Octreotide-acetate-SMS-201-995-acetate-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEOctreotide acetateCat. No.: HY-17365CAS No.: 79517-01-4Synonyms: SMS 201-995 (acetate)分式: CHNOS分量: 1079.29作靶点: Somatostatin Receptor作通路: GPCR/G Protein; Neuronal Signaling储存式: 4C, protect from light* In solvent : -80C, 6 months;

2、 -20C, 1 month (protect fromlight)溶解性数据体外实验 DMSO : 29 mg/mL (26.87 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 0.9265 mL 4.6327 mL 9.2654 mL5 mM 0.1853 mL 0.9265 mL 1.8531 mL10 mM 0.0927 mL 0.4633 mL 0.9265 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和

3、期限。BIOLOGICAL ACTIVITY物活性 Octreotide acetate长效的天然长抑素合成类似物， 长抑素更有效的长激素，胰糖素和胰岛素的抑制剂。体内研究Octreotide-treated groups show a significant reduction in the tumor volume when compared with salinegroup. Octreotide-PPSG (1.4 mg/kg, i.p.) shows greater antitumor effect than Octreotide-soln (100 g/kg,i.p.). Octr

4、eotide-treatments results in significant inhibitory effect on the expression levels of SSTR2 and1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESSTR5 in primary HCC-bearing rats compared with the saline group. Octreotide-PPSG appears to inhibit theexpression of SSTR2 and SSTR5 to a greater extent t

5、han that of Octreotide-soln treated group 1. A testdose of octreotide acetate significantly decreases the serum gastrin level to approximately one third of thebaseline in 2 hr and the effect lasted approximately for 6 hr. On day 21, treatment with sustained-releaseformulation of octreotide acetatea

6、(5 mg intramuscular, q 4 wk) is initiated 2.PROTOCOLAnimal Mice 1Administration 1 Thirty mice with HCC xenografts are randomLy divided into three groups: (A) Octreotide-soln group, (B)Octreotide-PPSG group, and (C) control group. Octreotide-soln group receives i.p. injection of 100 g/kgoctreotide-so

7、ln once a day and totally for consecutive 14 days. Octreotide-PPSG group receives a singlesubcutaneous injection of 1.4 mg/kg Octreotide-PPSG, and the injection volume is about 0.2 mL. Controlgroup receives i.p. injection of saline once a day for consecutive 14 days. Treatment starts on the next day

8、after injection of H22 hepatoma cell suspension and maintains for 14 days. Tumor growth is monitored byperiodic caliper measurements on day 7 and day 14 post seeding. Tumor volumes (V) are calculated basedon the length and width of tumor by Eq.Rats 1Twelve male SD rats are divided into two groups, a

9、nd housed in standard cages at 25C, with free access tofood and water for a week prior to the experiment. Rats are subcutaneously injected with Octreotidereotidesolution (Octreotide-soln) or Octreotide-PPSG at an equivalent single dose of 20 mg/kg. The dose isdetermined based on the clinical dose of

10、 Octreotide-soln in human. Rats are fasted for 12 h before dosingand food is returned approximately 2 h post dosing. Blood samples are collected at predetermined timepoints using heparinized Eppendorf tubes. Immediately after collection, the blood samples are placed on iceuntil centrifuged at 3000 g

11、 for 10 min within 1 h. The plasma is collected and stored at 20C until analysis.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Faculty of Biological and Environmental Sciences. University of Helsinki Finland. 2018 Dec.See more customer val

12、idations on HYPERLINK / www.MedChemEREFERENCES1. Wang M, et al. Pharmacokinetic and pharmacodynamic study of a phospholipid-based phase separation gel for once a monthadministration of octreotide. J Control Release. 2016 May 28;230:45-56.2. Kim S, et al. Treatment of Gastrin-Secreting Tumor With Sustained-Release Octreotide Acetate in a Dog. J Am Anim Hosp Assoc. 2015Nov-Dec;51(6):407-12.McePdfHeightCauti