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RO1138452
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Catalog No. T4436Cas No. 221529-58-4
Alias CAY10441
RO1138452 (CAY10441) is a selective and orally bioavailable antagonist of prostacyclin receptor (pKi: 8.3). It antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cyclic AMP accumulation in a dose-dependent manner. Likewise, it inhibits the binding of tritiated iloprost to rodent neuroblastoma cells with a Ki of about 1.5 nM. At levels between 2-20 mg/kg in rats, CAY10441 shows significant analgesic activity in standard antinociceptive assays [1].
RO1138452
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Purity: 99.34%
Catalog No. T4436Alias CAY10441Cas No. 221529-58-4
RO1138452 (CAY10441) is a selective and orally bioavailable antagonist of prostacyclin receptor (pKi: 8.3). It antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cyclic AMP accumulation in a dose-dependent manner. Likewise, it inhibits the binding of tritiated iloprost to rodent neuroblastoma cells with a Ki of about 1.5 nM. At levels between 2-20 mg/kg in rats, CAY10441 shows significant analgesic activity in standard antinociceptive assays [1].
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $44 | In Stock | In Stock | |
| 2 mg | $63 | In Stock | In Stock | |
| 5 mg | $97 | In Stock | In Stock | |
| 10 mg | $155 | In Stock | In Stock | |
| 25 mg | $347 | In Stock | In Stock | |
| 50 mg | $597 | In Stock | In Stock | |
| 100 mg | $852 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $97 | 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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Purity:99.34%
Appearance:Solid
Color:White to Yellow
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | RO1138452 (CAY10441) is a selective and orally bioavailable antagonist of prostacyclin receptor (pKi: 8.3). It antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cyclic AMP accumulation in a dose-dependent manner. Likewise, it inhibits the binding of tritiated iloprost to rodent neuroblastoma cells with a Ki of about 1.5 nM. At levels between 2-20 mg/kg in rats, CAY10441 shows significant analgesic activity in standard antinociceptive assays [1]. |
| Targets&IC50 | 5-HT2A receptor (rat):5.71 (pKi), 5-HT2A receptor (rat):3040 nM, 5-HT1B receptor (rat):6.11 (pKi), 5-HT1B receptor (rat):1130 nM, 5-HT2C (porcine):6.11 (pKi), 5-HT2C (porcine):1190 nM, PAF Receptor (rabbit):52.9 nM, PAF Receptor (rabbit):7.9 (pKi), I2R (rat):8.33 (pKi), I2R (rat):7 nM, Muscarinic M1 receptor (human):2570 nM, Muscarinic M1 receptor (human):5.66 (pKi), Muscarinic M4 receptor (human):1450 nM, Muscarinic M4 receptor (human):6.14 (pKi), α1B-adrenoceptor (rat):5.87 (pKi), α1B-adrenoceptor (rat):3280 nM, 5-HT1A receptor (human):5.37 (pKi), 5-HT1A receptor (human):8580 nM, Muscarinic M2 receptor (human):2220 nM, Muscarinic M2 receptor (human):5.88 (pKi), α2A-adrenoceptor (human):6.49 (pKi), α2A-adrenoceptor (human):724 nM, 5-HT4 receptor (guinea pig):5.35 (pKi), 5-HT4 receptor (guinea pig):8910 nM, Muscarinic M5 receptor (human):5.81 (pKi), Muscarinic M5 receptor (human):3110 nM |
| Synonyms | CAY10441 |
| Molecular Weight | 309.41 |
| Formula | C19H23N3O |
| Cas No. | 221529-58-4 |
| Smiles | CC(C)Oc1ccc(Cc2ccc(NC3=NCCN3)cc2)cc1 |
| Relative Density. | 1.13 g/cm3 (Predicted) |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 45 mg/mL (145.44 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.46 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 | ||||||||||||||||||||||||||||||||||||
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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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