Olcegepant NEW
| Price | $31 | $47 | $97 |
| Package | 1mg | 2mg | 5mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-19 |
Product Details
| Product Name: Olcegepant | CAS No.: 204697-65-4 |
| Purity: 96.08% | Supply Ability: 10g |
| Release date: 2024/11/19 |
Product Introduction
Bioactivity
| Name | Olcegepant |
| Description | Olcegepant (BIBN-4096) is an effective and selective non-peptide calcitonin gene-related peptide 1 (CGRP1) receptor antagonist (IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP). |
| In vitro | Olcegepant exhibits exceptional efficacy at primate CGRP receptors, demonstrating a high affinity (Ki) of 14.4±6.3 (n=4) pM for human CGRP receptors, surpassing that of the endogenous ligand CGRP and demonstrating a 150-fold greater affinity than the peptidic antagonist CGRP8-37. It competitively antagonizes CGRP-induced concentration-dependent relaxation, effectively reversing CGRP-mediated vasodilation in human cerebral vessels and inhibiting neurogenic vasodilation in a surrogate animal model for migraine pathophysiology. This suggests that Olcegepant, acting as a CGRP receptor antagonist, may be a potential novel abortive treatment for migraines. Its competitive antagonism has also been confirmed in SK-N-MC cells, with its effects observed in isolated human cerebral, coronary, and omental arteries using sensitive myograph techniques[1][2][3]. |
| In vivo | Pre-treatment with Olcegepant (900 μg/kg) inhibits capsaicin-induced Fos expression in the spinal trigeminal nucleus by 57%, without altering phosphorylated extracellular signal-regulated kinase expression in the trigeminal ganglion. Olcegepant (1-30 μg/kg, i.v.) suppresses CGRP effects on facial blood flow in marmosets and significantly reduces mechanical allodynia in CCI-ION rats (0.3-0.9 mg/kg, i.v.). Additionally, Olcegepant (0.6 mg/kg, i.v.) decreases c-Fos immunolabeled cells and ATF3 transcript upregulation, but not interleukin-6, in the trigeminal ganglion of CCI-ION rats [2][4][5]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 23.81 mg/mL (27.38 mM), Sonication is recommended. |
| Keywords | inhibit | BIBN 4096 | Olcegepant | BIBN4096 | CGRP Receptor | Calcitonin gene-related peptide receptor | Inhibitor |
| Inhibitors Related | HCGRP-(8-37) acetate | Ubrogepant | Rimegepant | Vazegepant hydrochloride | Vazegepant | CGRP 8-37 (rat) | β-CGRP, human acetate | Calcitonin（salmon） Acetate(47931-85-1(free base)) | Galcanezumab | Calcitonin (salmon) | Erenumab | CGRP antagonist 1 |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library | Ion Channel Targeted Library | Anti-Cancer Drug Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
You may like
Recommended supplier
| Product name | Price | Suppliers | Update time | |
|---|---|---|---|---|
| $31.00/1mg |
VIP5Y
|
TargetMol Chemicals Inc.
|
2024-11-19 | |
| $15.00/1KG |
Zhuozhou Wenxi import and Export Co., Ltd
|
2021-07-10 | ||
| $15.00/1KG |
Zhuozhou Wenxi import and Export Co., Ltd
|
2021-07-08 |
United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
INQUIRY