奥曲肽

奥曲肽用途

Octreotide acetate是长效的天然生长抑素合成类似物,是比生长抑素更有效的生长激素,胰高血糖素和胰岛素的抑制剂。

奥曲肽作用

体外活性：与盐水组相比，奥曲肽治疗组显示肿瘤体积显着减少。奥曲肽-PPSG（1.4mg / kg，腹膜内）显示出比奥曲肽溶液（100μg/ kg，腹膜内注射）更强的抗肿瘤效果。与盐水组相比，奥曲肽处理对携带原代HCC的大鼠中SSTR2和SSTR5的表达水平具有显着的抑制作用。奥曲肽-PPSG似乎比奥曲肽 - 溶液治疗组更能抑制SSTR2和SSTR5的表达。醋酸奥曲肽的测试剂量在2小时内将血清胃泌素水平显着降低至基线的约三分之一，并且效果持续约6小时。在第21天，开始用缓释制剂醋酸奥曲肽（5mg肌肉注射，q 4周）治疗。

奥曲肽名称

[ CAS 号 ]:
79517-01-4

[ 中文名 ]:
奥曲肽

[ 英文名 ]:
Octreotide acetate salt

[英文别名 ]:

Sandostatin (TN)
Octreotide acetate (USAN)
Octreotide (acetate)
Octreotide
Octreotide Acetate
SMS 201-995
Sandostatin LAR
Sandostatin
zacycloicosane-4-carboxamide acetate

奥曲肽生物活性

[ 描述 ]:

Octreotide acetate是长效的天然生长抑素合成类似物,是比生长抑素更有效的生长激素,胰高血糖素和胰岛素的抑制剂。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 生长抑素受体

多肽产品

研究领域 >> 心血管疾病

研究领域 >> 炎症/免疫

多肽产品

[体内研究]

与盐水组相比,奥曲肽治疗组显示肿瘤体积显着减少。奥曲肽-PPSG(1.4mg/kg,ip)显示出比奥曲肽溶液(100μg/ kg,ip)更强的抗肿瘤效果。与盐水组相比,奥曲肽处理对携带原代HCC的大鼠中SSTR2和SSTR5的表达水平具有显着的抑制作用。与Octreotide-soln治疗组相比,奥曲肽-PPSG似乎更能抑制SSTR2和SSTR5的表达[1]。醋酸奥曲肽的测试剂量在2小时内将血清胃泌素水平显着降低至基线的约三分之一,并且效果持续约6小时。在第21天,开始用缓释制剂醋酸奥曲肽(5mg肌内,q 4周)治疗[2]。

[动物实验]

小鼠[1]将30只HCC异种移植物小鼠随机分成三组：（A）奥曲肽 - 溶质组，（B）奥曲肽 - PPSG组和（C）对照组。奥曲肽 - 溶质组每天一次腹膜内注射100μg/ kg奥曲肽 - 溶液，连续14天。奥曲肽-PPSG组单次皮下注射1.4 mg / kg奥曲肽-PPSG，注射量约为0.2 mL。对照组每天一次腹腔注射盐水，连续14天。在注射H22肝细胞瘤细胞悬液后第二天开始治疗并维持14天。通过在接种后第7天和第14天的定期测径器测量来监测肿瘤生长。肿瘤体积（V）基于肿瘤的长度和宽度通过等式计算。大鼠[1]将12只雄性SD大鼠分成两组，并置于25℃的标准笼中，在实验前自由获取食物和水一周。给大鼠皮下注射奥曲肽 - 戊二酸溶液（奥曲肽 - 溶液）或奥曲肽 - PPSG，剂量相当于20mg / kg。剂量基于人体中奥曲肽 - soln的临床剂量确定。在给药前将大鼠禁食12小时，并在给药后约2小时返回食物。使用肝素化的Eppendorf管在预定时间点收集血液样品。收集后立即将血液样品置于冰上，直至在1小时内以3000g离心10分钟。收集血浆并储存在-20℃直至分析。

[参考文献]

[1]. Wang M, 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, 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.

[相关活性小分子]

MK-4256 | 醋酸伐普肽

奥曲肽物理化学性质

[ 密度 ]:
1.4±0.1 g/cm3

[ 沸点 ]:
1447.2±65.0 °C at 760 mmHg

[ 熔点 ]:
153-156ºC

[ 分子式 ]:
C₅₁H₇₀N₁₀O₁₂S₂

[ 分子量 ]:
1079.29

[ 闪点 ]:
829.1±34.3 °C

[ PSA ]:
382.82000

[ LogP ]:
0.77

[ 外观性状 ]:
无色至灰白色冻干的固体

[ 蒸汽压 ]:
0.0±0.3 mmHg at 25°C

[ 折射率 ]:
1.673

[ 储存条件 ]:
库房低温,通风,干燥,与食品原料分开存放

奥曲肽毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: HA1000000

CHEMICAL NAME :: L-Cysteinamide, D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophy l-L-lysyl-L-threonyl- N- (2-hydroxy-1-(hydroxymethyl)propyl)-, cyclic(2-7)-disulfide, (R-(R*,R*))-, acetate (salt)

CAS REGISTRY NUMBER :: 79517-01-4

LAST UPDATED :: 199709

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C49-H66-N10-O10-S2.2C2-H4-O2

MOLECULAR WEIGHT :: 1139.49

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 2587 ug/kg

TOXIC EFFECTS :: Gastrointestinal - changes in structure or function of endocrine pancreas Liver - liver function tests impaired

REFERENCE :: LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 348,1668,1996

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 1429 ug/kg

TOXIC EFFECTS :: Gastrointestinal - changes in structure or function of endocrine pancreas Liver - liver function tests impaired

REFERENCE :: LANCAO Lancet. (7 Adam St., London WC2N 6AD, UK) V.1- 1823- Volume(issue)/page/year: 348,1668,1996

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >50 mg/kg

TOXIC EFFECTS :: Skin and Appendages - dermatitis, allergic (after topical exposure) Skin and Appendages - hair

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 21,5151,1987

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 18100 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 22,967,1991

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >100 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - somnolence (general depressed activity) Behavioral - ataxia

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 21,5151,1987

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 72300 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 22,967,1991

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >20 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,240,1990 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 18200 ug/kg/13W-C

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes Blood - other changes Biochemical - Metabolism (Intermediary) - Plasma proteins not involving coagulation

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 21,5151,1987

奥曲肽安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

奥曲肽