AZD5462
Based on 1 publication(s) in Google Scholar
AZD5462 is a RXFP1 modulator, can be used for heart failure research. RXFP1 is the cognate receptor for human relaxin, belongs to GPCR family 1c number with anti-fibrotic and anti-inflammatory properties.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.89%
- No. CAS: 2787501-83-9
- Fòrmula: C30H41FN2O6
- Peso molecular:544.65
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) AZD5462
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Actividad biológica
RXFP1[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
>250 μM
Compound: 6; AZD5462
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Cytotoxicity against human HepG2 cells assessed as cell viability by Glu/Gal assay
Cytotoxicity against human HepG2 cells assessed as cell viability by Glu/Gal assay
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[PMID: 38502782] |
| HepG2 | IC50 |
>250 μM
Compound: 6; AZD5462
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Cytotoxicity against human HepG2 cells assessed as spheroid formation by C3a spheroid assay
Cytotoxicity against human HepG2 cells assessed as spheroid formation by C3a spheroid assay
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[PMID: 38502782] |
| THP-1 | IC50 |
>250 μM
Compound: 6; AZD5462
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Cytotoxicity against human THP-1 cells assessed as cell viability incubated for 48 hrs by resazurin assay
Cytotoxicity against human THP-1 cells assessed as cell viability incubated for 48 hrs by resazurin assay
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[PMID: 38502782] |
AZD5462 (example 1) shows stimulatory activity on cAMP or cGMP production with EC50s of 17 nM and 50 nM, respectively[1].
AZD5462 binds human plasma protein with fraction unbound (free) rate of 4.3%, and shows the stability with Clint values of 23 μL/min/mg (human licer microsomal), 4.8 μL/min/106 cells (human hepatocyte), and 11 μL/min/106 cells (rat hepatocyte)[1].
AZD5462 enhances phosphorylation of ERK with an EC50 value of 6.3 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2787501-83-9
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Appearance Solid
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Peso molecular 544.65
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Fòrmula C30H41FN2O6
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Color White to off-white
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SMILES
C[C@]1(C(O)=O)CC[C@@H](OC2=C(F)C=C(OC)C(C(N[C@@H]3[C@H](C4)CC[C@H]4[C@@H]3C(NCC5(CCC5)C)=O)=O)=C2)CC1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Biomed Chromatogr
Liquid Chromatography Combined With Electrospray Ionization Tandem Mass Spectrometry for the Determination and Identification of AZD5462 and Its Metabolites in Rat Plasma. [Abstract]2025 Jun;39(6):e70095. PMID: 40277352
Solvente y solubilidad
DMSO : 100 mg/mL (183.60 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (4.59 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 (4.59 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 (275 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
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8360 mL | 9.1802 mL | 18.3604 mL | 45.9010 mL |
| 5 mM | 0.3672 mL | 1.8360 mL | 3.6721 mL | 9.1802 mL | |
| 10 mM | 0.1836 mL | 0.9180 mL | 1.8360 mL | 4.5901 mL | |
| 15 mM | 0.1224 mL | 0.6120 mL | 1.2240 mL | 3.0601 mL | |
| 20 mM | 0.0918 mL | 0.4590 mL | 0.9180 mL | 2.2951 mL | |
| 25 mM | 0.0734 mL | 0.3672 mL | 0.7344 mL | 1.8360 mL | |
| 30 mM | 0.0612 mL | 0.3060 mL | 0.6120 mL | 1.5300 mL | |
| 40 mM | 0.0459 mL | 0.2295 mL | 0.4590 mL | 1.1475 mL | |
| 50 mM | 0.0367 mL | 0.1836 mL | 0.3672 mL | 0.9180 mL | |
| 60 mM | 0.0306 mL | 0.1530 mL | 0.3060 mL | 0.7650 mL | |
| 80 mM | 0.0230 mL | 0.1148 mL | 0.2295 mL | 0.5738 mL | |
| 100 mM | 0.0184 mL | 0.0918 mL | 0.1836 mL | 0.4590 mL |
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