Volagidemab (anti-GCGR), 胰高血糖素受体抑制剂

COA

级别和纯度:

≥95%(SDS-PAGE&SEC-HPLC)
见COA

应用:

Animal Model
ELISA
Flow Cytometry
Functional Assay

宿主种属: 人(Human)
种属反应性: 人(Human), 小鼠(Mouse)
亚型: Human IgG2
偶联: Unconjugated

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货号 (SKU)	包装规格	是否现货
Ab177921-100μg	100μg	现货
Ab177921-1mg	1mg	现货
Ab177921-5mg	5mg	现货
Ab177921-10mg	10mg	期货

查看相关系列

点击查看靶蛋白信息: GCGR

Accession#:P47871 (2) Class B GPCR (425) GCGR (65) Gene ID:2642 (2)

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基本信息

产品名称	Volagidemab (anti-GCGR), 胰高血糖素受体抑制剂
别名	沃拉吉单抗（抗GCGR）
英文别名	GL-R
规格或纯度	无载体, 重组, ExactAb™, 低内毒素, 无叠氮钠, 已验证, 无动物源, ≥95%(SDS-PAGE&SEC-HPLC), 见COA
宿主种属	人(Human)
特异性	GCGR
种属反应性	人(Human),小鼠(Mouse)
偶联	Unconjugated
作用类型	抑制剂
作用机制	胰高血糖素受体抑制剂

产品属性

克隆类型	重组抗体
Format	Whole IgG
亚型	Human IgG2
轻链亚型	kappa
SDS-PAGE	26.8 kDa (Light Chain) & 51.8 kDa (Heavy Chain), under reducing conditions; 177.3 kDa, under non-reducing conditions.
纯化方法	Protein A purified
纯度	>95%
物理外观	Liquid
防腐剂	No
浓度	见COA
储存温度	-80℃储存,避免反复冻融
运输条件	超低温冰袋运输
稳定性与储存	在 -80℃ 下保存 24 个月。收货后建议分装。避免冷冻/解冻循环。
CAS编号和信息	1233956-13-2
分子类型	抗体

关联靶点（人）

GCGR Tclin 胰高血糖素受体(Glucagon receptor) (0 活性数据)

点击查看靶蛋白信息： GCGR

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

图片

ELISA: Volagidemab (anti-GCGR) (Ab177921)

Volagidemab (anti-GCGR) (Ab177921) - ELISA
Immobilized Human GCGR/GLR-VLP at 2.0 μg/mL can bind Volagidemab (anti-GCGR) (Ab177921) with the EC₅₀ of 78.24 ng/mL.

SEC: Volagidemab (anti-GCGR) (Ab177921)

Volagidemab (anti-GCGR) (Ab177921) - SEC
The purity of Volagidemab (anti-GCGR) (Ab177921) is more than 95% verified by HPLC.

质检证书（CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):

输入批号以搜索分析图谱:

通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！

找到6个结果

批号(Lot Number)	证书类型	货号
ZJ24F1114526	分析证书	Ab177921
ZJ24F1114525	分析证书	Ab177921
ZJ24F1114524	分析证书	Ab177921
ZJ24F0404033	分析证书	Ab177921
ZJ24F0404035	分析证书	Ab177921
ZJ24F0404034	分析证书	Ab177921

