H-VAL-LYS-PHE-GLY-VAL-GLY-PHE-LYS-OH

H-VAL-LYS-PHE-GLY-VAL-GLY-PHE-LYS-OH化学性质

H-VAL-LYS-PHE-GLY-VAL-GLY-PHE-LYS-OH性质、用途与生产工艺

生物活性 CALP3 是一种类似于 Ca2+ 的肽，是有效的 Ca2+ 通道阻滞剂，可激活 Ca2+ 结合蛋白的 EF 手。CALP3 可以通过调节钙调蛋白 (CaM)，Ca2+ 通道和泵的活性来模拟增加的 [Ca2+]i。CALP3 具有控制诸如艾滋病或由于缺血引起的神经元丢失等疾病中细胞凋亡的潜力。
靶点

Ca ²⁺
体外研究

CALP3 (50, 100, 150, 200 μM) inhibits glutamate caused a large sustained increase in [Ca ²⁺ ] _i in a dose-dependent manner (IC ₅₀ =37.25 μM) in Fura-2-loaded neuronal cultures.
CALP3 (50, 100, 150, 200 μM) inhibits glutamate-induced cytotoxicity in a dose-dependent manner (IC ₅₀ =50.97 μM) in cultured rat neocortical neurons. CALP3 causes dose-dependent inhibition of apoptosis (IC ₅₀ =33.41 μM).
CALP3 (100 μM) inhibits apoptosis induced by HIV gp120 and SAg in Human T cells.
CALP3 (100 μM; 15 min pretreatment) reduces gossypol-induced necrosis and increases the fraction of live cells.
Cyclic-CALP3 is synthesized starting from Fmoc-Asp(PEG-PS)-OAl. Cyclic CALP3 is unable to inhibit Ca21 influx, and this peptide served as a negative control. Cyclic CALP3 does not inhibit the effect of glutamate.

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