Evocalcet
Based on 3 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.28%
- No. CAS: 870964-67-3
- Fòrmula: C24H26N2O2
- Peso molecular:374.48
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Evocalcet
More
Actividad biológica
CaSR[1]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague Dawley chronic kidney disease (CKD) rats with adenine induced secondary hyperparathyroidism (SHPT)[1]
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Dosage:0.03 and 0.3 mg/kg
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Administration:Oral Administration; 0.03 and 0.3 mg/kg, once
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Result:Decreased the serum PTH and Ca levels at a dose of 0.3 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 870964-67-3
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Appearance Solid
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Peso molecular 374.48
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Fòrmula C24H26N2O2
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Color White to off-white
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SMILES
O=C(O)CC1=CC=C(N2C[C@@H](N[C@@H](C3=C4C=CC=CC4=CC=C3)C)CC2)C=C1
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Synonyms
KHK7580
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Nature
2021 Jul;595(7867):455-459 PMID: 34194040 -
Biochem Pharmacol
Detailed functional characterization of four nanobodies as positive allosteric modulators of the human calcium-sensing receptor. [Abstract]2024 Nov 8:116619. PMID: 39522703 -
J Clin Endocrinol Metab
Heterogenous Origins of Calcium Homeostasis Disorders Arising from Five Heterozygous Calcium-Sensing Receptor Variants. [Abstract]2024 Oct 16:dgae735. PMID: 39413244
Solvente y solubilidad
DMSO : 50 mg/mL (133.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
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 | |
| 100 mM | 0.0267 mL | 0.1335 mL | 0.2670 mL | 0.6676 mL |
Evocalcet Related Classifications
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