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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

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
规格或纯度 ≥95%(HPLC)
英文名称 Exendin Fragment 9-39
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 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.

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

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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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