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849479-74-9

849479-74-9

中文名稱849479-74-9
中文同義詞RC-160 ACETATE; BMY-41606 ACETATE;(4R,7S,10S,13R,16S,19R)-13-((1H-吲哚-3-基)甲基)-N-((S)-1-氨基-3-(1H-茚-3-基)-1-氧代丙-2-基)-19-((R)-2-氨基-3-苯基丙酰胺基)-10-(4-氨基丁基)-16-(4-羥基芐基)-7-異丙基-6,9,12,15,18-五氧代-1,2-二噻-5,8,11,14,17-五氮雜環(huán)二十烷-4-甲酰胺 x乙酸鹽;rno-miR-146b-3p mimicrno-miR-146b-3p 模擬物;rno-miR-146b-3p mimicrno-miR-146b-3p 模擬物;伐普利肽醋酸鹽
英文名稱VAPREOTIDE ACETATE
英文同義詞VAPREOTIDE ACETATE;Vapreotide (RC160) acetate;Vapreotide acetate (1:x);BMY 41606 acetate;BMY41606 acetate;BMY-41606 acetate;RC 160 acetate;RC160 acetate
CAS號849479-74-9
分子式C59H74N12O11S2
分子量1191.43
EINECS號
相關(guān)類別多肽中間體
Mol文件849479-74-9.mol
結(jié)構(gòu)式849479-74-9 結(jié)構(gòu)式

849479-74-9 性質(zhì)

熔點176-180°C
儲存條件Hygroscopic, Refrigerator, under inert atmosphere
溶解度可溶于醋酸(少許)、甲醇(少許)
形態(tài)固體
顏色白色至類白色
序列{d-Phe}-Cys-Tyr-{d-Trp}-Lys-Val-Cys-Trp-NH2 (Disulfide bridge: Cys2-Cys7)
穩(wěn)定性吸濕性

849479-74-9 用途與合成方法

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。

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).

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.

安全信息

MSDS信息

更新日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2026/06/05HY-P0061A849479-74-9
Vapreotide acetate
849479-74-95mg800元
2026/06/05HY-P0061A849479-74-9
Vapreotide acetate
849479-74-910mg1300元

849479-74-9 上下游產(chǎn)品信息

"849479-74-9"相關(guān)產(chǎn)品信息
[ARG8]-VASOTOCINACETATESALT 加壓素 精氨縮宮素 GLY-LEU-SER-LYS-GLY-CYS-PHE-GLY-LEU-LYS-LEU-ASP-ARG-ILE-GLY-SER-MET-SER-GLY-LEU-GLY-CYS-ASN-SER-PHE-ARG-TYR ArginineVasopressin-d5 CYS-GLU-ASP-ALA-GLU-VAL-PHE-LYS-ASP-SER-MET-VAL-PRO-GLY-GLU-LYS VasonatrinPeptide(VNP) 加壓素 伐普肽
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