基本描述

英文别名	Exendin-3 (9-39) \| DTXSID00158156 \| p \| EX-A7432 \| Exendin (9-39) \| Exendin-3 (9-39) amide \| Asp-LEU-SER-LYS-GLN-MET-GLU-GLU-GLU-ALA-VAL-ARG-LEU-PHE-ILE-GLU-TR \| AKOS024456934 \| ASP-LEU-SER-LYS-GLN-MET-GLU-GLU-GLU-ALA-VAL-ARG-LEU-PHE-ILE-GLU-TRP-LEU-LYS-A
规格或纯度	Moligand™, ≥95%(HPLC)
英文名称	Exendin Fragment 9-39
生化机理	GLP-1（胰高血糖素样肽-1）受体拮抗剂。强效、选择性 GLP-1 受体拮抗剂（K d = 1.7 nM）。抑制 GLP-1 (7-36)、exendin-3 和 exendin-4 诱导的细胞内 cAMP 的生成。在食欲调节、水盐平衡和胰岛素释放中发挥作用。在以下方面具有活性
储存温度	-20°C储存
运输条件	超低温冰袋运输
作用类型	拮抗剂
作用机制	GLP-1 受体拮抗剂
备注	如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，这些产品最多可以使用一周。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍	Amino Acid Sequence 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 Exendin Fragment 9-39 is an antagonist of glucagon-like peptide-1 (GLP-1) receptor, and also acts as an inhibitor of glucosedependent insulinotropic polypeptide (GIP)-receptor binding. It also prevents the production of cAMP by GIP. GLP-1, along with GIP, acts as a physiological incretin.Exendin Fragment 9-39 has been used to study its effect on basal microvascular permeability. Amino Acid Sequence 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 Exendin Fragment 9-39 is an antagonist of Glukagon-like peptide-1 (GLP-1) receptor, and also acts as an inhibitor of glucosedependent insulinotropic polypeptide (GIP)-receptor binding. It also prevents the production of cAMP by GIP. GLP-1, along with GIP, acts as a physiological incretin. Exendin Fragment 9-39 has been used to study its effect on basal microvascular permeability.
纯度	≥95%(HPLC)

关联靶点（人）

GLP1R Tclin 胰高血糖素类肽1受体(Glucagon-like peptide 1 receptor) (0 活性数据)

