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MedChemExpress - Model Octreotide pamoate -135467-16-2

Octreotide (SMS 201-995) pamoate is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide pamoate can bind to the somatostatin receptors which are mainly subtypes 2, 3 and 5. Octreotide pamoate increases Gi activity and reduces intracellular cAMP production. Octreotide pamoate has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly[1][2].

Octreotide pamoate

MCE China：Octreotide pamoate

Brand：MedChemExpress (MCE)

Cat. No.HY-P0036B

CAS：135467-16-2

Synonyms：SMS 201-995 pamoate

Storage：Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Octreotide (SMS 201-995) pamoate is a somatostatin receptor agonist and synthetic octapeptide endogenous somatostatin analogue. Octreotide pamoate can bind to the somatostatin receptors which are mainly subtypes 2, 3 and 5. Octreotide pamoate increases Gi activity and reduces intracellular cAMP production. Octreotide pamoate has antitumor activity, mediates apoptosis and may also be used in disease studies in acromegaly.

In Vitro：Octreotide pamoate (10?8mM, 6 hours) induces phosphorylated?glycogen synthase kinase 3β (GSK3β) phosphorylation and increases glycogen synthase (GS) activity[3].

In Vivo：Octreotide pamoate (subcutaneous injection, 30 mg/kg, once) can inhibit tumor growth significantly with no effect on body weight[1]. Octreotide pamoate (intramuscular injection, 60 mg/kg, every 21 days, 42 days) inhibits serum insulin-like growth factor (IGF-I) without toxicity in dogs with appendicular osteosarcoma (OSA)[2]. Octreotide pamoate (subcutaneous injection, 40 μg/kg, Every 12 hours, 8 days) improves hepatic glycogen synthesis in obese male Sprague?Dawley (SD) rats[3].

IC50 & Target：SSTR2 SSTR3 SSTR5

Sequence：{d-Phe}-Cys-Phe-{d-Trp}-Lys-Thr-Cys-{d-Threoninol} (Disulfide bridge: Cys2-Cys7)

References：

[1]. G. Weckbecker，et al. Indirect antiproliferative effect of the somatostatin analog octreotide on MIA PaCa-2 human pancreatic carcinoma in nude mice. Yale J Biol Med. 1997 Sep-Dec;70(5-6):549-54.

[2]. Chand Khanna，et al. A randomized controlled trial of octreotide pamoate long-acting release and carboplatin versus carboplatin alone in dogs with naturally occurring osteosarcoma: evaluation of insulin-like growth factor suppression and chemotherapy. Clin Cancer Res. 2002 Jul;8(7):2406-12 [Content Brief]

[3]. Xiao-Xia Wang,et al. Effects of octreotide on hepatic glycogenesis in rats with high fat diet‑induced obesity. Mol Med Rep. 2017 Jul;16(1):109-118. [Content Brief]

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MedChemExpress - Model Octreotide pamoate -135467-16-2

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Octreotide pamoate