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Merck
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Key Documents

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號碼:
分類程式碼代碼:
51111800
NACRES:
NA.32

品質等級

化驗

≥97%

儲存溫度

−20°C

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 密鑰

HTQBXNHDCUEHJF-XWLPCZSASA-N

基因資訊

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

一般說明

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。

應用

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。

包裝

无底玻璃瓶。内含物装在插入的融合锥内。

其他說明

合成生产
从0.1%TFA水溶液中冻干

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable

個人防護裝備

Eyeshields, Gloves, type N95 (US)


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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
SIRT1 mediates the effect of GLP-1 receptor agonist exenatide on ameliorating hepatic steatosis
Xu F, et al.
Diabetes, 63(11), 3637-3646 (2014)
Anujith Kumar et al.
PloS one, 8(5), e63491-e63491 (2013-05-15)
β-cell replacement may efficiently cure type 1 diabetic (T1D) patients whose insulin-secreting β-cells have been selectively destroyed by autoantigen-reactive T cells. To generate insulin-secreting cells we used two cell sources: rat multipotent adult progenitor cells (rMAPC) and the highly similar
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
Abdul Bari Muhammad et al.
American journal of physiology. Endocrinology and metabolism, 313(2), E148-E166 (2017-03-09)
Menin is a scaffold protein that interacts with several epigenetic mediators to regulate gene transcription, and suppresses pancreatic β-cell proliferation. Tamoxifen-inducible deletion of multiple endocrine neoplasia type 1 (

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