Olcegepant
Based on 45 publication(s) in Google Scholar
Olcegepant (BIBN-4096) is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.07%
- CAS. Nr.: 204697-65-4
- Formel: C38H47Br2N9O5
- Molecular Weight:869.65
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) Olcegepant
More- Nat Med. 2016 Oct;22(10):1160-1169. [Abstract]
- Cell. 2026 May 19:S0092-8674(26)00505-2. [Abstract]
- Cell. 2024 Jun 6;187(12):2935-2951.e19. [Abstract]
- Adv Sci (Weinh). 2026 Apr;13(21):e24181. [Abstract]
- Adv Sci (Weinh). 2025 Apr;12(14):e2409251. [Abstract]
- Adv Sci (Weinh). 2024 Aug;11(30):e2400242. [Abstract]
- Adv Sci (Weinh). 2021 Oct 28;e2103005. [Abstract]
- J Orthop Translat. 2026 May 8:58:101113. [Abstract]
- Small Methods. 2024 Dec;8(12):e2400216. [Abstract]
- J Headache Pain. 2024 Oct 10;25(1):176. [Abstract]
- J Headache Pain. 2024 Aug 21;25(1):136. [Abstract]
- J Headache Pain. 2022 Sep 30;23(1):128. [Abstract]
- J Headache Pain. 2022 Mar 8;23(1):35. [Abstract]
- Cell Rep. 2026 Mar 24;45(4):117201. [Abstract]
- Cell Rep. 2024 Oct 15;43(10):114859. [Abstract]
- Br J Pharmacol. 2024 Sep;181(17):3136-3159. [Abstract]
- J Invest Dermatol. 2019 Mar;139(3):656-664. [Abstract]
- Biochem Pharmacol. 2026 Jun:248:117840. [Abstract]
- Cell Mol Life Sci. 2024 Aug 28;81(1):373. [Abstract]
- Int Endod J. 2024 Jan;57(1):37-49. [Abstract]
- Cephalalgia. 2024 Jul;44(7):3331024241254088. [Abstract]
- Cephalalgia. 2021 Mar;41(3):329-339. [Abstract]
- Cephalalgia. 2020 Aug;40(9):924-934. [Abstract]
- Cephalalgia. 2019 Dec;39(14):1827-1837. [Abstract]
- Int Immunopharmacol. 2024 Mar 30:130:111766. [Abstract]
- Int J Mol Sci. 2019 Nov 20;20(23):5826. [Abstract]
- Invest Ophthalmol Vis Sci. 2026 Apr 1;67(4):60. [Abstract]
- Invest Ophthalmol Vis Sci. 2026 Jan 5;67(1):10. [Abstract]
- Sci Rep. 2022 Aug 16;12(1):13894. [Abstract]
- Sci Rep. 2020 Jul 10;10(1):11408. [Abstract]
- Sci Rep. 2018 Jan 30;8(1):1836. [Abstract]
- Front Cell Neurosci. 2018 Sep 11:12:304. [Abstract]
- Korean J Pain. 2022 Apr 1;35(2):173-182. [Abstract]
- Vascul Pharmacol. 2017 Mar:90:36-43. [Abstract]
- Peptides. 2021 Jan:135:170423. [Abstract]
- Tissue Cell. 2026 Apr:99:103243. [Abstract]
- Biomed Res Int. 2022 Jun 16;2022:1585840. [Abstract]
- Orthop J Sports Med. 2021 Jul 13;9(7):23259671211003982. [Abstract]
- Neuropeptides. 2015 Aug:52:31-7. [Abstract]
- Cell Physiol Biochem. 2017;41(4):1457-1467. [Abstract]
- Biomed Pharmacother. 2025 Aug:189:118344. [Abstract]
- Research Square Print. August 19th, 2022.
- J Tradit Chinese Medical Sci. 21 June 2022.
- Freie Universitt Berlin. 2021 Feb.
- Department of Biology, Chemistry, Pharmacy. 2020 Oct.
Customer Validation & Images
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In Vivo Efficacy Study
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Histological Imaging/Staining
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Flow Cytometry
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ELISA
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In Vivo Efficacy Study
Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SK-N-MC | EC50 |
0.026 nM
Compound: 1, BIBN-4096BS
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Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of alpha-CGRP-induced c-AMP formation after 15 mins by radioimmunoassay
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[PMID: 24794104] |
| SK-N-MC | IC50 |
0.004 μM
Compound: BIBN4096
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Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
Antagonist activity at CGRP receptor in human SK-N-MC cells assessed as inhibition of CGRP-stimulated cAMP production preincubated for 30 mins followed by CGRP addition measured after 3 hrs by beta-lactamase reporter gene-based FRET assay
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[PMID: 24405707] |
| SK-N-MC | IC50 |
0.02 nM
Compound: 1, BIBN-4096
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Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
Displacement of [125I]CGRP from CGRP receptor in human SK-N-MC cells
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[PMID: 22732695] |
Olcegepant possesses higher affinity for the human CGRP receptor than the endogenous ligand CGRP and 150-fold higher affinity compared to the peptidic antagonist CGRP8-37. Olcegepant reverses CGRP-mediated vasodilation in human cerebral vessels and inhibits neurogenic vasodilation in a surrogate animal model of migraine pathophysiology[1]. Olcegepant (BIBN4096BS) is extremely potent at primate CGRP receptors exhibiting an affinity (Ki) for human CGRP receptors of 14.4±6.3 (n=4) pM[2]. Several lines of evidence suggest that a calcitonin-gene related peptide (CGRP) receptor antagonist may serve as a novel abortive migraine treatment. Olcegepant (BIBN4096BS) exhibits competitive antagonism at the CGRP receptor present in SK-N-MC cells. Isolated human cerebral, coronary, and omental arteries are studied with a sensitive myograph technique. CGRP induces a concentration-dependent relaxation that is antagonized by Olcegepant in a competitive manner[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 204697-65-4
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Appearance Solid
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Molecular Weight 869.65
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Formel C38H47Br2N9O5
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Color White to off-white
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SMILES
O=C1N(CC2=C(N1)C=CC=C2)C3CCN(C(N[C@@H](C(N[C@H](C(N4CCN(C5=CC=NC=C5)CC4)=O)CCCCN)=O)CC6=CC(Br)=C(C(Br)=C6)O)=O)CC3
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Synonyms
BIBN-4096; BIBN 4096BS
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (45)
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Journal Impact Factor
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Most Recent
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Nat Med
Implant-derived magnesium induces local neuronal production of CGRP to improve bone-fracture healing in rats. [Abstract]2016 Oct;22(10):1160-1169. PMID: 27571347
Olcegepant purchased from MedChemExpress. Usage Cited in: Nat Med. 2016 Oct;22(10):1160-1169. [Abstract]
In vivo imaging (by IVIS200 system) of different organs in a rat 2 weeks after injections of Cy5‐labeled Olcegepant (BIBN4096BS, BIBN, 750 µg/mL, 100 µL, pH 6.0, every other day) , a CGRP receptor antagonist, into left femur.
