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Merck
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主要文件

E7144

Sigma-Aldrich

毒晰外泌肽-4

≥97%

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About This Item

经验公式(希尔记法):
C184H282N50O60S
分子量:
4186.57
MDL编号:
UNSPSC代码:
51111800
NACRES:
NA.32

质量水平

方案

≥97%

储存温度

−20°C

SMILES字符串

S(CC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](N)Cc9[nH]cnc9)CCC(=O)O)[C@H](O)C)Cc8ccccc8)[C@H](O)C)CO)CC(=O)O)CC(C)C)CO)CCCCN)CCC(=O)N

InChI

1S/C184H282N50O60S/c1-16-94(10)147(178(289)213-114(52-58-144(257)258)163(274)218-121(73-101-77-195-105-39-24-23-38-103(101)105)168(279)215-116(68-90(2)3)165(276)205-107(41-26-28-61-186)158(269)219-122(75-134(189)243)154(265)198-79-135(244)196-83-139(248)231-63-30-43-129(231)175(286)225-127(87-238)174(285)223-125(85-236)155(266)200-80-136(245)202-96(12)181(292)233-65-32-45-131(233)183(294)234-66-33-46-132(234)182(293)232-64-31-44-130(232)176(287)222-124(84-235)150(190)261)229-170(281)119(71-99-34-19-17-20-35-99)217-166(277)117(69-91(4)5)214-159(270)108(42-29-62-194-184(191)192)212-177(288)146(93(8)9)228-151(262)95(11)203-156(267)111(49-55-141(251)252)208-161(272)112(50-56-142(253)254)209-162(273)113(51-57-143(255)256)210-164(275)115(59-67-295-15)211-160(271)110(47-53-133(188)242)207-157(268)106(40-25-27-60-185)206-172(283)126(86-237)224-167(278)118(70-92(6)7)216-169(280)123(76-145(259)260)220-173(284)128(88-239)226-180(291)149(98(14)241)230-171(282)120(72-100-36-21-18-22-37-100)221-179(290)148(97(13)240)227-138(247)82-199-153(264)109(48-54-140(249)250)204-137(246)81-197-152(263)104(187)74-102-78-193-89-201-102/h17-24,34-39,77-78,89-98,104,106-132,146-149,195,235-241H,16,25-33,40-76,79-88,185-187H2,1-15H3,(H2,188,242)(H2,189,243)(H2,190,261)(H,193,201)(H,196,244)(H,197,263)(H,198,265)(H,199,264)(H,200,266)(H,202,245)(H,203,267)(H,204,246)(H,205,276)(H,206,283)(H,207,268)(H,208,272)(H,209,273)(H,210,275)(H,211,271)(H,212,288)(H,213,289)(H,214,270)(H,215,279)(H,216,280)(H,217,277)(H,218,274)(H,219,269)(H,220,284)(H,221,290)(H,222,287)(H,223,285)(H,224,278)(H,225,286)(H,226,291)(H,227,247)(H,228,262)(H,229,281)(H,230,282)(H,249,250)(H,251,252)(H,253,254)(H,255,256)(H,257,258)(H,259,260)(H4,191,192,194)/t94-,95-,96-,97+,98+,104-,106-,107-,108-,109-,110-,111-,112-,113-,114-,115-,116-,117-,118-,119-,120-,121-,122-,123-,124-,125-,126-,127-,128-,129-,130-,131-,132-,146-,147-,148-,149-/m0/s1

InChI key

HTQBXNHDCUEHJF-XWLPCZSASA-N

基因信息

human ... GLP1R(2740)

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Amino Acid Sequence

His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2

一般描述

毒晰外泌肽4是一种肠促胰岛素模拟肽,由39个氨基酸组成。它是胰高血糖素样肽1(GLP-1)类似物和促胰岛素分泌剂,半衰期长。最初从学名为钝尾毒蜥(Heloderma suspectum)的吉拉毒蜥的毒液中分离得到。

应用

毒晰外泌肽4可作为肠促胰岛素模拟物用于处理HepG2细胞,以排除辅助材料的影响。它也可用作r(GLP-1R)激动剂,以排除辅助材料的干扰。
毒晰外泌肽4可用于处理ob/ob小鼠模型,以确定葡萄糖和胰岛素的浓度以及内稳态评估模型(HOMA),还可用于测定毒晰外泌肽4处理的巨噬细胞中核因子-κΒ(NF-κB)p65水平。

生化/生理作用

可激活GLP-1(胰高血糖素样肽1)受体,增加胰腺腺泡细胞的细胞内cAMP; 对VIP受体没有作用。
毒晰外泌肽4模拟哺乳动物肠促胰岛素激素胰高血糖素样肽1(GLP-1)的活性,从而起到控制葡萄糖的作用。这包括以葡萄糖依赖性方式分泌胰岛素、高胰高血糖素分泌的负调节和胃排空持续时间的增加。在2型糖尿病患者体内,当二甲双胍作用不足时,可以皮下注射这种肽控制血糖。它可促进β-细胞的新生和增殖,从而有助于胰腺的再生。它是毒晰外泌肽受体的配体,还可导致腺泡细胞cAMP水平升高。

包装

无底玻璃瓶。内含物装在插入的融合锥内。

其他说明

合成生产
从0.1%TFA水溶液中冻干

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

Eyeshields, Gloves, type N95 (US)


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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访问文档库

Junling Liu et al.
EBioMedicine, 41, 73-84 (2019-03-05)
Glucagon-like peptide-1 (GLP-1) and its based agents improve glycemic control. Although their attenuating effect on hepatic glucose output has drawn our attention for decades, the potential mechanisms remain unclear. Cytokine array kit was used to assess cytokine profiles in db/db
Ralph A DeFronzo et al.
Diabetes care, 28(5), 1092-1100 (2005-04-28)
This study evaluates the ability of the incretin mimetic exenatide (exendin-4) to improve glycemic control in patients with type 2 diabetes failing to achieve glycemic control with maximally effective metformin doses. A triple-blind, placebo-controlled, 30-week study at 82 U.S. sites
Xiaokun Ding et al.
Hepatology (Baltimore, Md.), 43(1), 173-181 (2005-12-24)
Nonalcoholic fatty liver disease (NAFLD) represents a burgeoning problem in hepatology, and is associated with insulin resistance. Exendin-4 is a peptide agonist of the glucagon-like peptide (GLP) receptor that promotes insulin secretion. The aim of this study was to determine
C Montrose-Rafizadeh et al.
The Journal of biological chemistry, 272(34), 21201-21206 (1997-08-22)
GLP-1-(7-36)-amide and exendin-4-(1-39) are glucagon-like peptide-1 (GLP-1) receptor agonists, whereas exendin-(9-39) is the only known antagonist. To analyze the transition from agonist to antagonist and to identify the amino acid residues involved in ligand activation of the GLP-1 receptor, we
G Singh et al.
Regulatory peptides, 53(1), 47-59 (1994-08-31)
We synthesized and iodinated an exendin-4 analogue, [Y39]exendin-4 (700 Ci/mmol), for use as a radioligand to characterize exendin receptors on dispersed pancreatic acini and gastric chief cells from guinea pig. Binding of this bioactive radioligand was rapid, temperature-dependent and specific

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