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Exendin 片段 9-39

高效的选择性GLP-1受体拮抗剂
规格或纯度: ≥95%(HPLC)
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
E101622-0.5mg
 0.5mg 现货 Stock Image
E101622-1mg
 1mg 现货 Stock Image
E101622-5mg
 5mg 现货 Stock Image
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GLP-1 receptor Antagonist
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基本描述

规格或纯度 ≥95%(HPLC)
英文名称 Exendin Fragment 9-39
别名 Exendin (9-39)
英文别名 Exendin (9-39) H-Asp-Leu-Ser-Lys-Gln-Met-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
生化机理 GLP-1 (glucagon-like peptide-1) receptor antagonist. Competitive inhibitor of exendin-3 and exendin-4.Potent, selective GLP-1 receptor antagonist (K d = 1.7 nM). Inhibits the generation of intracellular cAMP induced by GLP-1 (7-36), exendin-3 and exendin-4 . Role in appetite modulation, water and salt homeostasis and insulin release. Active in
储存温度 -20°C储存
运输条件 超低温冰袋运输
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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.

名称和标识符

IUPAC 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 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
Canonical 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
WGK Germany 3
PubChem CID 16198321
分子量 3369.76

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

关联配体

Ligand ID 1138
名称 exendin-(9-39)
别名 exendin (9-39)
类别 Peptide
学名 4-amino-N-(4,6-dimethylpyrimidin-2-yl)benzenesulfonamide
生物活性评价 The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in ).
评价 Exendin-(9-39) is a N-terminally truncated analogue of glucagon-like peptide 1 receptor (GLP-1R) agonist exendin-4. It acts as a GLP-1R antagonist, thus blocking the glucagonostatic and insulinotropic effects of GLP-1 . The C-terminally amidated peptide has the INN avexitide.
单字母多肽序列 DLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
三字母多肽序列 H-Asp-Leu-Ser-Lys-D-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
翻译后修饰
化学修饰
临床描述 The overall goal of this project is to understand the mechanisms by which gastric bypass surgery improves glucose metabolism. The central hypothesis guiding this project is that the reconfiguration of intestinal transit with the Roux-en-Y will increase the release of insulinotropic GI hormones, termed incretins that improve insulin secretion and glucose metabolism. The study is divided into three specific aims. 1. To determine the role of incretin hormones on insulin secretion in patients with gastric bypass surgery using intravenous-oral hyperglycemic clamp. 2. To compare incretin effect and glucose tolerance among patient who suffer from hypoglycemia after RYGB and asymptomatic surgical and non-surgical individuals. 3. To quantify the contribution of GLP-1 to incretin effect enhancement following surgery.
The purpose of this study is learn the effect of gastric bypass surgery and sleeve gastrectomy on glucose metabolism mediated by neural and hormonal factors initiated after eating.
来源公司 The University of Texas Health Science Center at San Antonio
The University of Texas Health Science Center at San Antonio

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参考文献

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  (13):  (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]
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