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Key Documents

579051

Sigma-Aldrich

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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About This Item

经验公式(希尔记法):
C26H37N5O5
分子量:
499.60
分類程式碼代碼:
12352200
NACRES:
NA.77

product name

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.

品質等級

化驗

≥97% (HPLC)

形狀

solid

製造商/商標名

Calbiochem®

儲存條件

OK to freeze
desiccated (hygroscopic)
protect from light

顏色

white

溶解度

methanol: 1 mg/mL
DMSO: 5 mg/mL

運輸包裝

ambient

儲存溫度

−20°C

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 密鑰

AWNBSWDIOCXWJW-OWHMDLSXSA-N

一般說明

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).

生化/生理作用

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

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

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

其他說明

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.

法律資訊

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

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 1

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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