Biological Activity
Selective prostacyclin IP receptor antagonist (pKi = 8.3). Exhibits no affinity at other prostanoid receptors (EP1-4, FP and TP) in a radioligand binding assay. Demonstrates analgesic activity in rats. Orally bioavailable.
Compound Libraries
Ro 1138452 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 345.87 |
| Formula | C19H23N3O.HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| PubChem ID | 91826074 |
| InChI Key | OYPSAMWVIBGRMV-UHFFFAOYSA-N |
| Smiles | CC(C)OC1=CC=C(CC2=CC=C(NC3=NCCN3)C=C2)C=C1.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 34.59 | 100 | |
| water | 34.59 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 345.87. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.89 mL | 14.46 mL | 28.91 mL |
| 5 mM | 0.58 mL | 2.89 mL | 5.78 mL |
| 10 mM | 0.29 mL | 1.45 mL | 2.89 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.58 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Clark et al (2004) Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists. Bioorg.Med.Chem.Lett. 14 1053 PMID: 15013022
Jones et al (2006) Investigation of the prostacyclin (IP) receptor antagonist RO1138452 on isolated blood vessel and platelet preparations. Br.J.Pharmacol. 149 110 PMID: 16880763
Bley et al (2006) RO1138452 and RO3244794: characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists. Br.J.Pharmacol. 147 335 PMID: 16331286
Keywords: Ro 1138452 hydrochloride, supplier, Ro1138452, hydrochloride, supplier, IP, receptors, antagonists, prostanoid, prostaglandins, prostacyclins, eicosanoids, analgesic, CAS, 221529-58-4, Prostanoid, Receptors, Prostanoid, Receptors, Tocris Bioscience
