1. GPCR/G Protein Neuronal Signaling
  2. Somatostatin Receptor
  3. 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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  • 参考文献


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]


0.025 nM (Ki)


4.8 nM (IC50)

(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.





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sst2 Receptor agonist-1 相关分类

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.


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