RO1138452

RO1138452 is a potent and selective IP (prostacyclin) receptor antagonist. RO1138452 displays high affinity for IP receptors. In human platelets, pKi is 9.3±0.1; in a recombinant IP receptor system, pKi is 8.7±0.06.

Product Specifications

CAS Number

[221529-58-4]

Product Name Alternative

CAY10441

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Prostaglandin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Endocrinology

Assay Protocol

https://www.medchemexpress.com/RO1138452.html

Purity

99.26

Solubility

DMSO : 100 mg/mL (ultrasonic) |Ethanol : 50 mg/mL (ultrasonic)

Smiles

CC(C)OC1=CC=C(CC2=CC=C(NC3=NCCN3)C=C2)C=C1

Molecular Formula

C19H23N3O

Molecular Weight

309.41

Precautions

H302, H315, H319, H335

References & Citations

[1]Bley KR, et al. RO1138452 and RO3244794: characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists. Br J Pharmacol. 2006 Feb;147 (3) :335-45.|[2]Ayer LM, et al. 4,5-Dihydro-1H-imidazol-2-yl) -[4- (4-isopropoxy-benzyl) -phenyl]-amine (RO1138452) is a selective, pseudo-irreversible orthosteric antagonist at the prostacyclin (IP) -receptor expressed by human airway epithelial cells: IP-receptor-mediated inhibition of CXCL9 and CXCL10 release. J Pharmacol Exp Ther. 2008 Feb;324 (2) :815-26.