Description: Selective prostacyclin IP receptor antagonist
Chemical Name: 4,5-Dihydro-N-[4-[[4-(1-methylethoxy)phenyl]methyl]phenyl]-1H-imidazol-2-amine hydrochloride
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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
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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
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Clarket al (2004) Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists. Bioorg.Med.Chem.Lett. 14 1053 PMID: 15013022
Joneset al (2006) Investigation of the prostacyclin (IP) receptor antagonist RO1138452 on isolated blood vessel and platelet preparations. Br.J.Pharmacol. 149 110 PMID: 16880763
Bleyet al (2006) RO1138452 and RO3244794: characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists. Br.J.Pharmacol. 147 335 PMID: 16331286