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RO1138452
🥰Excellent
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
🥰Excellent
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 | Availability | Quantity |
|---|---|---|---|
| 1 mg | $44 | In Stock | |
| 2 mg | $63 | In Stock | |
| 5 mg | $97 | In Stock | |
| 10 mg | $155 | In Stock | |
| 25 mg | $347 | In Stock | |
| 50 mg | $597 | In Stock | |
| 100 mg | $852 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $97 | In Stock |
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Purity:99.34%
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Product Introduction
Bioactivity
Chemical Properties
| 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 | α1B-adrenoceptor (rat):5.87 (pKi), Muscarinic M1 receptor (human):5.66 (pKi), Muscarinic M2 receptor (human):5.88 (pKi), α1B-adrenoceptor (rat):3280 nM, Muscarinic M5 receptor (human):3110 nM, 5-HT1A receptor (human):8580 nM, Muscarinic M4 receptor (human):6.14 (pKi), 5-HT1A receptor (human):5.37 (pKi), I2R (rat):8.33 (pKi), 5-HT2A receptor (rat):3040 nM, 5-HT2C (porcine):6.11 (pKi), α2A-adrenoceptor (human):6.49 (pKi), α2A-adrenoceptor (human):724 nM, Muscarinic M5 receptor (human):5.81 (pKi), 5-HT1B receptor (rat):1130 nM, 5-HT2A receptor (rat):5.71 (pKi), I2R (rat):7 nM, PAF Receptor (rabbit):7.9 (pKi), 5-HT2C (porcine):1190 nM, 5-HT4 receptor (guinea pig):8910 nM, Muscarinic M2 receptor (human):2220 nM, 5-HT1B receptor (rat):6.11 (pKi), 5-HT4 receptor (guinea pig):5.35 (pKi), Muscarinic M1 receptor (human):2570 nM, PAF Receptor (rabbit):52.9 nM, Muscarinic M4 receptor (human):1450 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) |
| Color | White |
| Appearance | Solid |
Storage & Solubility Information
| 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.  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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