sst2 Receptor agonist-1 是一种有效的生长抑素 2 型受体 (sst2) 激动剂，Ki为 0.025 nM，cAMPIC50为 4.8 nM。sst2 Receptor agonist-1 可抑制大鼠生长激素 (GH) 分泌和眼部新生血管病变的形成。具有抗血管形成作用。
| 生物活性 | sst2 Receptor agonist-1 is a potentsomatostatin receptorsubtype 2 (sst2)agonist with aKivalue of 0.025 nM and a cAMPIC50value of 4.8 nM. sst2 Receptor agonist-1 can inhibit rat growth hormone (GH) secretion and ocular neovascular lesion formation. Antiangiogenic effect[1]. |
| IC50& Target[1] | SSTR2 0.025 nM (Ki) | SSTR2 4.8 nM (IC50) |
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体内研究
(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].
| species | dog (IV 0.125 mg/kg) | rat (IV 2 mg/kg or 5 mg/kg) | | CLplasma(mL/min/kg) | 7.1 | 52 | | t1/2(h) | 11 | 2.9 | | VdSS(L/kg) | 5.7 | 9.4 | | F (%) | ND | 17 |
| 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
