Home GPCR & G Protein CaSR activator Evocalcet

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Evocalcet CaSR activator

Cat.No.E0359

Evocalcet (KHK7580) is an novel oral calcimimetic agent which acts via allosteric activation of the calcium sensing receptor (CaSR). This compound (0, 20 and 60 nM) dose-dependently increases cytoplasmic [Ca2+] concentrations with an EC50 value of 92.7 nM in hCaR-HEK293 cells.
Evocalcet CaSR activator Chemical Structure

Chemical Structure

Molecular Weight: 374.48

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: E035901 DMSO]75 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.73%
99.73

Chemical Information, Storage & Stability

Molecular Weight 374.48 Formula

C24H26N2O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 870964-67-3 -- Storage of Stock Solutions

Solubility

In vitro
Batch:

DMSO : 75 mg/mL (200.27 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
CaSR [1]
92.7 nM(EC50)
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01935856 Completed
Hyperparathyroidism
Kyowa Kirin Co. Ltd.
 August 2013 Phase 1|Phase 2

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