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Rimcazole 2HCl {[allProObj[0].p_purity_real_show]}

货号:A363715 同义名: BW 234U dihydrochloride;Rimcazole dihydrochloride

Rimcazole 2HCl 是一种咔唑衍生物,部分用作 σ 受体拮抗剂。它以中等亲和力结合多巴胺转运蛋白并抑制多巴胺摄取,从而减弱运动活动和致敏作用,也可用于癌症研究。

Rimcazole 2HCl 化学结构 CAS号:75859-03-9
Rimcazole 2HCl 化学结构
CAS号:75859-03-9
Rimcazole 2HCl 3D分子结构
CAS号:75859-03-9
Rimcazole 2HCl 化学结构 CAS号:75859-03-9
Rimcazole 2HCl 3D分子结构 CAS号:75859-03-9
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Rimcazole 2HCl 纯度/质量文件 产品仅供科研

货号:A363715 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 D1 receptor D2 receptor D3 receptor D4 receptor D5 receptor DAT Dopamine receptor 其他靶点 纯度
Penfluridol +

Dopamine receptor, Ki: 1.6 μM

98%
Ansofaxine HCl ++

Dopamine receptor, IC50: 491 nM

98%
Tetrahydroberberine,THB +

D2 receptor, pKi: 6.08

98+%
Prochlorperazine Maleate 95%
Olanzapine 99+%
Trifluoperazine ++++

Dopamine D2 receptor, IC50: 1.1 nM

98%
Ropinirole hydrochloride ++

D2 receptor, Ki: 29 nM

99%
Lurasidone ++++

D2 receptor, Ki: 1 nM

98%
Levosulpiride 99+%
Pridopidine 95%
Metoclopramide 99+%
Molindone HCl 98%
Sulpiride 99+%
Perospirone ++++

D2 receptor, Ki: 1.4 nM

99%
Perospirone HCl ++++

D2 receptor, Ki: 1.4 nM

98+%
Phenothiazine 98%
Pimozide +

Dopamine D1 receptor, Ki: 6600 nM

+++

Dopamine D2 receptor, Ki: 3.0 nM

++++

Dopamine D3 receptor, Ki: 0.83 nM

98%
Rotundine ++

D1 receptor, IC50: 166 nM

+

D2 receptor, IC50: 1.47 μM

+

D3 receptor, IC50: 3.25 μM

98%
Domperidone 99+%
ONC206 97%
Pimethixene maleate ++

Dopamine D1 Receptor, pKi: 6.37

+++

Dopamine D2 Receptor, pKi: 8.19

++

Dopamine D4.4 Receptor, pKi: 7.54

97%
Loxapine succinate ++

D1 receptor (human), Ki: 26 nM

D2 receptor (Human), Ki: 62 nM

++

D2 receptor (human), Ki: 24 nM

D2 receptor (bovine), Ki: 26 nM

+++

D4 receptor (human), Ki: 7.5 nM

99%
Chlorprothixene +++

D1 receptor, Ki: 18 nM

+++

D2 receptor, Ki: 2.96 nM

+++

D3 receptor, Ki: 4.56 nM

+++

D5 receptor, Ki: 9 nM

98%
SCH-23390 HCl ++++

D1 dopamine receptor, Ki: 0.2 nM

++++

D5 dopamine receptor, Ki: 0.3 nM

98%
MPP+ iodide 97%
σ1 Receptor antagonist-1 +

DAT, pKi: 5.8

97%
Benztropine mesylate ++

DAT, IC50: 118 nM

98%
Azaperone 98%
Ziprasidone HCl 98+%
Paliperidone 98%
Alizapride HCl 99+%
Amisulpride 98%
Quetiapine hemifumarate Adrenergic Receptor 98%
Clozapine N-oxide 99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Rimcazole 2HCl 生物活性

描述 Rimcazole 2HCl is a carbazole derivative that acts in part as a σ-receptor antagonist. Rimcazole 2HCl also binds with moderate affinity to the dopamine transporter and inhibits dopamine uptake. Rimcazole 2HCl reduces locomotor activity and sensitivity. Rimcazole 2HCl has also been used in cancer research[ 1][2][3][4].At a concentration range of 1-50 μM, acting for 24-48 hours, Rimcazole 2HCl reduces the number of HCT-116 cells (p53+/+ ) in a concentration-dependent manner[2].At a concentration of 50 μM, acting for 1-24 h, Rimcazole 2HCl induces transient accumulation of the HIF-1α protein in cancer cells (HCT-116 p53+/+ and MDA MB 231 cells), with a maximum at 6 h, whereas it does not in normal human dermal fibroblasts[2].

Rimcazole 2HCl 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.

Rimcazole 2HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.54mL

0.51mL

0.25mL

12.68mL

2.54mL

1.27mL

25.36mL

5.07mL

2.54mL

Rimcazole 2HCl 技术信息

CAS号75859-03-9
分子式C21H29Cl2N3
分子量 394.381
别名 BW 234U dihydrochloride;Rimcazole dihydrochloride;Rimcazole dihydrochloride, Rimcazole 2HCl;BW 234U
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

溶解度

DMSO: 12 mg/mL(30.43 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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