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1021912-42-4

1021912-42-4 Structure

1021912-42-4 Structure
IdentificationBack Directory
[Name]

TC-G 1003
[CAS]

1021912-42-4
[Synonyms]

TC-G 1003
TCG1003,TC-G-1003
3-[4-(3-Aminopropoxy)-7-chloro-3-(3,5-dimethylphenyl)-6-quinolinyl]phenol
Phenol, 3-[4-(3-aminopropoxy)-7-chloro-3-(3,5-dimethylphenyl)-6-quinolinyl]-
[Molecular Formula]

C26H25ClN2O2
[MDL Number]

MFCD30182254
[MOL File]

1021912-42-4.mol
[Molecular Weight]

432.94
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

Soluble in DMSO
Hazard InformationBack Directory
[Uses]

TC-G 1003 is a selective somatostatin receptor subtype 2 agonist.
[in vivo]

sst2 Receptor agonist-1 (compound 21) (0.2 or 2 mg/kg; IV; single dosage) shows a dose-dependent decrease in growth hormone (GH) secretion[1].
sst2 Receptor agonist-1 (5 or 15 μg/per eye; intraocular; once every 4 days) reduces neovascular lesion area in laser choroidal neovascularization (CNV) rat model[1].
Pharmacokinetic Parameters of sst2 Receptor agonist-1 (compound 21) in dogs and rats[1].

speciesdog (IV 0.125 mg/kg)rat (IV 2 mg/kg or 5 mg/kg)
CLplasma (mL/min/kg)7.152
t1/2 (h)112.9
VdSS (L/kg)5.79.4
F (%)ND17
Animal Model:Female Wistar rats (200-250 g; IP injection with 50 mg/kg pentobarbital, then injected with tested compound via jugular cannula, after 40 or 50 min administration, injected with GH secretagogue via jugular cannula)[1]
Dosage:0.2 or 2 mg/kg
Administration:IV; single dosage
Result:Caused a dose-dependent decrease in GH secretion (38 and 91% reduction in plasma GH AUC following administration of 0.2 and 2 mg/kg, respectively).
Animal Model:Male Brown Norway rats (175-225 g; lasered and perfused, a 27G needle was used to make a small hole in the eye 3 mm posterior to iris angled 45° toward the optic nerve)[1]
Dosage:5 or 15 μg/per eye, 5 μL
Administration:Intraocular administration; inject at day 0, 4 and 8
Result:Exhibited a dose-dependent antiangiogenic effect by a 35 and 53% reduction in neovascular lesion area with 5 or 15 μg per eye, respectively.
[IC 50]

SSTR2: 0.025 nM (Ki); SSTR2: 4.8 nM (IC50)
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