Evocalcet_product_DataBase

Bioactivity

Evocalcet (KHK7580) is an orally active calcium sensing receptor (CaSR) agonist. Evocalcet inhibits the secretion of parathyroid hormone (PTH) from parathyroid gland cells. Evocalcet can be used for the research of hyperparathyroidism[1][2].

Target

CaSR

Invitro

Evocalcet (0，20 和 60 nM) 剂量依赖性地增加了 [Ca2+]i, EC50 值为 92.7 nM 在 hCaR-HEK293 细胞中[2]。Evocalcet 对任何 (细胞色素 P450) CYP 同工酶的特异性活性均无显著抑制作用[2]。

In Vivo

Evocalcet (0.03 或 0.3 mg/kg；口服给药，一次) 影响血清甲状旁腺激素和钙水平[1]。Evocalcet (0.3 mg/kg；口服，每天一次，持续 5 周) 降低血清甲状旁腺激素和钙水平，增加血清中的无机磷[1]。 Animal Model:

Name

Evocalcet

CAS

870964-67-3

Formula

C24H26N2O2

Molar Mass

374.48

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Sakai M, et al. Evocalcet prevents ectopic calcification and parathyroid hyperplasia in rats with secondary hyperparathyroidism. PLoS One. 2020 Apr 28;15(4):e0232428. [2]. Kawata T, et al. A novel calcimimetic agent, evocalcet (MT-4580/KHK7580), suppresses the parathyroid cell function with little effect on the gastrointestinal tract or CYP isozymes in vivo and in vitro. PLoS One. 2018 Apr 3;13(4):e0195316.

PeptideDB

Evocalcet

CAS: 870964-67-3 F: C24H26N2O2 W: 374.48