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PB28 dihydrochloride

CAS No. : 172907-03-8

MCE 站：PB28 dihydrochloride

产品活性：PB28 dihydrochloride，一种环己基哌嗪衍生物，是一种 K_i 值为 0.68 nM 的高亲和力和选择性 sigma 2 (σ2) 受体激动剂。PB28 dihydrochloride 也是一种 σ1 受体拮抗剂，K_i 为 0.38 nM，对其他受体的亲和力较小。PB28 dihydrochloride 抑制豚鼠膀胱和回肠中的电诱发抽搐，其 EC₅₀ 值分别为 2.62 μM 和 3.96 μM。PB28 dihydrochloride 可以调节 SARS-CoV-2-人之间的蛋白质与蛋白质的相互作用。PB28 dihydrochloride 可诱导非 caspase 依赖性的细胞凋亡 (apoptosis)，并具有抗肿瘤活性。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Apoptosis  |  Anti-infection

作用靶点：Sigma Receptor  |  Apoptosis  |  SARS-CoV

In Vitro: PB28 (15-25 nM; 24-48 hours; MCF7 ａnd MCF7 ADR cells) dihydrochloride treatment shows an accumulation in the G0-G1 phase for MCF7 ａnd MCF7 ADR cells that are time ａnd concentration independent.
PB28 dihydrochloride has a higher σ2 receptor affinity expressed as K_i (0.28 nM ａnd 0.17 nM in MCF7 ａnd MCF7 ADR cells, respectively) than σ1 receptor affinity (13.0 nMand 10.0 nM, respectively).
PB28 dihydrochloride inhibits cell growth of MCF7 ａnd MCF7 ADR cells with IC₅₀s of 25 nM ａnd 15 nM, respectively after 2-day treatment.
PB28 dihydrochloride induces apoptosis through a caspase-independent pathway.
PB28 dihydrochloride also reduces P-gp expression in a concentration- ａnd time-dependent manner (approximately 60% in MCF7 ａnd 90% in MCF7 ADR).
PB28 dihydrochloride displays antiproliferative ａnd cytotoxic effects in both C6 rat glioma ａnd SK-N-SH human neuroblastoma cell lines.

In Vivo: PB28 (10.7 mg/mL; intraperitoneal injection; daily; for two weeks; C57BL/6 female mice) dihydrochloride treatment inhibits tumor growth in Panc02 tumor burden mice. PB28 also conferres a survival advantage for mice.

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