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四肽胃泌素

四肽胃泌素用途

四胃泌素(胆囊收缩素四肽；CCK-4)是胃泌素的C端四肽。四胃泌素能刺激胃分泌[1]。四胃泌素是一种胆囊收缩素(CCK-4)受体激动剂[2]。胃粘膜保护[3]。

四肽胃泌素名称

[ CAS 号 ]:
1947-37-1

[ 中文名 ]:
四肽胃泌素

[ 英文名 ]:
CCK-4

[英文别名 ]:

Cholecystokinin Fragment 30-33 Amide
cholecystokinin-4
H-Trp-Met-Asp-Phe-NH2
cholecystokinin tetrapeptide
Cholecystokinin fragment 30-33 amide
Cholecystokinin C-terminal tetrapeptide

四肽胃泌素生物活性

[ 描述 ]:

四胃泌素(胆囊收缩素四肽；CCK-4)是胃泌素的C端四肽。四胃泌素能刺激胃分泌[1]。四胃泌素是一种胆囊收缩素(CCK-4)受体激动剂[2]。胃粘膜保护[3]。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 胆囊收缩素受体

研究领域 >> 代谢疾病

[体外研究]

组胺H2受体拮抗剂西咪替丁在体外抑制组胺的刺激作用,并激活四胃泌素对腺苷酸环化酶活性的刺激。四胃泌素和组胺通过不同受体激活大鼠胃粘膜腺苷酸环化酶[4]。

[体内研究]

在用N-甲基-N'-硝基-N-亚硝基胍治疗的近交系Wistar大鼠中,四胃泌素(s.c.；1 mg/kg；每隔一天)治疗可显著降低腺癌的发病率和数量,并显著降低胃窦粘膜的标记指数[1]。四胃泌素具有增强大鼠胃粘膜表面粘液分泌和/或粘液合成相关的胃粘膜保护作用。粘液凝胶和表面粘膜层的粘蛋白含量显著增加。因此,由于施用四胃泌素,粘液凝胶和表面粘膜中的粘液蛋白会增加[3]。动物模型：7周龄雄性Wistar大鼠,每只体重约160 g[3]剂量：12、120或400μg/kg给药：皮下注射(皮下注射)；其次是50%乙醇诱导的胃损伤结果：导致胃体粘膜粘蛋白含量显著增加,并以剂量依赖性方式预防50%乙醇诱导的胃粘膜损伤。

[参考文献]

[1]. M Tatsuta, et al. Effect of 6-hydroxydopamine on gastric carcinogenesis and tetragastrin inhibition of gastric carcinogenesis induced by N-methyl-N'-nitro-N-nitrosoguanidine in Wistar rats. Cancer Res. 1989 Aug 1;49(15):4199-203.

[2]. Nathalie Lara, et al. Pulmonary and systemic nitric oxide measurements during CCK-5-induced panic attacks. Neuropsychopharmacology. 2003 Oct;28(10):1840-5.

[3]. Y Komuro,et al. Effects of tetragastrin on mucus glycoprotein in rat gastric mucosal protection. Gastroenterol Jpn. 1992 Oct;27(5):597-603.

[4]. A A Karelin,et al. Tetragastrin activation of rat gastric mucosa adenyl cyclase in vitro. Biull Eksp Biol Med. 1981 Apr;91(4):440-1.

四肽胃泌素物理化学性质

[ 密度 ]:
1.341g/cm3

[ 沸点 ]:
1159.2ºC at 760mmHg

[ 分子式 ]:
C₂₉H₃₆N₆O₆S

[ 分子量 ]:
596.70

[ 闪点 ]:
654.8ºC

[ 精确质量 ]:
730.27800

[ PSA ]:
247.11000

[ LogP ]:
4.67950

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
0mmHg at 25°C

[ 折射率 ]:
1.643

[ 储存条件 ]:
-20°C，密封，干燥

四肽胃泌素MSDS

详细MSDS(安全技术说明书)

四肽胃泌素毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: SQ7310000

CHEMICAL NAME :: L-Phenylalaninamide, N-((phenylmethoxy)carbonyl)-L-tryptophyl-L-methionyl- L-aspartyl-

CAS REGISTRY NUMBER :: 1947-37-1

LAST UPDATED :: 199806

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C37-H42-N6-O8-S

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2 gm/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: -,816,1995

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >1 gm/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: -,816,1995

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >2 gm/kg

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 3,121,1969

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >2 gm/kg

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 3,121,1969

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >1 gm/kg

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 3,121,1969

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >100 mg/kg

TOXIC EFFECTS :: Behavioral - excitement Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 3,121,1969

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >5 gm/kg

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 3,121,1969 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 46800 mg/kg/26W-I

TOXIC EFFECTS :: Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 3,121,1969

四肽胃泌素安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

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

四肽胃泌素文献

Overexpression of the Promigratory and Prometastatic PTK7 Receptor Is Associated with an Adverse Clinical Outcome in Colorectal Cancer.

PLoS ONE 10 , e0123768, (2015)

Biomarkers and novel therapeutic targets are urgently needed in colorectal cancer (CRC). The pseudo tyrosine kinase receptor 7 (PTK7) is involved in planar cell polarity and it is deregulated in vario...

CI-988 Inhibits EGFR Transactivation and Proliferation Caused by Addition of CCK/Gastrin to Lung Cancer Cells.

J. Mol. Neurosci. 56 , 663-72, (2015)

Cholecystokinin (CCK) receptors are G-protein coupled receptors (GPCR) which are present on lung cancer cells. CCK-8 stimulates the proliferation of lung cancer cells, whereas the CCK2R receptor antag...

Synthesis, characterization and in vitro evaluation of new oxorhenium- and oxotechnetium-CCK4 derivatives as molecular imaging agents for CCK2-receptor targeting.

Eur. J. Med. Chem. 45(2) , 423-9, (2010)

The goal of this study is to design new (99m)Tc-radiolabelled shortened CCK derivatives that might be suitable for the molecular imaging of cholecystokinin-2 receptors (CCK2-R), these receptors being ...

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