点击查看靶蛋白信息： GLP1R

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

作用机制

作用机制	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	参考文献

名称和识别符

分子类型	小分子
IIUPAC Name	(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-5-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-amino-3-carboxypropanoyl]amino]-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]-5-oxopentanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-4-amino-1-[[2-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[(2S)-2-[(2S)-2-[(2S)-2-[[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidine-1-carbonyl]pyrrolidine-1-carbonyl]pyrrolidin-1-yl]-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-2-oxoethyl]amino]-1,4-dioxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-4-carboxy-1-oxobutan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
INCHI	1S/C149H234N40O47S/c1-14-78(10)120(185-139(227)98(62-81-29-16-15-17-30-81)177-136(224)97(61-76(6)7)175-129(217)88(35-24-53-158-149(156)157)172-144(232)119(77(8)9)184-122(210)79(11)164-126(214)90(41-46-114(199)200)168-131(219)91(42-47-115(201)202)169-132(220)92(43-48-116(203)204)170-134(222)94(50-58-237-13)171-130(218)89(40-45-109(153)194)167-127(215)86(33-20-22-51-150)166-140(228)103(72-192)182-137(225)95(59-74(2)3)174-123(211)84(152)64-118(207)208)145(233)173-93(44-49-117(205)206)133(221)178-99(63-82-66-159-85-32-19-18-31-83(82)85)138(226)176-96(60-75(4)5)135(223)165-87(34-21-23-52-151)128(216)179-100(65-110(154)195)124(212)161-67-111(196)160-69-113(198)186-54-25-36-105(186)142(230)183-104(73-193)141(229)181-102(71-191)125(213)162-68-112(197)163-80(12)146(234)188-56-27-38-107(188)148(236)189-57-28-39-108(189)147(235)187-55-26-37-106(187)143(231)180-101(70-190)121(155)209/h15-19,29-32,66,74-80,84,86-108,119-120,159,190-193H,14,20-28,33-65,67-73,150-152H2,1-13H3,(H2,153,194)(H2,154,195)(H2,155,209)(H,160,196)(H,161,212)(H,162,213)(H,163,197)(H,164,214)(H,165,223)(H,166,228)(H,167,215)(H,168,219)(H,169,220)(H,170,222)(H,171,218)(H,172,232)(H,173,233)(H,174,211)(H,175,217)(H,176,226)(H,177,224)(H,178,221)(H,179,216)(H,180,231)(H,181,229)(H,182,225)(H,183,230)(H,184,210)(H,185,227)(H,199,200)(H,201,202)(H,203,204)(H,205,206)(H,207,208)(H4,156,157,158)/t78-,79-,80-,84-,86-,87-,88-,89-,90-,91-,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,119-,120-/m0/s1
InChi Key	WSEVKKHALHSUMB-MVNVRWBSSA-N
Smiles	CCC(C)C(C(=O)NC(CCC(=O)O)C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CC(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NCC(=O)NCC(=O)N3CCCC3C(=O)NC(CO)C(=O)NC(CO)C(=O)NCC(=O)NC(C)C(=O)N4CCCC4C(=O)N5CCCC5C(=O)N6CCCC6C(=O)NC(CO)C(=O)N)NC(=O)C(CC7=CC=CC=C7)NC(=O)C(CC(C)C)NC(=O)C(CCCNC(=N)N)NC(=O)C(C(C)C)NC(=O)C(C)NC(=O)C(CCC(=O)O)NC(=O)C(CCC(=O)O)NC(=O)C(CCC(=O)O)NC(=O)C(CCSC)NC(=O)C(CCC(=O)N)NC(=O)C(CCCCN)NC(=O)C(CO)NC(=O)C(CC(C)C)NC(=O)C(CC(=O)O)N
Isomeric SMILES	CC[C@H](C)[C@@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)N)C(=O)NCC(=O)NCC(=O)N3CCC[C@H]3C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N4CCC[C@H]4C(=O)N5CCC[C@H]5C(=O)N6CCC[C@H]6C(=O)N[C@@H](CO)C(=O)N)NC(=O)[C@H](CC7=CC=CC=C7)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(=O)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)N
PubChem CID	16198321
分子量	3369.76

化学和物理性质

分子量	3369.800 g/mol
XLogP3	-16.700
氢键供体数Hydrogen Bond Donor Count	45
氢键受体数Hydrogen Bond Acceptor Count	52
可旋转键计数Rotatable Bond Count	109
精确质量Exact Mass	3368.69 Da
单同位素质量Monoisotopic Mass	3367.69 Da
拓扑极表面积Topological Polar Surface Area	1420.000 Å²
重原子数Heavy Atom Count	237
形式电荷Formal Charge	0
复杂度Complexity	8000.000
同位素原子数Isotope Atom Count	0
定义的原子立体中心计数Defined Atom Stereocenter Count	29
未定义的原子立体中心计数Undefined Atom Stereocenter Count	0
定义的键立体中心计数Defined Bond Stereocenter Count	0
未定义的键立体中心计数Undefined Bond Stereocenter Count	0
所有立体化学键的总数The total count of all stereochemical bonds	0
共价键合单元计数Covalently-Bonded Unit Count	1

安全和危险性（GHS）

WGK Germany	3
个人防护装备	Eyeshields,Gloves,type N95 (US),type P1 (EN143) respirator filter

质检证书（CoA,COO,BSE/TSE 和分析图谱)

