Product Name :
RO1138452
Description:
RO1138452 is a selective antagonist of prostacyclin (IP) receptor with pKi of 9.3 0.1 in human platelets.
CAS:
221529-58-4
Molecular Weight:
309.41
Formula:
C19H23N3O
Chemical Name:
N-(4-(4-isopropoxybenzyl)phenyl)-4,5-dihydro-1H-imidazol-2-amine4,5-Dihydro-N-(4-((4-(1-methylethoxy)phenyl)methyl)phenyl)-1H-imadazol-2-amine
Smiles :
CC(C)OC1C=CC(CC2C=CC(=CC=2)NC2NCCN=2)=CC=1
InChiKey:
GYYRMJMXXLJZAB-UHFFFAOYSA-N
InChi :
InChI=1S/C19H23N3O/c1-14(2)23-18-9-5-16(6-10-18)13-15-3-7-17(8-4-15)22-19-20-11-12-21-19/h3-10,14H,11-13H2,1-2H3,(H2,20,21,22)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.{{Ingenol Mebutate} site|{Ingenol Mebutate} TGF-beta/Smad|{Ingenol Mebutate} Purity & Documentation|{Ingenol Mebutate} In Vitro|{Ingenol Mebutate} manufacturer|{Ingenol Mebutate} Epigenetic Reader Domain}
Additional information:
RO1138452 is a selective antagonist of prostacyclin (IP) receptor with pKi of 9.3 0.1 in human platelets.|Product information|CAS Number: 221529-58-4|Molecular Weight: 309.41|Formula: C19H23N3O|Synonym:|CAY10441|Chemical Name: N-(4-(4-isopropoxybenzyl)phenyl)-4,5-dihydro-1H-imidazol-2-amine4,5-Dihydro-N-(4-((4-(1-methylethoxy)phenyl)methyl)phenyl)-1H-imadazol-2-amine|Smiles: CC(C)OC1C=CC(CC2C=CC(=CC=2)NC2NCCN=2)=CC=1|InChiKey: GYYRMJMXXLJZAB-UHFFFAOYSA-N|InChi: InChI=1S/C19H23N3O/c1-14(2)23-18-9-5-16(6-10-18)13-15-3-7-17(8-4-15)22-19-20-11-12-21-19/h3-10,14H,11-13H2,1-2H3,(H2,20,21,22)|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 33.33 mg/mL (107.72 mM; Need ultrasonic) Ethanol : 25 mg/mL (80.80 mM; Need ultrasonic) H2O : Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.{{Thiamine} web|{Thiamine} Endogenous Metabolite|{Thiamine} Technical Information|{Thiamine} Description|{Thiamine} manufacturer|{Thiamine} Autophagy} |Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|RO1138452 is IP receptor antagonist.PMID:23695992 The pIC50 values of RO1138452 in attenuating cAMP accumulation is 7.0±0.07. Functional antagonism of RO1138452 is studied by measuring inhibition of carbaprostacyclin-induced cAMP accumulation in CHO-K1 cells stably expressing the human IP receptor. The antagonist affinity (pKi) of RO1138452 is 9.0±0.06. Selectivity profiles for RO1138452 are determined via a panel of receptor binding and enzyme assays. RO1138452 displays affinity at imidazoline2 (I2) (8.3) and platelet activating factor (PAF) (7.9) receptors[1]. RO1138452 (10 pM-10 μM) added to cells concurrently with a fixed concentration of Taprostene (1 μM) prevents, in a concentration-dependent manner, the inhibition of CXCL9 and CXCL10 release, with p[A]50 (molar) values of -8.73±0.11 and -8.47±0.16 (p>0.05), respectively[2].|In Vivo:|RO1138452 is a potent and selective antagonist for both human and rat IP receptors and that is possesses analgesic and anti-inflammatory potential. RO1138452 (1-10 mg/kg, i.v.) significantly reduces acetic acid-induced abdominal constrictions. RO1138452 (3-100 mg/kg, p.o.) significantly reduces carrageenan-induced mechanical hyperalgesia and edema formation. One hour after administration of RO1138452 (5 mg/kg, i.v.) to rats, the total plasma concentration is 0.189 μg/mL, whereas the free plasma concentrations is calculated to be 0.009 μg/mL (28 nM)[1].|References:|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.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.Products are for research use only. Not for human use.|
