货号:A1365943
同义名:
Calhex 231 hydrochloride
Calhex 231 HCl是一种通过负变构调节抑制钙敏感受体 (CaSR) 的化合物,能够阻断 Ca2+ 诱导的肌醇磷酸酯积累,IC50 为 0.39 μM。该化合物广泛用于糖尿病性心肌病 (DCM) 及其他钙调节相关疾病的研究。


| 规格 | 价格 | 会员价 | 库存 | 数量 | |||
|---|---|---|---|---|---|---|---|
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| 产品名称 | CaSR ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| NPS-2143 |
++++
Ca(2+) receptor, IC50: 43 nM |
98+% | |||||||||||||||||
| 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。 | |||||||||||||||||||
| Concentration | Treated Time | Description | References | |
| rabbit mesenteric artery smooth muscle cells | 1 µM, 3 µM, 10 µM | inhibited whole-cell VGCC currents by approximately 25%, 60%, and 95% respectively | Eur J Pharmacol. 2016 Nov 15;791:659-668 | |
| rabbit mesenteric artery endothelial cells (ECs) | 3 μM | 20 min | To investigate the inhibitory effect of Calhex-231 on CaSR-mediated NO production, results showed that Calhex-231 inhibited [Ca2+]o-induced NO production. | Vascul Pharmacol. 2016 May;80:75-84 |
| rabbit mesenteric artery endothelial cells (ECs) | 3 μM | 30 min | To investigate the inhibitory effect of Calhex-231 on CaSR-mediated vasorelaxation, results showed that Calhex-231 significantly inhibited [Ca2+]o-induced vasorelaxation. | Vascul Pharmacol. 2016 May;80:75-84 |
| mouse descending colon mucosa | 10 μM | inhibited Gln-induced changes in Isc | Br J Pharmacol. 2013 Nov;170(5):1092-101 | |
| HepG2 cells | 10 µM | 120 h | Inhibits CaSR activation, preventing HepG2 cell senescence and mitochondrial dysfunction | Int J Mol Sci. 2023 Mar 9;24(6):5217 |
| SW872 pre-adipocytes | 10 µM | 16 h | Inhibits calcium-sensing receptor (CaSR) activation, preventing pro-inflammatory factor secretion from pre-adipocytes | Int J Mol Sci. 2023 Mar 9;24(6):5217 |
| rat mesenteric artery endothelial cells | 1 μM and 3 μM | Calhex 231 inhibited calindol-induced myocyte hyperpolarization, indicating its role as a negative allosteric modulator of CaR. | Br J Pharmacol. 2008 Jun;154(3):652-62 |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | PYY knockout mice | 10 μM | Inhibited Gln-induced changes in Isc | Br J Pharmacol. 2013 Nov;170(5):1092-101 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.26mL 0.45mL 0.23mL |
11.28mL 2.26mL 1.13mL |
22.55mL 4.51mL 2.26mL |
|
| CAS号 | 2387505-78-2 |
| 分子式 | C25H28Cl2N2O |
| 分子量 | 443.41 |
| SMILES Code | O=C(C1=CC=C(C=C1)Cl)N[C@@H]2[C@H](CCCC2)N[C@H](C)C3=C4C=CC=CC4=CC=C3.[H]Cl |
| MDL No. | MFCD22580412 |
| 别名 | Calhex 231 hydrochloride |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, store in freezer, under -20°C |
| 溶解方案 |
DMSO: 35 mg/mL(78.93 mM),配合低频超声助溶,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 以下溶解方案都请先按照体外实验的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
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