4,5-DIHYDRO-N-[4-[[4-(1-METHYLETHOXY)PHENYL]METHYL]PHENYL]-1H-IMIDAZOL-2-AMINE
4,5-DIHYDRO-N-[4-[[4-(1-METHYLETHOXY)PHENYL]METHYL]PHENYL]-1H-IMIDAZOL-2-AMINE
CAS: 221529-58-4
Molecular Formula: C19H23N3O
4,5-DIHYDRO-N-[4-[[4-(1-METHYLETHOXY)PHENYL]METHYL]PHENYL]-1H-IMIDAZOL-2-AMINE - Names and Identifiers
4,5-DIHYDRO-N-[4-[[4-(1-METHYLETHOXY)PHENYL]METHYL]PHENYL]-1H-IMIDAZOL-2-AMINE - Physico-chemical Properties
| Molecular Formula | C19H23N3O |
| Molar Mass | 309.41 |
| Density | 1.13±0.1 g/cm3(Predicted) |
| Boling Point | 449.7±47.0 °C(Predicted) |
| pKa | 9.94±0.33(Predicted) |
| Storage Condition | under inert gas (nitrogen or Argon) at 2–8 °C |
| In vitro study | RO1138452 is IP receptor antagonist. The pIC 50 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 (pK i ) 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 imidazoline 2 (I 2 ) (8.3) and platelet activating factor (PAF) (7.9) receptors. 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. |
| In vivo study | 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). |
4,5-DIHYDRO-N-[4-[[4-(1-METHYLETHOXY)PHENYL]METHYL]PHENYL]-1H-IMIDAZOL-2-AMINE - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.232 ml | 16.16 ml | 32.32 ml |
| 5 mM | 0.646 ml | 3.232 ml | 6.464 ml |
| 10 mM | 0.323 ml | 1.616 ml | 3.232 ml |
| 5 mM | 0.065 ml | 0.323 ml | 0.646 ml |
Last Update：2024-01-02 23:10:35
4,5-DIHYDRO-N-[4-[[4-(1-METHYLETHOXY)PHENYL]METHYL]PHENYL]-1H-IMIDAZOL-2-AMINE - Reference Information
| biological activity | RO1138452 is an effective selective prostacyclin IP (prostacyclin) receptor antagonist. RO1138452 have high affinity for IP receptors. In human platelets, the pKi value is 9.3±0.1; in the recombinant IP receptor system, the pKi value is 8.7±0.06. |
| target | TargetValue PGI2 (in human platelets) 9.3(pKi) PGI2 (in a recombinant IP receptor system) 8.7(pKi) |
| Target | Value |
| PGI2 (in human platelets) | 9.3(pKi) |
| PGI2 (in a recombinant IP receptor system) | 8.7(pKi) |
| in vitro study | RO1138452 is IP receptor antagonist. The pIC 50 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 stable expressing the human IP receptor. The antagonist affinity (pK I) of RO1138452 is 9.0±0.06. Selectivity profiles for RO1138452 are determined via a panel of receptor binding and enzyme RO1138452 displays affinity at imidazoline 2 (I 2 ) (8.3) and platelet activating factor (PAF) (7.9) receptors. 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. |
| in vivo study | 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 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). |
Last Update：2024-04-10 22:29:15
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4,5-DIHYDRO-N-[4-[[4-(1-METHYLETHOXY)PHENYL]METHYL]PHENYL]-1H-IMIDAZOL-2-AMINE
ethyl 4-(4-chlorophenyl)-1-phenyl-4,5-dihydro-1',3'-dioxospiro[1H-pyrazole-5,2'-indane]-3-carboxylate
4-HYDROXYPSORALEN
4-(4-氯-3,5-二甲基-吡唑-1-基甲基)-苯甲酸甲酯
4-氨基-4-四羧水基噻喃
3-亚甲基环丁烷羧酸甲酯
(3,4-二氯苄基)磷酸二乙酯
二乙胺基镓
S-(-)-4-PHENYL-3-PROPIONYL-2-OXAZOLIDINONE
protostemonine
ethyl 4-(4-chlorophenyl)-1-phenyl-4,5-dihydro-1',3'-dioxospiro[1H-pyrazole-5,2'-indane]-3-carboxylate
4-HYDROXYPSORALEN
4-(4-氯-3,5-二甲基-吡唑-1-基甲基)-苯甲酸甲酯
4-氨基-4-四羧水基噻喃
3-亚甲基环丁烷羧酸甲酯
(3,4-二氯苄基)磷酸二乙酯
二乙胺基镓
S-(-)-4-PHENYL-3-PROPIONYL-2-OXAZOLIDINONE
protostemonine