Octreotide acetate

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Chemical Structure| 79517-01-4 同义名 : SMS 201-995 acetate
CAS号 : 79517-01-4
货号 : A589099
分子式 : C51H70N10O12S2
纯度 : 99%
分子量 : 1079.29
MDL号 : MFCD00871400
存储条件:

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 250 mg/mL(231.63 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 25 mg/mL(23.16 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 Octreotide acetate, a long-acting synthetic analog of native somatostatin, inhibits growth hormone, glucagon, and insulin more potently. Octreotide-treated groups show a significant reduction in the tumor volume when compared with saline group. Octreotide-PPSG (1.4 mg/kg, i.p.) shows greater antitumor effect than Octreotide-soln (100 μg/kg, i.p.). Octreotide-treatments results in significant inhibitory effect on the expression levels of SSTR2 and SSTR5 in primary HCC-bearing rats compared with the saline group[3]. Octreotide can decrease the rate of postoperative complication after pancreatic resection by diminishing exocrine function of the pancreas. Prophylactic octreotide is not effective to inhibit the exocrine secretion of the remnant pancreas and does not decrease the incidence of pancreatic fistula after pancreaticoduodenectomy[4]. The prophylactic use of LAO (long-acting octreotide acetate) did not prevent the incidence or reduce the severity of diarrhea and had no notable impact on patient-reported bowel function or QoL(quality of life)[5]. Octreotide LAR (octreotide acetate) 20 mg shows significant efficacy in terms of objective response rate (PR + SD), biochemical and symptomatic control in patients with metastatic NETs (neuroendocrine tumors) of the GEP system pretreated and progressing on slow release lanreotide[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00274170 Migraine Headache Phase 1 Phase 2 Unknown - United States, Texas ... 展开 >> CR Darnall Army Medical Center Recruiting Ft. Hood, Texas, United States, 76544 收起 <<
NCT00616551 Acromegaly Phase 3 Completed - Belarus ... 展开 >> Republican Centre for Medical Rehabilitation and Water-therapy Minsk, Belarus Hungary Semmelweis Egyetem Általános Orvostudományi Budapest, Hungary Romania Institute of Endocrinology "C. I. Parhon" Bucharest Bucharest, Romania Serbia Institute of Endocrinology, University Clinical Center Belgrade, Serbia Slovakia Fakultná Nemocnica s Poliklinkou Bratislava Bratislava, Slovakia Ukraine V.P. Komisarenko Institute of Endocrinology and Metabolism, AMS Ukraine Kiev, Ukraine 收起 <<
NCT00003057 Colorectal Cancer ... 展开 >> Diarrhea 收起 << Phase 3 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.93mL

0.19mL

0.09mL

4.63mL

0.93mL

0.46mL

9.27mL

1.85mL

0.93mL

参考文献

[1]Wang M, Shan F, et al. Pharmacokinetic and pharmacodynamic study of a phospholipid-based phase separation gel for once a month administration of octreotide. J Control Release. 2016 May 28;230:45-56.

[2]Kim S, Hosoya K, et al. Treatment of Gastrin-Secreting Tumor With Sustained-Release Octreotide Acetate in a Dog. J Am Anim Hosp Assoc. 2015 Nov-Dec;51(6):407-12.

[3]Wang M, Shan F, Zou Y, Sun X, Zhang ZR, Fu Y, Gong T. Pharmacokinetic and pharmacodynamic study of a phospholipid-based phase separation gel for once a month administration of octreotide. J Control Release. 2016 May 28;230:45-56

[4]You DD, Paik KY, Park IY, Yoo YK. Randomized controlled study of the effect of octreotide on pancreatic exocrine secretion and pancreatic fistula after pancreatoduodenectomy. Asian J Surg. 2019 Feb;42(2):458-463

[5]Zachariah B, Gwede CK, James J, Ajani J, Chin LJ, Donath D, Rosenthal SA, Kane BL, Rotman M, Berk L, Kachnic LA. Octreotide acetate in prevention of chemoradiation-induced diarrhea in anorectal cancer: randomized RTOG trial 0315. J Natl Cancer Inst. 2010 Apr 21;102(8):547-56

[6]Ricci S, Antonuzzo A, Galli L, Ferdeghini M, Bodei L, Orlandini C, Conte PF. Octreotide acetate long-acting release in patients with metastatic neuroendocrine tumors pretreated with lanreotide. Ann Oncol. 2000 Sep;11(9):1127-30