2. GPCR/G Protein Neuronal Signaling
  3. Somatostatin Receptor
  4. sst2 Receptor agonist-1

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，cAMP IC50 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。

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sst2 Receptor agonist-1 Chemical Structure

sst2 Receptor agonist-1 Chemical Structure

CAS No. : 1021912-42-4

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sst2 Receptor agonist-1 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target[1]

SSTR2

0.025 nM (Ki)

SSTR2

4.8 nM (IC50)

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
分子量

432.94

Formula

C26H25ClN2O2
CAS 号
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.
纯度 & 产品资料
参考文献

sst2 Receptor agonist-1 相关分类

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Keywords:

sst2 Receptor agonist-11021912-42-4Somatostatin ReceptorSSTRsSSTRgrowth hormoneocularneovascularlesionantiangiogenicWistar ratsBrown Norway ratsInhibitorinhibitorinhibit

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