σ1 Receptor antagonist-1
目录号 : KM3393 CAS No. : 1204401-49-9 纯度 : 98%

σ1 Receptor antagonist-1 是一种高效且选择性的 sigma 1 受体拮抗剂 (pKi=10.28)。σ1 Receptor antagonist-1 抑制细胞生长,在 G0/G1 期阻滞细胞周期并诱导 MCF-7/ADR 细胞凋亡 (apoptosis)。

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5mg
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25mg
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50mg
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100mg
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200mg 询价 In-stock
500mg 询价 In-stock

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生物活性

σ1 Receptor antagonist-1 is a highly potent and selective sigma 1 receptor antagonist (pKi=10.28). σ1 Receptor antagonist-1 inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells.

体外研究

σ1 Receptor antagonist-1 (compound 9) (10 μM; 48 hours) inhibits cell growth, arrests cell cycle at G0/G1 phase and induces apoptosis of MCF-7/ADR cells.

Cell Cycle Analysis

Cell Line: MCF-7/ADR, MCF-7 cells
Concentration: 10 μM
Incubation Time: 48 hours
Result: Increased the number of cells in G0/G1 (27.8%) and decreased those in S phase (46.7%), in a sigma 1-dependent manner. It selectively affects the high sigma 1 receptor expressing MCF-7/ADR but not the low sigma 1 receptor expressing MCF-7 cells.
体内研究

Pretreatment withσ1 Receptor antagonist-1 (1 mg/kg; s.c.) significantly increases the anti-nociceptive effect produces by morphine over the entire time course starting at 60 min.

Animal Model: Male CD-1 mice
Dosage: 1 mg/kg
Administration: S.c.
Result: Significantly increased the anti-nociceptive effect produced by morphine over the entire time course starting at 60 min.
分子式
C21H23NOs
分子量
337.48
CAS号
1204401-49-9
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
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (296.31 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9631 mL 14.8157 mL 29.6314 mL
5 mM 0.5926 mL 2.9631 mL 5.9263 mL
10 mM 0.2963 mL 1.4816 mL 2.9631 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。-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    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.41 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.41 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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