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849479-74-9

中文名稱 849479-74-9
CAS 849479-74-9
分子式 C57H68N12O9S2
分子量 1129.35
MOL 文件 849479-74-9.mol
更新日期 2024/11/03 16:22:41
849479-74-9 結(jié)構(gòu)式 849479-74-9 結(jié)構(gòu)式

基本信息

英文別名
RC160 acetate
RC-160 acetate
RC 160 acetate
BMY41606 acetate
BMY 41606 acetate
BMY-41606 acetate
VAPREOTIDE ACETATE
Vapreotide acetate (1:x)
Vapreotide (RC160) acetate
RC-160 ACETATE
BMY-41606 ACETATE
RC160 ACETATE
BMY41606 ACETATE
RC 160 ACETATE
BMY 41606 ACETATE
849479-74-9價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/08/19HY-P0061A849479-74-9
Vapreotide acetate
849479-74-95mg800元
2024/08/19HY-P0061A849479-74-9
Vapreotide acetate
849479-74-910mg1300元
2024/08/19HY-P0061A849479-74-9
Vapreotide acetate
849479-74-925mg2500元

常見問題列表

生物活性
Vapreotide acetate (RC-160 acetate; BMY-41606 acetate) 是 神經(jīng)激肽-1 (NK1) 受體拮抗劑,其 IC50 值為 330 nM。
體外研究

Vapreotide attenuates the Substance P (SP)-triggered intracellular calcium increases and NF-κB activation in a dose-dependent manner. Vapreotide also inhibits SP-induced IL-8 and MCP-1 production in HEK293-NK1R and U373MG cell lines. Vapreotide inhibits HIV-1 infection of human MDM in vitro , an effect that is reversible by SP pretreatment. Vapreotide significantly inhibits GH-, PRL, and/or alpha-subunit release by human GH-secreting pituitary adenoma cells in concentrations as low as 10 -12 -10 -14 M. Vapreotide inhibits GH release with an IC 50 of 0.1 pM. Vapreotide exhibits moderate-to-high affinities for SSTR2, -3, and -5 (IC 50 =0.17, 0.1 and 21 nM, respectively) and low affinity for SSTR1 and -4 (IC 50 =200 and 620 nM, respectively). RC-160 inhibits serum-induced proliferation of CHO cells expressing SSTR2 and SSTR5 (EC 50 =53 and 150 pM, respectively).

體內(nèi)研究

In cirrhosis, bleeding by rupture of oesophagogastric varices is a severe complication of portal hypertension. The acute administration of vapreotide to rats decreases collateral circulation blood flow while chronic administration attenuated its development. Tumor volumes and weights are reduced by about 40% by RC-160 by s.c. injections at doses of 100 μg/day/animal. Vapreotide can inhibit the growth of androgen-independent prostate cancer when the therapy is started at an early stage of tumor development.

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