PB28 dihydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PB28 dihydrochloride，一种环己基哌嗪衍生物，是一种 Ki 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，Ki 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。

PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a Ki of 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulate SARS-CoV-2-human protein-protein interaction. PB28 dihydrochloride induces caspase-independent apoptosis and has antitumor activity.

Cell Viability Assay Cell Line:MCF7 and MCF7 ADR cells Concentration:25 nM and 15 nM Incubation Time:24 hours, 48 hours Result:Showed an accumulation in the G0-G1 phase for MCF7 and MCF7 ADR cells that were time and concentration independent.

Animal Model:C57BL/6 female mice (10 weeks old) injected with Panc02 cells Dosage:10.7 mg/mL Administration:Intraperitoneal injection; daily; for two weeks Result:Inhibited tumor growth in Panc02 tumor burden mice.

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Others

Other Targets

Others

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172907-03-8

443.49

C24H40Cl2N2O

>98% (HPLC)

In Vitro:? H2O 中的溶解度 : 9 mg/mL (20.29 mM; 超声加热助溶) DMSO 中的溶解度 : 5 mg/mL (11.27 mM; 超声助溶 (<60°C)

COC1=CC=CC2=C1CCCC2CCCN3CCN(C4CCCCC4)CC3.Cl.Cl

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(-20℃)

With Ice Pack

≥ 2 years