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Merck
CN

SML0132

醋酸兰瑞肽

≥98% (HPLC), SRIF-1 sst2 subtype of somatostatin receptor agonist, powder

别名:

3-(2-萘基)-D-丙氨酰基-L-半胱氨酰基-L-酪氨酸-D-色氨酸-L-赖氨酰基-L-戊酰基-L-半胱氨酰-L-苏氨酸酰胺环状(2→7)-乙酸二硫, BIM-23014C, 醋酸血管肽素

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关于此项目

经验公式（希尔记法）:
C54H69N11O10S2 · xC2H4O2
化学文摘社编号:
127984-74-1
分子量:
1096.32 (free base basis)
UNSPSC Code:
12352200
PubChem Substance ID:
329825182
NACRES:
NA.25

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产品名称

醋酸兰瑞肽, ≥98% (HPLC)

form

powder

SMILES string

CC(O)=O.CC(C)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](CSSC[C@H](NC1=O)C(=O)N[C@@H]([C@@H](C)O)C(N)=O)NC(=O)[C@H](N)Cc5ccc6ccccc6c5

InChI

1S/C54H69N11O10S2.C2H4O2/c1-29(2)45-54(75)63-44(53(74)65-46(30(3)66)47(57)68)28-77-76-27-43(62-48(69)38(56)23-32-15-18-33-10-4-5-11-34(33)22-32)52(73)60-41(24-31-16-19-36(67)20-17-31)50(71)61-42(25-35-26-58-39-13-7-6-12-37(35)39)51(72)59-40(49(70)64-45)14-8-9-21-55;1-2(3)4/h4-7,10-13,15-20,22,26,29-30,38,40-46,58,66-67H,8-9,14,21,23-25,27-28,55-56H2,1-3H3,(H2,57,68)(H,59,72)(H,60,73)(H,61,71)(H,62,69)(H,63,75)(H,64,70)(H,65,74);1H3,(H,3,4)/t30-,38-,40+,41+,42-,43+,44?,45+,46+;/m1./s1

InChI key

DEXPIBGCLCPUHE-HPDHVNDUSA-N

assay

≥98% (HPLC)

color

white to off-white

shipped in

wet ice

storage temp.

−20°C

Quality Level

100

相关类别

Application

乙酸兰瑞肽已被用作抑制剂，以测试野生型小鼠中生长激素/甲状腺激素信号转导对硫化氢调节的可变性。

Biochem/physiol Actions

八肽生长抑素类似物；sst2生长抑素受体激动剂；抗肿瘤
醋酸兰瑞肽是一种生长抑素类似物，是生长抑素受体SRIF-1 sst2亚型的选择性激动剂，对sst2的结合亲和力为0.8 nM，对sst5的结合亲和力为5.2 nM，对sst3的结合亲和力为100 nM，对于SRIF-2亚型sst1和sst4受体的结合亲和力为1000 nM以上。它在临床上可用于肢端肥大症和神经内分泌肿瘤所引起的症状的治疗，并且在最近的研究中还可以用于抑制肿瘤的生长，并显示出对非内分泌肿瘤的活性。

pictograms

Health hazard
GHS08

signalword

Warning

hcodes

H361

pcodes

P281

Hazard Classifications

Repr. 2

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

涉药品监管产品
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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000482799
0000482779
0000482799
0000482779
0000424559

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The Journal of clinical endocrinology and metabolism, 99(4), 1282-1290 (2014-01-16)
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Maxime Palazzo et al.
European journal of gastroenterology & hepatology, 25(2), 232-238 (2012-10-31)
An antiproliferative effect of somatostatin analogs was recently demonstrated. To identify factors associated with tumor control in a group of patients with well-differentiated malignant digestive neuroendocrine tumors treated with lanreotide. A retrospective study was conducted in 68 patients treated with
Shaun Coughlin et al.
World journal of surgery, 36(5), 1016-1029 (2012-03-16)
Enterocutaneous fistulas are abnormal connections between the skin and gastrointestinal tract that most commonly occur after surgery. Somatostatin analogues have been used in their treatment. The objective of the present study was to determine if somatostatin analogues shorten the time
Ivan Borbath et al.
Acta gastro-enterologica Belgica, 75(2), 270-273 (2012-08-09)
We describe the case of a 54 years old woman, with hepatitis B, in whom the diagnosis of a 6 cm hepatocellular carcinoma (HCC) in the left liver was made in 2001. Alpha-foeto-protein (AFP) was 63 ng/mL (NI < 10
Nan Zheng et al.
Molecular pharmaceutics, 9(5), 1175-1188 (2012-03-23)
Many tumor cells specifically overexpress somatostatin receptors, in particular, subtype 2 (SSTR2). Lanreotide, a somatostatin analogue with high affinity for SSTR2, can be exploited as a ligand for tumor targeted therapy. In this study, lanreotide was first conjugated to poly(ethylene
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