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引用文献

1. Ladouceur GH, Cook JH, Doherty EM, Schoen WR, MacDougall ML, Livingston JN.. (2002) Discovery of 5-hydroxyalkyl-4-phenylpyridines as a new class of glucagon receptor antagonists.. Bioorg Med Chem Lett, 12 (3): (461-464). [PMID:11814820] [10.1016/s0960-894x(01)00766-1]
2. Madsen P, Ling A, Plewe M, Sams CK, Knudsen LB, Sidelmann UG, Ynddal L, Brand CL, Andersen B, Murphy D, Teng M, Truesdale L, Kiel D, May J, Kuki A, Shi S, Johnson MD, Teston KA, Feng J, Lakis J, Anderes K, Gregor V, Lau J.. (2002) Optimization of alkylidene hydrazide based human glucagon receptor antagonists. Discovery of the highly potent and orally available 3-cyano-4-hydroxybenzoic acid [1-(2,3,5,6-tetramethylbenzyl)-1H-indol-4-ylmethylene]hydrazide.. J Med Chem, 45 (26): (5755-5775). [PMID:12477359] [10.1021/jm0208572]
3. Lok S, Kuijper JL, Jelinek LJ, Kramer JM, Whitmore TE, Sprecher CA, Mathewes S, Grant FJ, Biggs SH, Rosenberg GB et al.. (1994) The human glucagon receptor encoding gene: structure, cDNA sequence and chromosomal localization.. Gene, 140 (2): (203-9). [PMID:8144028]
4. Menzel S, Stoffel M, Espinosa 3rd R, Fernald AA, Le Beau MM, Bell GI. (1994) Localization of the glucagon receptor gene to human chromosome band 17q25.. Genomics, 20 (2): (327-8). [PMID:8020989]
5. MacNeil DJ, Occi JL, Hey PJ, Strader CD, Graziano MP. (1994) Cloning and expression of a human glucagon receptor.. Biochem Biophys Res Commun, 198 (1): (328-34). [PMID:7507321]
6. Petersen KF, Sullivan JT. (2001) Effects of a novel glucagon receptor antagonist (Bay 27-9955) on glucagon-stimulated glucose production in humans.. Diabetologia, 44 (11): (2018-24). [PMID:11719833]
7. Siu FY, He M, de Graaf C, Han GW, Yang D, Zhang Z, Zhou C, Xu Q, Wacker D, Joseph JS et al.. (2013) Structure of the human glucagon class B G-protein-coupled receptor.. Nature, 499 (7459): (444-9). [PMID:23863937]
8. Koth CM, Murray JM, Mukund S, Madjidi A, Minn A, Clarke HJ, Wong T, Chiang V, Luis E, Estevez A et al.. (2012) Molecular basis for negative regulation of the glucagon receptor.. Proc Natl Acad Sci USA, 109 (36): (14393-8). [PMID:22908259]
9. Ma ML, Li M, Gou JJ, Ruan TY, Jin HS, Zhang LH, Wu LC, Li XY, Hu YH, Wen K et al.. (2014) Design, synthesis and biological activity of flavonoid derivatives as selective agonists for neuromedin U 2 receptor.. Bioorg Med Chem, 22 (21): (6117-23). [PMID:25262941]
10. Xiong Y, Guo J, Candelore MR, Liang R, Miller C, Dallas-Yang Q, Jiang G, McCann PE, Qureshi SA, Tong X et al.. (2012) Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes.. J Med Chem, 55 (13): (6137-48). [PMID:22708876]
11. Jazayeri A, Doré AS, Lamb D, Krishnamurthy H, Southall SM, Baig AH, Bortolato A, Koglin M, Robertson NJ, Errey JC et al.. (2016) Extra-helical binding site of a glucagon receptor antagonist.. Nature, 533 (7602): (274-7). [PMID:27111510]
12. Kazda CM, Ding Y, Kelly RP, Garhyan P, Shi C, Lim CN, Fu H, Watson DE, Lewin AJ, Landschulz WH et al.. (2016) Evaluation of Efficacy and Safety of the Glucagon Receptor Antagonist LY2409021 in Patients With Type 2 Diabetes: 12- and 24-Week Phase 2 Studies.. Diabetes Care, 39 (7): (1241-9). [PMID:26681715]
13. Kelly RP, Garhyan P, Raddad E, Fu H, Lim CN, Prince MJ, Pinaire JA, Loh MT, Deeg MA. (2015) Short-term administration of the glucagon receptor antagonist LY2409021 lowers blood glucose in healthy people and in those with type 2 diabetes.. Diabetes Obes Metab, 17 (4): (414-22). [PMID:25656305]
14. Zhang H, Qiao A, Yang D, Yang L, Dai A, de Graaf C, Reedtz-Runge S, Dharmarajan V, Zhang H, Han GW et al.. (2017) Structure of the full-length glucagon class B G-protein-coupled receptor.. Nature, 546 (7657): (259-264). [PMID:28514451]
