PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selectivesigma 2 (σ2) receptoragonist with aK_iof 0.68 nM. PB28 dihydrochloride is also aσ1antagonist with aK_iof 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guinea pig bladder and ileum withEC₅₀values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulateSARS-CoV-2-humanprotein-protein interaction. PB28 dihydrochloride induces caspase-independentapoptosisand has antitumor activity^{[1][2][3][4][5]}.

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^[1].
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)^[1].
PB28 dihydrochloride inhibits cell growth of MCF7 and MCF7 ADR cells with IC₅₀s of 25 nM and 15 nM, respectively after 2-day treatment^[1].
PB28 dihydrochloride induces apoptosis through a caspase-independent pathway^[1].
PB28 dihydrochloride also reduces P-gp expression in a concentration- and time-dependent manner (approximately 60% in MCF7 and 90% in MCF7 ADR)^[1].
PB28 dihydrochloride displays antiproliferative and cytotoxic effects in both C6 rat glioma and SK-N-SH human neuroblastoma cell lines^[1].

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^[2].

443.49

Solid

C₂₄H₄₀Cl₂N₂O

172907-03-8

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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℃)

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

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-CDin 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 μL20% 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。