Rimcazole dihydrochloride(Synonyms: BW 234U dihydrochloride)

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Rimcazole dihydrochloride (Synonyms: BW 234U dihydrochloride) 纯度: 99.80%

Rimcazole (BW 234U) dihydrochloride 是一种咔唑衍生物,部分用作 σ 受体拮抗剂。Rimcazole dihydrochloride 以中等亲和力结合多巴胺转运蛋白并抑制多巴胺摄取。Rimcazole dihydrochloride 可以减弱可卡因诱导的运动活动和致敏作用。Rimcazole dihydrochloride 也可用于癌症的研究。

Rimcazole dihydrochloride(Synonyms: BW 234U dihydrochloride)

Rimcazole dihydrochloride Chemical Structure

CAS No. : 75859-03-9

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Rimcazole dihydrochloride 相关产品

相关化合物库:

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生物活性

Rimcazole (BW 234U) dihydrochloride is a carbazole derivative that acts in part as a sigma (σ) receptor antagonist. Rimcazole dihydrochloride also binds with moderate affinity to the dopamine transporter and inhibit dopamine uptake. Rimcazole dihydrochloride can attenuate cocaine-induced locomotor activity and sensitization. Rimcazole dihydrochloride also can be used for the research of cancer[1][2][3][4].

IC50 & Target

sigma (σ) receptor[1]
dopamine transporter[1]

体外研究
(In Vitro)

Rimcazole (1-50 μM; 24-48 h) concentration-dependently decreases the number HCT-116p53+/+ cells[2].
Rimcazole (50 μM; 1-24 h) dihydrochloride induces a transient accumulation of HIF-1α protei in cancer cells (HCT-116p53+/+ and MDA MB 231 cells) but not in normal human dermal fibroblasts[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

Cell Line: HCT-116p53+/+ cells
Concentration: 50 μM
Incubation Time: 1, 2, 3, 5, 6, 24 hours
Result: Accumulation of HIF-1α protein, maximal at 6 h.
No change in p53 protein levels.
HIF-1α protein levels returned to normal steady-state levels within 24 h.

分子量

394.38

Formula

C21H29Cl2N3

CAS 号

75859-03-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

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

溶解性数据
In Vitro: 

DMSO : 12.5 mg/mL (31.70 mM; ultrasonic and warming and heat to 60°C)

H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5356 mL 12.6781 mL 25.3563 mL
5 mM 0.5071 mL 2.5356 mL 5.0713 mL
10 mM 0.2536 mL 1.2678 mL 2.5356 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 and light)。-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: ≥ 1.25 mg/mL (3.17 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (3.17 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 12.5 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: ≥ 1.25 mg/mL (3.17 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (3.17 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 12.5 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: ≥ 1.25 mg/mL (3.17 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (3.17 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 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
  • [1]. Gilmore DL, et, al. Review of the pharmacological and clinical profile of rimcazole. CNS Drug Rev. Spring 2004;10(1):1-22.

    [2]. Achison M, et, al. HIF-1alpha contributes to tumour-selective killing by the sigma receptor antagonist rimcazole. Oncogene. 2007 Feb 22;26(8):1137-46.

    [3]. Matsumoto RR, et, al. Rimcazole analogs attenuate the convulsive effects of cocaine: correlation with binding to sigma receptors rather than dopamine transporters. Neuropharmacology. 2001 Dec;41(7):878-86.

    [4]. Job MO, et, al. A behavioral economic analysis of the effects of rimcazole on reinforcing effects of cocaine injection and food presentation in rats. Psychopharmacology (Berl). 2019 Dec;236(12):3601-3612.

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