPI-1, 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.

SMILES string

N(O)C(=O)CC(CC(C)C)C(=O)N[C@@H](Cc1cc2c(cc1)cccc2)C(=O)N[C@@H](C)C(=O)NCCN

InChI

1S/C26H37N5O5/c1-16(2)12-21(15-23(32)31-36)25(34)30-22(26(35)29-17(3)24(33)28-11-10-27)14-18-8-9-19-6-4-5-7-20(19)13-18/h4-9,13,16-17,21-22,36H,10-12,14-15,27H2,1-3H3,(H,28,33)(H,29,35)(H,30,34)(H,31,32)/t17-,21?,22-/m0/s1

InChI key

AWNBSWDIOCXWJW-OWHMDLSXSA-N

assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

color

white

solubility

methanol: 1 mg/mL
DMSO: 5 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

100

相关类别

Biochem/physiol Actions

Cell permeable: no
Primary Target
MMPs and TACE
Product does not compete with ATP.
Reversible: no
Target IC50: 8.09 µM and 3.61 µM blocking constitutive and muscarinic receptor-stimulated sAAPα release in HEK 293 cells expressing M3 muscarinic receptors, respectively

Disclaimer

Toxicity: Standard Handling (A)

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 converting enzyme/ADAM17). TAPI-1 also blocks the shedding of several cell surface proteins such as IL-6 receptor, p60 TNF receptor, and p80 TNF receptor. Blocks constitutive (IC50 = 8.09 µM) and muscarinic receptor-stimulated (IC50 = 3.61 µM) sAAPα release in HEK 293 cells expressing M3 muscarinic receptors. A 10 mM (500 µg/100 µl) solution of TAPI-1 (Cat. No. 579050) in DMSO is also available.
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).

Legal Information

Manufactured exclusively by Peptides International, Louisville, Kentucky, USA.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Slack, B.E., et al. 2001. Biochem. J.357, 787.
Vincent, B., et al. 2001. J. Biol. Chem.276, 37743.
Hooper, N.M., et al. 1997. Biochem. J.321, 265.
Crowe, P.D., et al. 1995. J. Exp. Med.181, 1205.
Mullberg, J., et al. 1995. J. Immunol.155, 5198.
Mohler, K.M., et al. 1994. Nature370, 218.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

存储类别

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

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