产品说明书

Tecalcet HCl

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Chemical Structure| 177172-49-5 同义名 : R-568 hydrochloride;KRN 568;Tecalcet;NPS R-568;R-568;Tecalcet Hydrochloride
CAS号 : 177172-49-5
货号 : A413858
分子式 : C18H23Cl2NO
纯度 : 99%+
分子量 : 340.287
MDL号 : MFCD16038895
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(146.93 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

动物实验配方:
生物活性
描述 Tecalcet HCl, also known as R 568 HCl, is an orally active calcimimetic compound that allosterically upregulates the calcium-sensing receptor (CaSR). Tecalcet HCl enhances the sensitivity to extracellular Ca2+ activation[1][2][3]. Tecalcet HCl increases intracellular calcium concentration ([Ca2+]i) in a concentration-dependent and stereoselective manner within the range of 0.1-100 μM. It shifts the concentration-response curve for extracellular Ca2+ to the left without affecting the maximum response, thereby reducing the EC50 value for extracellular Ca2+ to 0.61±0.04 mM[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.94mL

0.59mL

0.29mL

14.69mL

2.94mL

1.47mL

29.39mL

5.88mL

2.94mL

参考文献

[1]Wada, M., et al. The calcimimetic compound NPS R-568 suppresses parathyroid cell proliferation in rats with renal insufficiency. Control of parathyroid cell growth via a calcium receptor. Journal of Clinical Investigation 100(12), 2977-2983 (1997).

[2]Nemeth, E.F., et al. The parathyroid calcium receptor: a novel therapeutic target for treating hyperparathyroidism. Pediatr.Nephrol. 10(3), 275-279 (1996).

[3]Nemeth, E.F., et al. Calcimimetics with potent and selective activity on the parathyroid calcium receptor. Proceedings of the National Academy of Sciences of the United States of America 95(7), 4040-4045 (1998).