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製品番号: HY-108511A

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PB28

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

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CAS 番号: 172906-90-0
分子式: C₂₄H₃₈N₂O
分子量:370.57

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

PB28 構造式

CAS 番号: 172906-90-0

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
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生物活性

製品説明

IC₅₀ & Target

Ki: 0.68 nM (σ2 receptor); 0.38 nM (σ1 receptor)^[4]

Sigma Receptor アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	EC₅₀	0.55 μM Compound: PB-28	Inhibition of human Pgp mediated [3H]vinblastine transport in human Caco-2 cells Inhibition of human Pgp mediated [3H]vinblastine transport in human Caco-2 cells	[PMID: 17936633]
MCF7	EC₅₀	27.4 μM Compound: PB, PB28	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 23415062]
MCF7	EC₅₀	31.2 μM Compound: PB, PB28	Antiproliferative activity against human MCF7 cells transfected with human sigma1 receptor after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells transfected with human sigma1 receptor after 48 hrs by MTT assay	[PMID: 23415062]
MCF7	IC₅₀	1.2 nM Compound: 1, PB28	Displacement of [3H]DTG from sigma 2 receptor in human MCF7 cells after 45 mins by FACS analysis Displacement of [3H]DTG from sigma 2 receptor in human MCF7 cells after 45 mins by FACS analysis	[PMID: 24697311]
MCF7	IC₅₀	4.27 nM Compound: 1, PB28	Displacement of 2-(6-{1-[3-(4-Cyclohexylpiperazin-1-yl)propyl]-1,2,3,4-tetrahydronaphthalen-5-yloxy}hexyl)-5-dimethylamino-1H-isoindole-1,3(2H)-dione from sigma 2 receptor in human MCF7 cells after 45 mins by FACS analysis Displacement of 2-(6-{1-[3-(4-Cyclohexylpiperazin-1-yl)propyl]-1,2,3,4-tetrahydronaphthalen-5-yloxy}hexyl)-5-dimethylamino-1H-isoindole-1,3(2H)-dione from sigma 2 receptor in human MCF7 cells after 45 mins by FACS analysis	[PMID: 24697311]
PC-3	EC₅₀	64.2 μM Compound: 36, PB-28	Cytotoxicity against human PC3 cells assessed as LDH release after 24 hrs Cytotoxicity against human PC3 cells assessed as LDH release after 24 hrs	[PMID: 19053780]
RPMI-8226	IC₅₀	9.29 μM Compound: 3, PB28	Cytotoxicity against human RPMI8226 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human RPMI8226 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 24331758]
SK-N-SH	EC₅₀	9.04 μM Compound: (+/-)-1, PB-28	Antiproliferative activity against human SK-N-SH cells after 48 hts by MTT assay Antiproliferative activity against human SK-N-SH cells after 48 hts by MTT assay	[PMID: 21229979]
SK-N-SH	EC₅₀	9.97 μM Compound: 7, PB-28	Antiproliferative activity against human SK-N-SH cells after 48 hrs by MTT assay Antiproliferative activity against human SK-N-SH cells after 48 hrs by MTT assay	[PMID: 19842660]

体外実験

PB28 (15-25 nM; 24-48 hours; MCF7 and MCF7 ADR cells) treatment shows an accumulation in the G0-G1 phase for MCF7 and MCF7 ADR cells that are time and concentration independent^[1].
PB28 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 inhibits cell growth of MCF7 and MCF7 ADR cells with IC₅₀s of 25 nM and 15 nM, respectively after 2-day treatment^[1].
PB28 induces apoptosis through a caspase-independent pathway^[1].
PB28 also reduces P-gp expression in a concentration- and time-dependent manner (approximately 60% in MCF7 and 90% in MCF7 ADR)^[1].
PB28 displays antiproliferative and cytotoxic effects in both C6 rat glioma and SK-N-SH human neuroblastoma cell lines^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cycle Analysis^[1]

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.

体内実験

PB28 (10.7 mg/mL; intraperitoneal injection; daily; for two weeks; C57BL/6 female mice) treatment inhibits tumor growth in Panc02 tumor burden mice. PB28 also conferres a survival advantage for mice^[2].

MedChemExpress (MCE) 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^[2]
Dosage:

10.7 mg/mL
Administration:

Intraperitoneal injection; daily; for two weeks
Result:

Inhibited tumor growth in Panc02 tumor burden mice.

Related Protocols :

化学情報

CAS 番号 172906-90-0
分子量 370.57
分子式 C₂₄H₃₈N₂O
SMILES

COC1=CC=CC2=C1CCCC2CCCN3CCN(C4CCCCC4)CC3
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (273 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Amalia Azzariti, et al. Cyclohexylpiperazine Derivative PB28, a sigma2 Agonist and sigma1 Antagonist Receptor, Inhibits Cell Growth, Modulates P-glycoprotein, and Synergizes With Anthracyclines in Breast Cancer. Mol Cancer Ther. 2006 Jul;5(7):1807-16. [Content Brief]

[2]. Maria Laura Pati, et al. Sigma-2 Receptor Agonist Derivatives of 1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) Induce Cell Death via Mitochondrial Superoxide Production and Caspase Activation in Pancreatic Cancer. [Content Brief]

[3]. Nicola A Colabufo, et al. A New Method for Evaluating sigma(2) Ligand Activity in the Isolated Guinea-Pig Bladder. Naunyn Schmiedebergs Arch Pharmacol. 2003 Aug;368(2):106-12. [Content Brief]

[4]. Francesco Berardi, et al. Exploring the Importance of Piperazine N-atoms for sigma(2) Receptor Affinity and Activity in a Series of Analogs of 1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28). J Med Chem. 2009 Dec 10 [Content Brief]

[5]. David E Gordon, et al. A SARS-CoV-2-Human Protein-Protein Interaction Map Reveals Drug Targets and Potential Drug-Repurposing. bioRxiv. 2020 Mar 22;2020.03.22.002386. [Content Brief]

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Keywords

MOQ

Minimum order quantity

100 mg

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