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首页-小分子抑制剂&激动剂-GPCR-Calcium-sensing Receptor (CaSR)-Evocalcet
Evocalcet

Chemical Structure : Evocalcet

CAS No.: 870964-67-3

Evocalcet (KHK7580, KHK-7580, MT-4580)

货号: PC-21722Not For Human Use, Lab Use Only.

Evocalcet (MT-4580/KHK7580) is a calcimimetic agent and next-generation, oral allosteric CaSR agonist with EC50 of 93 nM (human CaSR).

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25 mg ¥1280 In stock
50 mg ¥1980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Evocalcet (MT-4580/KHK7580) is a calcimimetic agent and next-generation, oral allosteric CaSR agonist with EC50 of 93 nM (human CaSR).
Evocalcet (MT-4580/KHK7580) exhibits strong inhibition of rat PTH production with IC50 of 30.8 nM.
Oral administration of Evocalcet (MT-4580/KHK7580) efficiently suppressed the secretion of parathyroid hormone (PTH) in rat model of CKD induced by 5/6 nephrectomy.
CYP2D6 inhibition observed in cinacalcet is completely solved in evocalcet.

物理化学性质&存储条件

分子量 374.48
分子式 C24H26N2O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(4-((S)-3-(((R)-1-(Naphthalen-1-yl)ethyl)amino)pyrrolidin-1-yl)phenyl)acetic acid

参考文献

1. Kawata T, et al. PLoS One. 2018 Apr 3;13(4):e0195316.

2. Miyazaki H, et al. Bioorg Med Chem Lett. 2018 Jun 15;28(11):2055-2060.

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