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Submit ReviewRo 1138452 hydrochloride is a 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.
Ro 1138452 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
References are publications that support the biological activity of the product.
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, Ro 1138452 hydrochloride supplier, Ro1138452, hydrochloride, supplier, IP, receptors, antagonists, prostanoid, prostaglandins, prostacyclins, eicosanoids, analgesic, CAS, 221529-58-4, Prostanoid, Receptors, 4268, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Ro 1138452 hydrochloride include:
Maria Dulce et al (2022) Vascular Effects of Polyphenols from Agrimonia eupatoria L. and Role of Isoquercitrin in Its Vasorelaxant Potential in Human Arteries. Pharmaceuticals (Basel) 15 PMID: 35631463
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