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Submit ReviewBIBN 4096
说明： Potent and selective CGRP antagonist
别名： Olcegepant
化学名： 1-[3,5-Dibromo-N-[[4-(1,4-dihydro-2-oxo-3(2H)-quinazolinyl)-1-piperidinyl]carbonyl]-D-tyrosyl-L-lysyl]-4-(4-pyridinyl)-piperazine
纯度： ≥95% (HPLC)
生物活性 for BIBN 4096
BIBN 4096 is a potent and selective CGRP receptor antagonist (IC50 values are 0.03 and 6.4 nM for human and rat CGRP receptors respectively). Displays high affinity for human CGRP receptors (Ki = 14.4 pM); exhibits no significant affinity for 75 other receptors. BIBN 4096 improves pain symptoms in a mouse migraine model.
技术数据 for BIBN 4096
| 分子量 | 869.65 |
| 公式 | C38H47Br2N9O5 |
| 储存 | Store at -20°C |
| 纯度 | ≥95% (HPLC) |
| CAS Number | 204697-65-4 |
| PubChem ID | 6918509 |
| InChI Key | ITIXDWVDFFXNEG-JHOUSYSJSA-N |
| Smiles | O=C(N[C@H](CC4=CC(Br)=C(O)C(Br)=C4)C(N[C@@H](CCCCN)C(N5CCN(C6=CC=NC=C6)CC5)=O)=O)N(CC3)CCC3N2CC1=CC=CC=C1NC2=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for BIBN 4096
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 43.48 | 50 | |
| 2eq.HCl | 43.48 | 50 |
制备储备液 for BIBN 4096
以下数据基于产品分子量 869.65。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 2.3 mL | 11.5 mL | 23 mL |
| 2.5 mM | 0.46 mL | 2.3 mL | 4.6 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 25 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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产品说明书 for BIBN 4096
参考文献 for BIBN 4096
参考文献是支持产品生物活性的出版物。
Doods et al (2000) Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br.J.Pharmacol. 129 420 PMID: 10711339
Rudolf et al (2005) Development of human calcitonin gene-related peptide (CGRP) receptor antagonists. 1. Potent and selective small molecule CGRP antagonists. 1-[N2-[3,5-Dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1- piperidinyl J.Med.Chem. 48 5921 PMID: 16161996
Prado et al (2021) TREK channel activation suppresses migraine pain phenotype. iScience 24 102961 PMID: 34458705
If you know of a relevant reference for BIBN 4096, please let us know.
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关键词: BIBN 4096, BIBN 4096 supplier, BIBN4096, migraine, potent, selective, CGRP, receptors, antagonists, calcitonin, gene-related, peptides, Olcegepant, Calcitonin, and, Related, Receptors, 4561, Tocris Bioscience
15 篇 BIBN 4096 的引用文献
引用文献是使用了 Tocris 产品的出版物。 BIBN 4096 的部分引用包括：
Corey R et al (2022) Nociceptor neurons affect cancer immunosurveillance. Nature 611 405-412 PMID: 36323780
Kai et al (2022) Src Family Kinases Facilitate the Crosstalk between CGRP and Cytokines in Sensitizing Trigeminal Ganglion via Transmitting CGRP Receptor/PKA Pathway. Cells 11 PMID: 36359895
Shuai et al (2022) Nociceptor Neurons are Involved in the Host Response to Escherichia coli Urinary Tract Infections. J Inflamm Res 15 3337-3353 PMID: 35702548
Pinho-Ribeiro et al (2018) Blocking Neuronal Signaling to Immune Cells Treats Streptococcal Invasive Infection. Cell 173 1083 PMID: 29754819
Keith M et al (2020) Paracrine signalling by cardiac calcitonin controls atrial fibrogenesis and arrhythmia. Nature 587 460-465 PMID: 33149301
Qini et al (2020) Characterization of the effects of calcitonin gene-related peptide receptor antagonist for Alzheimer's disease. Neuropharmacology 168 108017 PMID: 32113968
Aubdool et al (2014) TRPA1 is essential for the vascular response to environmental cold exposure. Nat Commun 5 5732 PMID: 25501034
Engelstoft et al (2013) Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells. Mol Metab 2 376 PMID: 24327954
Zhen et al (2023) Lidocaine alleviates inflammation and pruritus in atopic dermatitis by blocking different population of sensory neurons. Br J Pharmacol 180 1339-1361 PMID: 36521846
Ian M et al (2023) Inhibition of CGRP signaling impairs fracture healing in mice. J Orthop Res 41 1228-1239 PMID: 36281531
Zhao and Levy (2018) The CGRP receptor antagonist BIBN4096 inhibits prolonged meningeal afferent activation evoked by brief local K+ stimulation but not cortical spreading depression-induced afferent sensitization. Pain Rep 3 e632 PMID: 29430561
Prado et al (2021) TREK channel activation suppresses migraine pain phenotype. iScience 24 102961 PMID: 34458705
Craig L et al (2021) Role of perivascular nerve and sensory neurotransmitter dysfunction in inflammatory bowel disease. Am J Physiol Heart Circ Physiol 320 H1887-H1902 PMID: 33710922
Stuart B et al (2018) Reflex regulation of breathing by the paratrigeminal nucleus via multiple bulbar circuits. Brain Struct Funct 223 4005-4022 PMID: 30116890
M et al (2016) Amylin modulates the formalin-induced tonic pain behaviours in rats. Eur J Pain 20 1741-1752 PMID: 27264026
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