PB28 dihydrochloride|cas:172907-03-8|西域试剂

PB28 dihydrochloride,99.97%

产品编号：Bellancom-108511| CAS NO：172907-03-8| 分子式：C₂₄H₄₀Cl₂N₂O| 分子量：443.49

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-108511	￥1400.00	杭州北京（现货）
Bellancom-108511	￥2200.00	杭州北京（现货）
Bellancom-108511	￥4400.00	杭州北京（现货）
Bellancom-108511	￥7000.00	杭州北京（现货）
Bellancom-108511	￥11200.00	杭州北京（现货）

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PB28 dihydrochloride

产品介绍

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。

生物活性

PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a K_i of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a K_i 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^[4]^[5].

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 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
(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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

H₂O : 9 mg/mL (20.29 mM; Need ultrasonic and warming)

DMSO : 5 mg/mL (11.27 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2548 mL	11.2742 mL	22.5484 mL
5 mM	0.4510 mL	2.2548 mL	4.5097 mL
10 mM	0.2255 mL	1.1274 mL	2.2548 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1 mg/mL (2.25 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.25 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1 mg/mL (2.25 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.25 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1 mg/mL (2.25 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.25 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。