15. Okamoto H, Kim J, Aglione J, Lee J, Cavino K, Na E, Rafique A, Kim JH, Harp J, Valenzuela DM et al.. (2015) Glucagon Receptor Blockade With a Human Antibody Normalizes Blood Glucose in Diabetic Mice and Monkeys.. Endocrinology, 156 (8): (2781-94). [PMID:26020795]
16. Rottmann M, McNamara C, Yeung BK, Lee MC, Zou B, Russell B, Seitz P, Plouffe DM, Dharia NV, Tan J et al.. (2010) Spiroindolones, a potent compound class for the treatment of malaria.. Science, 329 (5996): (1175-80). [PMID:20813948]
17. Zhang H, Qiao A, Yang L, Van Eps N, Frederiksen KS, Yang D, Dai A, Cai X, Zhang H, Yi C et al.. (2018) Structure of the glucagon receptor in complex with a glucagon analogue.. Nature, 553 (7686): (106-110). [PMID:29300013]
18. Wiśniewski K, Sueiras-Diaz J, Jiang G, Galyean R, Lu M, Thompson D, Wang YC, Croston G, Posch A, Hargrove DM et al.. (2016) Synthesis and Pharmacological Characterization of Novel Glucagon-like Peptide-2 (GLP-2) Analogues with Low Systemic Clearance.. J Med Chem, 59 (7): (3129-39). [PMID:26986178]
19. Angst D, Gessier F, Janser P, Vulpetti A, Wälchli R, Beerli C, Littlewood-Evans A, Dawson J, Nuesslein-Hildesheim B, Wieczorek G et al.. (2020) Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.. J Med Chem, 63 (10): (5102-5118). [PMID:32083858]
20. Liang R, Abrardo L, Brady EJ, Candelore MR, Ding V, Saperstein R, Tota LM, Wright M, Mock S, Tamvakopolous C, Tong S, Zheng S, Zhang BB, Tata JR, Parmee ER.. (2007) Design and synthesis of conformationally constrained tri-substituted ureas as potent antagonists of the human glucagon receptor.. Bioorg Med Chem Lett, 17 (3): (587-592). [PMID:17126016] [10.1016/j.bmcl.2006.11.014]
21. Knudsen LB, Kiel D, Teng M, Behrens C, Bhumralkar D, Kodra JT, Holst JJ, Jeppesen CB, Johnson MD, de Jong JC, Jorgensen AS, Kercher T, Kostrowicki J, Madsen P, Olesen PH, Petersen JS, Poulsen F, Sidelmann UG, Sturis J, Truesdale L, May J, Lau J.. (2007) Small-molecule agonists for the glucagon-like peptide 1 receptor.. Proc Natl Acad Sci U S A, 104 (3): (937-942). [PMID:17213325] [10.1073/pnas.0605701104]
22. Kim RM, Chang J, Lins AR, Brady E, Candelore MR, Dallas-Yang Q, Ding V, Dragovic J, Iliff S, Jiang G, Mock S, Qureshi S, Saperstein R, Szalkowski D, Tamvakopoulos C, Tota L, Wright M, Yang X, Tata JR, Chapman K, Zhang BB, Parmee ER.. (2008) Discovery of potent, orally active benzimidazole glucagon receptor antagonists.. Bioorg Med Chem Lett, 18 (13): (3701-3705). [PMID:18539028] [10.1016/j.bmcl.2008.05.072]
23. Kodra JT, Jørgensen AS, Andersen B, Behrens C, Brand CL, Christensen IT, Guldbrandt M, Jeppesen CB, Knudsen LB, Madsen P, Nishimura E, Sams C, Sidelmann UG, Pedersen RA, Lynn FC, Lau J.. (2008) Novel glucagon receptor antagonists with improved selectivity over the glucose-dependent insulinotropic polypeptide receptor.. J Med Chem, 51 (17): (5387-5396). [PMID:18707090] [10.1021/jm7015599]
24. Madsen P, Kodra JT, Behrens C, Nishimura E, Jeppesen CB, Pridal L, Andersen B, Knudsen LB, Valcarce-Aspegren C, Guldbrandt M, Christensen IT, Jørgensen AS, Ynddal L, Brand CL, Bagger MA, Lau J.. (2009) Human glucagon receptor antagonists with thiazole cores. A novel series with superior pharmacokinetic properties.. J Med Chem, 52 (9): (2989-3000). [PMID:19385613] [10.1021/jm8016249]
25. Mapelli C, Natarajan SI, Meyer JP, Bastos MM, Bernatowicz MS, Lee VG, Pluscec J, Riexinger DJ, Sieber-McMaster ES, Constantine KL, Smith-Monroy CA, Golla R, Ma Z, Longhi DA, Shi D, Xin L, Taylor JR, Koplowitz B, Chi CL, Khanna A, Robinson GW, Seethala R, Antal-Zimanyi IA, Stoffel RH, Han S, Whaley JM, Huang CS, Krupinski J, Ewing WR.. (2009) Eleven amino acid glucagon-like peptide-1 receptor agonists with antidiabetic activity.. J Med Chem, 52 (23): (7788-7799). [PMID:19702274] [10.1021/jm900752a]
