sst2 Receptor agonist-1
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.
For research use only. We do not sell to patients.
- CAS No.: 1021912-42-4
- Formula: C26H25ClN2O2
- Molecular Weight:432.94
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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SSTR2 0.025 nM (Ki) |
SSTR2 4.8 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
4.8 nM
Compound: 21
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Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
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[PMID: 21395312] |
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 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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]
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Dosage:0.2 or 2 mg/kg
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Administration:IV; single dosage
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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).
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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]
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Dosage:5 or 15 μg/per eye, 5 μL
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Administration:Intraocular administration; inject at day 0, 4 and 8
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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.
Chemical Information
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CAS No. 1021912-42-4
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Molecular Weight 432.94
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Formula C26H25ClN2O2
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SMILES
ClC1=CC2=NC=C(C(OCCCN)=C2C=C1C3=CC=CC(O)=C3)C4=CC(C)=CC(C)=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
sst2 Receptor agonist-1 Related Classifications
HY-110161 Related Classifications
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