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。
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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。 |
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]. |
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 |
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 |