26. Day JW, Ottaway N, Patterson JT, Gelfanov V, Smiley D, Gidda J, Findeisen H, Bruemmer D, Drucker DJ, Chaudhary N, Holland J, Hembree J, Abplanalp W, Grant E, Ruehl J, Wilson H, Kirchner H, Lockie SH, Hofmann S, Woods SC, Nogueiras R, Pfluger PT, Perez-Tilve D, DiMarchi R, Tschöp MH.. (2009) A new glucagon and GLP-1 co-agonist eliminates obesity in rodents.. Nat Chem Biol, 5 (10): (749-757). [PMID:19597507] [10.1038/nchembio.209]
27. Sinz C, Chang J, Lins AR, Brady E, Candelore M, Dallas-Yang Q, Ding V, Jiang G, Lin Z, Mock S, Qureshi S, Salituro G, Saperstein R, Shang J, Szalkowski D, Tota L, Vincent S, Wright M, Xu S, Yang X, Zhang B, Tata J, Kim R, Parmee E.. (2011) Discovery of cyclic guanidines as potent, orally active, human glucagon receptor antagonists.. Bioorg Med Chem Lett, 21 (23): (7131-7136). [PMID:22001094] [10.1016/j.bmcl.2011.09.085]
28. Filipski KJ, Bian J, Ebner DC, Lee EC, Li JC, Sammons MF, Wright SW, Stevens BD, Didiuk MT, Tu M, Perreault C, Brown J, Atkinson K, Tan B, Salatto CT, Litchfield J, Pfefferkorn JA, Guzman-Perez A.. (2012) A novel series of glucagon receptor antagonists with reduced molecular weight and lipophilicity.. Bioorg Med Chem Lett, 22 (1): (415-420). [PMID:22119466] [10.1016/j.bmcl.2011.10.113]
29. Guzman-Perez A, Pfefferkorn JA, Lee EC, Stevens BD, Aspnes GE, Bian J, Didiuk MT, Filipski KJ, Moore D, Perreault C, Sammons MF, Tu M, Brown J, Atkinson K, Litchfield J, Tan B, Samas B, Zavadoski WJ, Salatto CT, Treadway J.. (2013) The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus.. Bioorg Med Chem Lett, 23 (10): (3051-3058). [PMID:23562063] [10.1016/j.bmcl.2013.03.014]
30. DeMong D, Dai X, Hwa J, Miller M, Lin SI, Kang L, Stamford A, Greenlee W, Yu W, Wong M, Lavey B, Kozlowski J, Zhou G, Yang DY, Patel B, Soriano A, Zhai Y, Sondey C, Zhang H, Lachowicz J, Grotz D, Cox K, Morrison R, Andreani T, Cao Y, Liang M, Meng T, McNamara P, Wong J, Bradley P, Feng KI, Belani J, Chen P, Dai P, Gauuan J, Lin P, Zhao H.. (2014) The discovery of N-((2H-tetrazol-5-yl)methyl)-4-((R)-1-((5r,8R)-8-(tert-butyl)-3-(3,5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl)-4,4-dimethylpentyl)benzamide (SCH 900822): a potent and selective glucagon receptor antagonist.. J Med Chem, 57 (6): (2601-2610). [PMID:24527772] [10.1021/jm401858f]
31. Evers A, Bossart M, Pfeiffer-Marek S, Elvert R, Schreuder H, Kurz M, Stengelin S, Lorenz M, Herling A, Konkar A, Lukasczyk U, Pfenninger A, Lorenz K, Haack T, Kadereit D, Wagner M.. (2018) Dual Glucagon-like Peptide 1 (GLP-1)/Glucagon Receptor Agonists Specifically Optimized for Multidose Formulations.. J Med Chem, 61 (13): (5580-5593). [PMID:29879354] [10.1021/acs.jmedchem.8b00292]
32. Zhou J, Cai X, Huang X, Dai Y, Sun L, Zhang B, Yang B, Lin H, Huang W, Qian H.. (2017) A novel glucagon-like peptide-1/glucagon receptor dual agonist exhibits weight-lowering and diabetes-protective effects.. Eur J Med Chem, 138 (1158-1169). [PMID:28772236] [10.1016/j.ejmech.2017.07.046]
33. Choi H, Lee CY, Park EY, Lee KM, Shin D, Jun HS.. (2018) Design, synthesis, and effects of novel phenylpyrimidines as glucagon receptor antagonists.. Bioorg Med Chem, 26 (21): (5701-5710). [PMID:30366787] [10.1016/j.bmc.2018.10.013]
34. Méndez M, Matter H, Defossa E, Kurz M, Lebreton S, Li Z, Lohmann M, Löhn M, Mors H, Podeschwa M, Rackelmann N, Riedel J, Safar P, Thorpe DS, Schäfer M, Weitz D, Breitschopf K.. (2020) Design, Synthesis, and Pharmacological Evaluation of Potent Positive Allosteric Modulators of the Glucagon-like Peptide-1 Receptor (GLP-1R).. J Med Chem, 63 (5): (2292-2307). [PMID:31596080] [10.1021/acs.jmedchem.9b01071]
