Bioactivity | Calindol hydrochloride is a positive allosteric modulator (PAM) of calcimimetic calcium-sensing receptor (CaSR) with an EC50 of 132 nM[1]. |
Invitro | 在 2mM Ca2+ 存在的情况下,Calindol 刺激磷脂酰肌醇 (PI) 在表达大鼠或人 CaSR 的细胞中的 EC50 分别为 1.0 μM 或 0.31 μM[2]。在线肌造影研究中,Calindol (1-10 µM) 抑制 Methoxamine 和 KCl 诱导的预收缩张力,并抑制兔肠系膜动脉中的全细胞电压门控 Ca2+ 通道 (VGCC) 电流[3]。 |
Name | Calindol hydrochloride |
CAS | 729610-18-8 |
Formula | C21H21ClN2 |
Molar Mass | 336.86 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [1]. Lionel Kiefer, et al. Design and synthesis of calindol derivatives as potent and selective calcium sensing receptor agonists. Bioorg Med Chem. 2016 Feb 15;24(4):554-69. [2]. Albane Kessler, et al. N2-benzyl-N1-(1-(1-naphthyl)ethyl)-3-phenylpropane-1,2-diamines and conformationally restrained indole analogues: development of calindol as a new calcimimetic acting at the calcium sensing receptor. Bioorg Med Chem Lett. 2004 Jun 21;14(12):3345-9. [3]. Harry Z E Greenberg, et al. The calcilytics Calhex-231 and NPS 2143 and the calcimimetic Calindol reduce vascular reactivity via inhibition of voltage-gated Ca2+ channels. Eur J Pharmacol. 2016 Nov 15;791:659-668. |