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DAPT;N-[N-(3,5-二氟苯乙酰)-L-丙氨酰]-S-苯甘氨酸叔丁酯 [GSI-IX, LY-374973];Calbiochem®, ≥98% (HPLC)

别名:DAPT, 一种γ-secretase 抑制剂;(3,5-二氟苯乙酰基)-L-丙氨酰基-L-2-苯基甘氨酸叔丁酯;N-[N-(3,5-Difluorophenacetyl)-L-alanyl]-S-phenylglycine t-butyl ester

CAS号 208255-80-5 经验分子式(希尔表示法) C23H26F2N2O4 分子量 432.46 MDL number MFCD04974585
货号(SKU): 565770
CAS号: 208255-80-5
MDL号: MFCD04974585
增值税发票 √ 免费货运 [顺丰 联邦] √
¥1,576.97

产品描述

Gamma-Secretase Inhibitor IX - CAS 208255-80-5, is a cell-permeable inhibitor of γ-secretase (Aβtotal IC₅₀ = 115 nM, Aβ42 IC₅₀ = 200 nM).

General description

A cell-permeable dipeptide that inhibits γ-secretase activity and suppresses Aβ production (Aβ total IC50 = 115 nM; Aβ42 IC50 = 200 nM). Reported to be functionally active in both HEK293 cells overexpressing human APP751 and neuronal cultures, however, it does not affect the secretion of amyloid-b precursor protein (APP). Effective in acutely lowering Ab in APPV717F-transgenic mice. Also effective in inhibiting the production of an ~6 kDa C-terminal cleavage product (CTFg) in HEK293 cells stably transfected with the Swedish mutant, βAPP695. Reported to reduce extracellular Aβ plaques and intracellular Aβ accumulation in 3xTgAD transgenic mice.

A cell-permeable dipeptide that suppresses Aβ production by blocking γ-secretase (Aβtotal IC50 = 115 nM, Aβ42 IC50 = 200 nM). Prevents Aβ34 generation in murine N2a cells and hAPP/hBACE-1 transfected human HEK 293 cells. Reported to be functionally active in both HEK 293 cells and neuronal cultures without affecting the secretion of amyloid-β precursor protein (APP). Also shown to lower Aβ levels acutely in APP-transgenic mice. Reported to reduce extracellular Aβ plaques and intracellular Aβ accumulation in 3xTgAD transgenic mice. A 25 mM (5 mg/462 µl) solution of γ-Secretase Inhibitor IX (Cat. No. 565784) in DMSO is also available.

包装

10 mg in Plastic ampoule

5 mg in Glass bottle

Packaged under inert gas

Biochem/physiol Actions

Cell permeable: yes

Product does not compete with ATP.

Reversible: no

Target IC50: 115 nM suppressing Aβtotal production; 200 nM suppressing Aβ42 production

Warning

Toxicity: Standard Handling (A)

Other Notes

Morohashi, Y., et al. 2006. J. Bio. Chem.Vol. 281, 14670.
Nishitomo, K. et al. 2006 J. Neurochem.99, 1555.
Oddo, S., et al. 2004. Neuron43, 321.
Dovey, H.F., et al. 2001. J. Neurochem.76, 173.
Sastre, M., et al. 2001. EMBO Rep.2, 835.
Vandermeeren, M., et al. 2001. Neurosci. Lett.315, 145.

性质

Quality Level100
assay≥98% (HPLC)
formlyophilized
mfr. no.Calbiochem®
storage conditionOK to freeze
protect from light
storage conditions-20C
solubilityDMSO: 20 mg/mL
shipped inambient


安全信息

个人防护装备 EyeshieldsGlovestype N95 (US)
RIDADR NONH for all modes of transport
WGK德国 WGK 3
商品规格
属性名称属性值
储存温度 Storage temp.2-8°C冷藏
全球实时库存 Availability √美国St. Louis ≥ 190 | 欧洲Eur. ≥ 66 | 東京Tokyo ≥ 82 | 香港与北京 ≥ 55
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