35. Song F, Xu G, Gaul MD, Zhao B, Lu T, Zhang R, DesJarlais RL, DiLoreto K, Huebert N, Shook B, Rentzeperis D, Santulli R, Eckardt A, Demarest K.. (2019) Design, synthesis and structure activity relationships of indazole and indole derivatives as potent glucagon receptor antagonists.. Bioorg Med Chem Lett, 29 (15): (1974-1980). [PMID:31138472] [10.1016/j.bmcl.2019.05.036]
36. Xu G, Gaul MD, Song F, Du F, Liang Y, DesJarlais RL, DiLoreto K, Shook B, Rentzeperis D, Santulli R, Eckardt A, Demarest K.. (2019) Discovery of potent and orally bioavailable indazole-based glucagon receptor antagonists for the treatment of type 2 diabetes.. Bioorg Med Chem Lett, 29 (20): (126668-126668). [PMID:31519374] [10.1016/j.bmcl.2019.126668]
37. Mroz PA, Perez-Tilve D, Liu F, Gelfanov V, DiMarchi RD, Mayer JP.. (2016) Pyridyl-alanine as a Hydrophilic, Aromatic Element in Peptide Structural Optimization.. J Med Chem, 59 (17): (8061-8067). [PMID:27509198] [10.1021/acs.jmedchem.6b00840]
38. Wang C,Zhang YF,Guo S,Zhao Q,Zeng Y,Xie Z,Xie X,Lu B,Hu Y. (2021) GPR52 Antagonist Reduces Huntingtin Levels and Ameliorates Huntington's Disease-Related Phenotypes.. J Med Chem, 64 (2.0): (941-957). [PMID:33185430] [10.1021/acs.jmedchem.0c01133]
39. Fujisawa, T T and 8 more authors.. (1995) A mutation in the glucagon receptor gene (Gly40Ser): heterogeneity in the association with diabetes mellitus.. Diabetologia, [PMID:7589886]
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41. Rückert, Christine C and 8 more authors.. (2006) Conformational dimorphism of self-peptides and molecular mimicry in a disease-associated HLA-B27 subtype.. The Journal of biological chemistry, (27): [PMID:16221670]
42. Winzell, M Sörhede MS and 6 more authors.. (2007) Glucagon receptor antagonism improves islet function in mice with insulin resistance induced by a high-fat diet.. Diabetologia, [PMID:17479245]
43. Li, Pengyun P, Rogers, Tanya T, Smiley, David D, DiMarchi, Richard D RD and Zhang, Faming F.. (2007) Design, synthesis and crystallization of a novel glucagon analog as a therapeutic agent.. Acta crystallographica. Section F, Structural biology and crystallization communications, (1): [PMID:17620721]
44. Li, Xiao C XC and Zhuo, Jia L JL.. (2007) Targeting glucagon receptor signalling in treating metabolic syndrome and renal injury in Type 2 diabetes: theory versus promise.. Clinical science (London, England : 1979), [PMID:17623014]
45. Zhou, Cuiqi C, Dhall, Deepti D, Nissen, Nicholas N NN, Chen, Chun-Rong CR and Yu, Run R.. (2009) Homozygous P86S mutation of the human glucagon receptor is associated with hyperglucagonemia, alpha cell hyperplasia, and islet cell tumor.. Pancreas, [PMID:19657311]
46. Sipos, Bence B and 13 more authors.. (2015) Glucagon cell hyperplasia and neoplasia with and without glucagon receptor mutations.. The Journal of clinical endocrinology and metabolism, [PMID:25695890]
47. Gild, Matti L ML and 5 more authors.. (2018) Hypercalcemia in Glucagon Cell Hyperplasia and Neoplasia (Mahvash Syndrome): A New Association.. The Journal of clinical endocrinology and metabolism, (1): [PMID:30032256]
48. Li, Hong H and 9 more authors.. (2018) The first pediatric case of glucagon receptor defect due to biallelic mutations in GCGR is identified by newborn screening of elevated arginine.. Molecular genetics and metabolism reports, [PMID:30294546]

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Volagidemab (anti-GCGR), 胰高血糖素受体抑制剂

库存信息

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库存信息

基本信息

产品属性

关联靶点（人）

作用机制

图片

质检证书（CoA,COO,BSE/TSE 和分析图谱)

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引用文献

溶液计算器

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复溶计算器