849479-74-9
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- CAS号:
- 849479-74-9
- 英文名:
- VAPREOTIDE ACETATE
- 英文别名:
- 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;Vapreotide Acetate(acetate)
- 中文名:
- 849479-74-9
- 中文别名:
- RC-160 ACETATE; BMY-41606 ACETATE
- CBNumber:
- CB71265964
- 分子式:
- C59H74N12O11S2
- 分子量:
- 1191.43
- MOL File:
- 849479-74-9.mol
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849479-74-9化学性质
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熔点:
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176-180°C
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储存条件:
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Hygroscopic, Refrigerator, under inert atmosphere
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溶解度:
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Acetic Acid (Slightly), Methanol (Slightly)
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形态:
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Solid
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颜色:
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White to Off-White
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稳定性:
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Hygroscopic
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849479-74-9性质、用途与生产工艺
Vapreotide acetate (RC-160 acetate; BMY-41606 acetate) 是 神经激肽-1 (NK1) 受体拮抗剂，其 IC50 值为 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.
849479-74-9
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下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-P0061A | 849479-74-9
Vapreotide acetate | 849479-74-9 | 5mg | 800元 |
| 2024/04/30 | HY-P0061A | 849479-74-9
Vapreotide acetate | 849479-74-9 | 10mg | 1300元 |
849479-74-9, 849479-74-9 相关搜索:
- 生化试剂
- 多肽
- 多肽中间体
- RC-160 ACETATE; BMY-41606 ACETATE
- 849479-74-9
- Vapreotide acetate,Vapreotide,BMY-41606,BMY41606,NK receptor,Tachykinin receptor,RC 160,BMY 41606,RC160,Inhibitor,RC-160,inhibit,Neurokinin Receptor
- Vapreotide Acetate(acetate)
- RC-160 ACETATE; BMY-41606 ACETATE; RC160 ACETATE; BMY41606 ACETATE; RC 160 ACETATE; BMY 41606 ACETATE
- RC-160 acetate
- RC160 acetate
- RC 160 acetate
- BMY-41606 acetate
- BMY41606 acetate
- BMY 41606 acetate
- Vapreotide acetate (1:x)
- Vapreotide (RC160) acetate
- VAPREOTIDE ACETATE