| 中文名 | 奥曲肽 |
| 英文名 | Octreotide |
| 别名 | 奥曲肽 醋酸奥曲酞 奥曲肽杂质4 奥曲肽乙酸盐 奥曲肽-多肽原料委托生产 奥曲肽-多肽制剂一致性评价 (4R,7S,10S,13R,16S,19R)-13-((1H-吲哚-3-基)甲基)-19-((R)-2-氨基-3-苯基丙酰胺基)-10-(4-氨基丁基)-16-苄基-N-((2R,3R)-1,3-二羟基丁-2-基)-7-((R)-1-羟乙基)-6,9,12,15,18-五氧代 -1,2-二硫杂-5,8,11,14,17-五氮杂环二十烷-4-羧酰胺 X乙酸盐 |
| 英文别名 | CCRIS 8708 OCTREOTIDE Octreotide SMS 201-995 SMS-201-995 SANDOSTATIN Sandostatin UNII-75R0U2568I Sandostatin LAR (preservative free) Sandostatin LAR Depot OCTREOTIDE (SMS 201-995), ACETATE cyclic(2-7)-disulfide,(r-l-threonyl-n-(2-hydroxy-1-(hydroxymethyl)propyl) Octreotide(D-Phe5,Cys6·11,D-Trp8,L-Threoninol12)-SoMatostatin-14 (5-12), SMS-201-995 D-Phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-L-threonyl-N-[(1R,2R)-2-hydroxy-1-(hydroxyMethyl)propyl]- D-Phenylalanyl-L-hemicystyl-L-phenylalanyl-D-tryptophyl-L-lysyl-L-threonyl-L-hemicystyl-L-threoninol cyclic (2-7)-disulfide acetate (salt) D-Phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-L-threonyl-N-((1R,2R)-2-hydroxy-1-(hydroxymethyl)propyl)-L-cysteinamide cyclic (2-7)-disulfide acetate (salt) L-Cysteinamide, D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-L-threonyl-N-(2-hydroxy-1-(hydroxymethyl)propyl)-, cyclic(2-7)-disulfide, (R-(R*,R*))-, acetate (salt) L-Cysteinamide, D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-L-threonyl-N-(2-hydroxy-1-(hydroxymethyl)propyl)-, cyclic (2-7)-disulfide, (R-(R*,R*))-, acetate (salt) (4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-16-benzyl-7-[(1R)-1-hydroxyethyl]-N-[(1R,2R)-2-hydroxy-1-(hydroxymethyl)propyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-19-(D-phenylalanylamino)-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carboxamide acetate (salt) |
| CAS | 79517-01-4 |
| EINECS | 616-695-4 |
| 化学式 | C51H70N10O12S2 |
| 分子量 | 1079.3 |
| InChI | InChI=1/C49H66N10O10S2/c1-28(61)39(25-60)56-48(68)41-27-71-70-26-40(57-43(63)34(51)21-30-13-5-3-6-14-30)47(67)54-37(22-31-15-7-4-8-16-31)45(65)55-38(23-32-24-52-35-18-10-9-17-33(32)35)46(66)53-36(19-11-12-20-50)44(64)59-42(29(2)62)49(69)58-41/h3-10,13-18,24,28-29,34,36-42,52,60-62H,11-12,19-23,25-27,50-51H2,1-2H3,(H,53,66)(H,54,67)(H,55,65)(H,56,68)(H,57,63)(H,58,69)(H,59,64)/t28-,29?,34-,36+,37+,38-,39-,40+,41+,42+/m1/s1 |
| InChIKey | XQEJFZYLWPSJOV-XJQYZYIXSA-N |
| 熔点 | 153-156°C |
| 沸点 | 1447.2°C at 760 mmHg |
| 比旋光度 | D20 -42° (c = 0.5 in 95% acetic acid) |
| 闪点 | 829.1°C |
| 蒸汽压 | 0mmHg at 25°C |
| 溶解度 | H2O: soluble |
| 存储条件 | Inert atmosphere,Store in freezer, under -20°C |
| 体内研究 | 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. Octreotide-PPSG appears to inhibit the expression of SSTR2 and SSTR5 to a greater extent than that of Octreotide-soln treated group. A test dose of octreotide acetate significantly decreases the serum gastrin level to approximately one third of the baseline in 2 hr and the effect lasted approximately for 6 hr. On day 21, treatment with sustained-release formulation of octreotide acetatea (5 mg intramuscular, q 4 wk) is initiated. |