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质量水平
检测方案
≥97% (HPLC)
形式
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
desiccated (hygroscopic)
protect from light
颜色
white
溶解性
methanol: 1 mg/mL
DMSO: 5 mg/mL
运输
ambient
储存温度
−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 key
AWNBSWDIOCXWJW-OWHMDLSXSA-N
一般描述
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
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
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.
其他说明
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.
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.
法律信息
Manufactured exclusively by Peptides International, Louisville, Kentucky, USA.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 1
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Neuroscience, 453, 222-236 (2020-12-01)
The p75 neurotrophin receptor (p75NTR) is a multifunctional protein that regulates cellular responses to pathological conditions in specific regions of the nervous system. Activation of p75NTR in certain neuronal populations induces proteolytic processing of the receptor, thereby generating p75NTR fragments
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