TAPI-1,1MG,579051-1MGCN,Sigma

销售价: ¥ 5020.03 / 件
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订货号 0BV9647
品牌型号 Sigma 579051-1MGCN
货期 询货期
最小订货量 1件
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产品介绍 Product Description

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).


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


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.


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.


Legal Information

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


Disclaimer

Toxicity: Standard Handling (A)


技术参数 Specifications
Quality Segment100
assay≥97% (HPLC)
formsolid
manufacturer/tradenameCalbiochem®
storage conditionOK to freeze,desiccated (hygroscopic),protect from light
color white
solubilitymethanol: 1 mg/mL,DMSO: 5 mg/mL
shipped inambient
storage temp.−20°C
SMILES stringN(O)C(=O)CC(CC(C)C)C(=O)N[C@@H](Cc1cc2c(cc1)cccc2)C(=O)N[C@@H](C)C(=O)NCCN
InChI1S/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 keyAWNBSWDIOCXWJW-OWHMDLSXSA-N
长度(mm)
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高度(mm)
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