PB28 dihydrochloride
目录号 : KM3953 CAS No. : 172907-03-8 纯度 : 98%

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。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
50mg 询价 In-stock
100mg 询价 In-stock

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生物活性

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.

体外研究

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 Ki (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.

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.
体内研究

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.

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.
分子式
C24H40Cl2N2O
分子量
443.49
CAS号
172907-03-8
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
The molarity calculator equation
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The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2