Bioactivity | β-Sheet Breaker Peptide iAβ5 is a potent degrader of cerebral amyloid-beta (Abeta). Abeta deposition is associatied with the Alzheimer disease (AD), due to its related toxicity linked to its beta-sheet conformation and/or aggregation. β-Sheet Breaker Peptide iAβ5 reproducibly induces in vivo disassembly of fibrillar amyloid deposits. Thus, β-Sheet Breaker Peptide iAβ5 prevents and/or reverses neuronal shrinkage caused by Abeta, and reduces the extent of interleukin-1beta positive microglia-like cells that surround the Abeta deposits. β-Sheet Breaker Peptide iAβ5 reduces the size and/or number of cerebral amyloid plaques in AD. β-Sheet Breaker Peptide iAβ5 labeled by hydrophobic benzyl alcohol (HBA) tag, can be used for quantitative assay by showing vivid blue color under acidic conditions[1][2][3]. | ||||||
Invitro | β-Sheet Breaker Peptide iAβ5 (1.5 μg/μL;7 天) 与 Aβ1-42 (0.5 μg/μL) 孵育 7 天,抑制淀粉样蛋白 β 蛋白原纤维形成,在体外分解预先形成的原纤维,并防止细胞培养中原纤维诱导的神经元死亡[1]。β-Sheet Breaker Peptide iAβ5 (60 μM;48 小时) 在用 50 μM 聚集的 Aβ1-42 处理 2 天的人神经母细胞瘤 (IMR-32) 细胞中显示出不显着的细胞毒性[1]。 | ||||||
In Vivo | β-Sheet Breaker Peptide iAβ5 (100 nmol/大鼠;杏仁核内注射;7 天) 与 Aβ1-42 (5 nmol) 共同注射到大鼠杏仁核中,阻断组织培养中的 Aβ1-42 神经毒性,以及大鼠模型中淀粉样原纤维的形成[1]。β-Sheet Breaker Peptide iAβ5 (100 nmol/大鼠,200 nmol/大鼠;杏仁核内注射;7 天) 在 Aβ1-42 (5 nmol) 处理后注射,诱导体内预先存在的 Aβ 原纤维的分解,并导致逆转或预防 Aβ 诱导的大鼠模型组织病理学改变[2]。 | ||||||
Name | β-Sheet Breaker Peptide iAβ5 | ||||||
CAS | 182912-74-9 | ||||||
Sequence | Leu-Pro-Phe-Phe-Asp | ||||||
Shortening | LPFFD | ||||||
Formula | C33H43N5O8 | ||||||
Molar Mass | 637.72 | ||||||
Appearance | Solid | ||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||
Storage | Sealed storage, away from moisture and light, under nitrogen
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen) |
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Reference | [1]. Soto C, et al. Beta-sheet breaker peptides inhibit fibrillogenesis in a rat brain model of amyloidosis: implications for Alzheimer's therapy. Nat Med. 1998 Jul;4(7):822-6. [2]. Sigurdsson EM, et al. In vivo reversal of amyloid-beta lesions in rat brain. J Neuropathol Exp Neurol. 2000 Jan;59(1):11-7. [3]. Okada Y, et al. Acid-Triggered Colorimetric Hydrophobic Benzyl Alcohols for Soluble Tag-Assisted Liquid-Phase Synthesis. Org Lett. 2015 Sep 4;17(17):4264-7. |