2. GPCR/G Protein
  3. CaSR
  4. Evocalcet

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.

For research use only. We do not sell to patients.

Evocalcet Chemical Structure

Evocalcet Chemical Structure

CAS No. : 870964-67-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 71 In-stock
Solution
10 mM * 1 mL in DMSO USD 71 In-stock
Solid
1 mg USD 26 In-stock
5 mg USD 65 In-stock
10 mg USD 100 In-stock
50 mg USD 310 In-stock
100 mg USD 470 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Evocalcet:

Evocalcet Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Evocalcet

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

IC50 & Target

CaSR[1]
In Vitro

Evocalcet (0, 20 and 60 nM) dose-dependently increases [Ca2+]i with an EC50 value of 92.7 nM in hCaR-HEK293 cells[2].
Evocalcet shows no significant inhibitory effects on the specific activities of any (cytochrome P450) CYP isozymes[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Evocalcet Related Antibodies
In Vivo

Evocalcet (0.03 or 0.3 mg/kg; oral Administration, once) affects serum PTH and Ca levels[1].
Evocalcet (0.3 mg/kg; oral Administration, once daily, for 5 weeks) reduces the serum PTH and Ca levels and increases the serum IP (inorganic phosphorus) level[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague Dawley chronic kidney disease (CKD) rats with adenine induced secondary hyperparathyroidism (SHPT)[1]
Dosage: 0.03 and 0.3 mg/kg
Administration: Oral Administration; 0.03 and 0.3 mg/kg, once
Result: Decreased the serum PTH and Ca levels at a dose of 0.3 mg/kg.
Clinical Trial
Molecular Weight

374.48

Formula

C24H26N2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CC1=CC=C(N2C[C@@H](N[C@@H](C3=C4C=CC=CC4=CC=C3)C)CC2)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 30 mg/mL (80.11 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6704 mL 13.3518 mL 26.7037 mL
5 mM 0.5341 mL 2.6704 mL 5.3407 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.68 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.68 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6704 mL 13.3518 mL 26.7037 mL 66.7592 mL
5 mM 0.5341 mL 2.6704 mL 5.3407 mL 13.3518 mL
10 mM 0.2670 mL 1.3352 mL 2.6704 mL 6.6759 mL
15 mM 0.1780 mL 0.8901 mL 1.7802 mL 4.4506 mL
20 mM 0.1335 mL 0.6676 mL 1.3352 mL 3.3380 mL
25 mM 0.1068 mL 0.5341 mL 1.0681 mL 2.6704 mL
30 mM 0.0890 mL 0.4451 mL 0.8901 mL 2.2253 mL
40 mM 0.0668 mL 0.3338 mL 0.6676 mL 1.6690 mL
50 mM 0.0534 mL 0.2670 mL 0.5341 mL 1.3352 mL
60 mM 0.0445 mL 0.2225 mL 0.4451 mL 1.1127 mL
80 mM 0.0334 mL 0.1669 mL 0.3338 mL 0.8345 mL
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Evocalcet Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Evocalcet870964-67-3KHK7580KHK 7580KHK-7580CaSRCalcium-sensing receptorparathyroid hormonehyperparathyroidismHEK293CYPPTHCainorganic phosphorusratInhibitorinhibitorinhibit

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