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找到2个结果

批号(Lot Number)	证书类型	货号
L1708007	分析证书	E101622
L1708006	分析证书	E101622

此产品的引用文献

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引用文献

1. Ng CM, Tang F, Seeholzer SH, Zou Y, De León DD. (2018) Population pharmacokinetics of exendin-(9-39) and clinical dose selection in patients with congenital hyperinsulinism.. Br J Clin Pharmacol, 84 (3): (520-532). [PMID:29077992]
2. Gasbjerg LS, Bergmann NC, Stensen S, Christensen MB, Rosenkilde MM, Holst JJ, Nauck M, Knop FK. (2020) Evaluation of the incretin effect in humans using GIP and GLP-1 receptor antagonists.. Peptides, 125 (170183). [PMID:31693916]
3. Tan M, Lamendola C, Luong R, McLaughlin T, Craig C. (2020) Safety, efficacy and pharmacokinetics of repeat subcutaneous dosing of avexitide (exendin 9-39) for treatment of post-bariatric hypoglycaemia.. Diabetes Obes Metab, 22 (8): (1406-1416). [PMID:32250530]
4. Kim KS et al.. (2017) Activation of intestinal olfactory receptor stimulates glucagon-like peptide-1 secretion in enteroendocrine cells and attenuates hyperglycemia in type 2 diabetic mice.. Sci Rep, 7 (13978). [PMID:29070885]
5. Hwang I et al.. (2015) Alteration of gut microbiota by vancomycin and bacitracin improves insulin resistance via glucagon-like peptide 1 in diet-induced obesity.. FASEB J, 29 (6): (2397-411). [PMID:25713030]
6. Kim KH et al.. (2018) Cucurbitacin B Induces Hypoglycemic Effect in Diabetic Mice by Regulation of AMP-Activated Protein Kinase Alpha and Glucagon-Like Peptide-1 via Bitter Taste Receptor Signaling.. Front Pharmacol, 9 (1071). [PMID:30298009]
7. Okabe K et al.. (2020) DPP (Dipeptidyl Peptidase)-4 Inhibitor Attenuates Ang II (Angiotensin II)-Induced Cardiac Hypertrophy via GLP (Glucagon-Like Peptide)-1-Dependent Suppression of Nox (Nicotinamide Adenine Dinucleotide Phosphate Oxidase) 4-HDAC (Histone Deacetylase) 4 Pathway.. Hypertension, 75 (4): (991-1001). [PMID:32160098]
8. Ohbayashi K et al.. (2021) Gastrointestinal Distension by Pectin-Containing Carbonated Solution Suppresses Food Intake and Enhances Glucose Tolerance via GLP-1 Secretion and Vagal Afferent Activation.. Front Endocrinol (Lausanne), 12 (676869). [PMID:34168616]
9. Tu Y et al.. (2021) Geniposide Attenuates Hyperglycemia-Induced Oxidative Stress and Inflammation by Activating the Nrf2 Signaling Pathway in Experimental Diabetic Retinopathy.. Oxid Med Cell Longev, 2021 (9247947). [PMID:34938383]
10. Saitoh Y et al.. (2021) Improvement of hepatocyte engraftment by co-transplantation with pancreatic islets in hepatocyte transplantation.. J Tissue Eng Regen Med, 15 (4): (361-374). [PMID:33484496]
11. Zhang Jian-Mei, Sun Yin-Shuang, Zhao Li-Qin, Chen Tian-Tian, Fan Mei-Na, Jiao Hong-Chao, Zhao Jing-Peng, Wang Xiao-Juan, Li Fu-Chang, Li Hai-Fang, Lin Hai. (2019) SCFAs-Induced GLP-1 Secretion Links the Regulation of Gut Microbiome on Hepatic Lipogenesis in Chickens. Frontiers in Microbiology, 10 (2176). [PMID:31616396] [10.3389/fmicb.2019.02176]
12. GengShan , YangShan , TangXuejiao , XueShiyao , LiKe , LiuDongfang , ChenChen , ZhuZhiming , ZhengHongting , WangYuanqiang , YangGangyi , LiLing , YangMengliu. (2024) Intestinal NUCB2/nesfatin-1 regulates hepatic glucose production via the MC4R-cAMP-GLP-1 pathway. EMBO JOURNAL, [PMID:39562740] [10.1038/s44318-024-00300-4]

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货号 (SKU)	包装规格	是否现货
E101622-0.5mg	0.5mg	现货
E101622-1mg	1mg	现货
E101622-5mg	5mg	现货

Exendin 片段 9-39, GLP-1 受体拮抗剂

库存信息

库存信息

库存信息

基本描述

关联靶点（人）

作用机制

名称和识别符

化学和物理性质

安全和危险性（GHS）

质检证书（CoA,COO,BSE/TSE 和分析图谱)

此产品的引用文献

引用文献

溶液计算器

摩尔浓度计算器

稀释计算器

复溶计算器