产品
编 号：F011371
分子式：C26H25ClN2O2
分子量：432.94
分子式：C26H25ClN2O2
分子量：432.94
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CAS No: 1021912-42-4
产品详情
生物活性：
sst2 Receptor agonist-1 is a potent somatostatin receptor subtype 2 (sst2) agonist with a Ki value of 0.025 nM and a cAMP IC50 value of 4.8 nM. sst2 Receptor agonist-1 can?inhibit rat growth hormone (GH) secretion and ocular neovascular lesion formation. Antiangiogenic effect.
体内研究：
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.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.Pharmacokinetic Parameters of sst2 Receptor agonist-1 (compound 21) in dogs and rats.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)
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)
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.
sst2 Receptor agonist-1 is a potent somatostatin receptor subtype 2 (sst2) agonist with a Ki value of 0.025 nM and a cAMP IC50 value of 4.8 nM. sst2 Receptor agonist-1 can?inhibit rat growth hormone (GH) secretion and ocular neovascular lesion formation. Antiangiogenic effect.
体内研究：
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.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.Pharmacokinetic Parameters of sst2 Receptor agonist-1 (compound 21) in dogs and rats.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)
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)
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.
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