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Olodanrigan
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Catalog No. T4431Cas No. 1316755-16-4
Alias PD-126055, EMA401
Olodanrigan (EMA401), a highly selective AT2R antagonist, inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons. EMA401 blocks p38, p42/p44 mitogen-activated protein kinase (MAPK) activation, neurite outgrowth in adult rat DRG neurons, and sensitization of adult rat and human DRG neurons induced by AngII. It inhibits capsaicin responses in cultured hDRG neurons.
Olodanrigan
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Purity: 98.33%
Catalog No. T4431Alias PD-126055, EMA401Cas No. 1316755-16-4
Olodanrigan (EMA401), a highly selective AT2R antagonist, inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons. EMA401 blocks p38, p42/p44 mitogen-activated protein kinase (MAPK) activation, neurite outgrowth in adult rat DRG neurons, and sensitization of adult rat and human DRG neurons induced by AngII. It inhibits capsaicin responses in cultured hDRG neurons.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $35 | In Stock | In Stock | |
| 10 mg | $54 | In Stock | In Stock | |
| 25 mg | $108 | In Stock | In Stock | |
| 50 mg | $177 | In Stock | In Stock | |
| 100 mg | $263 | In Stock | In Stock | |
| 200 mg | $393 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $40 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:98.33%
Appearance:Solid
Color:White
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Product Introduction
Olodanrigan AI Summary
Olodanrigan exhibits a high binding affinity for the angiotensin II type 2 (AT2) receptor with an IC50 of 0.58 nM, showcasing exceptional selectivity over the angiotensin II type 1 (AT1) receptor with a selectivity ratio greater than 1,000,000. In contrast, its inhibitory activity against the AT1 receptor is very low, with an IC50 value greater than 10,000 nM. Additionally, Olodanrigan shows differential binding affinities with a Ki value of 39.5 nM for the type 2 receptor and 409.0 nM for the type 1 receptor. Beyond its angiotensin receptor interactions, Olodanrigan exhibits 17.36% inhibition of SARS-CoV-2 3CL-Pro protease at a concentration of 20µM and demonstrated minor inhibition of SARS-CoV-2 induced cytotoxicity in VERO-6 cells at 10µM concentration. It also has a high efflux ratio of 32.0 in human Caco-2 cells, suggesting potential transport issues, with a short half-life of 0.55 hours in cryopreserved human hepatocytes. The compound shows varying effects on cell growth, inhibiting U2OS cell growth while promoting the growth of human fibroblasts and HEK293T cells. Thermal shift assays reveal that Olodanrigan generally decreases protein stability across different domains, indicating complex interactions with protein structures. Additionally, it has diverse activities in GPCR beta-arrestin recruitment assays, suggesting a multi-target bioactivity profile..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Olodanrigan (EMA401), a highly selective AT2R antagonist, inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons. EMA401 blocks p38, p42/p44 mitogen-activated protein kinase (MAPK) activation, neurite outgrowth in adult rat DRG neurons, and sensitization of adult rat and human DRG neurons induced by AngII. It inhibits capsaicin responses in cultured hDRG neurons. |
| Synonyms | PD-126055, EMA401 |
| Molecular Weight | 507.58 |
| Formula | C32H29NO5 |
| Cas No. | 1316755-16-4 |
| Smiles | COc1ccc2CN([C@@H](Cc2c1OCc1ccccc1)C(O)=O)C(=O)C(c1ccccc1)c1ccccc1 |
| Relative Density. | 1.256 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (98.51 mM), Sonication is recommended.  | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Corn Oil: 5 mg/mL (9.85 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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