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Cell
2026 May 19:S0092-8674(26)00505-2. PMID: 42161272 -
Cell
Innervation of nociceptor neurons in the spleen promotes germinal center responses and humoral immunity. [Abstract]2024 Jun 6;187(12):2935-2951.e19. PMID: 38772371
Olcegepant purchased from MedChemExpress. Usage Cited in: Cell. 2024 Jun 6;187(12):2935-2951.e19. [Abstract]
Representative pseudocolor plots (L) and summary data (M) of proportions of splenic GC B cells and SPPCs 13 days after NP-KLH immunization in mice i.p. injected with vehicle or Olcegepant (BIBN4096, 5 mg/kg) every other day. n = 17 mice per group.
Olcegepant purchased from MedChemExpress. Usage Cited in: Cell. 2024 Jun 6;187(12):2935-2951.e19. [Abstract]
ELISA titration curves of NP-specific IgG antibodies on day 13 post NP-KLH immunization in mice i.p. injected with vehicle or Olcegepant (BIBN4096, 5 mg/kg) every other day. n = 12 mice per group.
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Adv Sci (Weinh)
Bioinspired Engineering of Streamlined Skeletal Interoception: Neural Bioprinted Piezoelectric Scaffolds for Neuro-Vascularized Bone Regeneration. [Abstract]2026 Apr;13(21):e24181. PMID: 41691467 -
Adv Sci (Weinh)
Staphylococcus Aureus Tames Nociceptive Neurons to Suppress Synovial Macrophage Responses for Sustained Infection in Septic Arthritis. [Abstract]2025 Apr;12(14):e2409251. PMID: 39960341
Olcegepant purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Apr;12(14):e2409251. [Abstract]
Typical micro‐CT images of knee joints on the 28th day after S. aureus infection in vehicle and Olcegepant (BIBN4096, 5 µg/5 µL; intra-articular injection into the knee joint 2 h before infection; once weekly) treated mice (left) and the differences in tibial epiphyseal volume between the two groups (right). n = 5 mice/group. (Scale bar: 500 µm).
Olcegepant purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Apr;12(14):e2409251. [Abstract]
Olcegepant (BIBN4096, 5 µg/5 µL; intra-articular injection into the knee joint 2 h before infection; once weekly).Typical H&E-stained images of knee joints (left) and scores based on H&E staining that show differences in synovial and bone damage between the two groups on the 28th day after S. aureus infection (right). n = 8 mice/group (Scale bar: 500 µm).
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Adv Sci (Weinh)
Sensory Nerve Regulation via H3K27 Demethylation Revealed in Akermanite Composite Microspheres Repairing Maxillofacial Bone Defect. [Abstract]2024 Aug;11(30):e2400242. PMID: 38874525 -
Adv Sci (Weinh)
Implantable Electrical Stimulation at Dorsal Root Ganglions Accelerates Osteoporotic Fracture Healing via Calcitonin Gene-Related Peptide. [Abstract]2021 Oct 28;e2103005. PMID: 34708571 -
J Orthop Translat
Talin1 loss activates DRG neurons to accelerate bone remodeling and fracture healing in mice. [Abstract]2026 May 8:58:101113. PMID: 42169959 -
Small Methods
Wireless Optogenetic Targeting Nociceptors Helps Host Cells Win the Competitive Colonization in Implant-Associated Infections. [Abstract]2024 Dec;8(12):e2400216. PMID: 39087367 -
J Headache Pain
Differential expression of components of the CGRP-receptor family in human coronary and human middle meningeal arteries: functional implications. [Abstract]2024 Oct 10;25(1):176. PMID: 39390360 -
J Headache Pain
2024 Aug 21;25(1):136. PMID: 39169303 -
J Headache Pain
2022 Sep 30;23(1):128. PMID: 36180824 -
J Headache Pain
Calcitonin gene-related peptide receptor antagonist BIBN4096BS regulates synaptic transmission in the vestibular nucleus and improves vestibular function via PKC/ERK/CREB pathway in an experimental chronic migraine rat model. [Abstract]2022 Mar 8;23(1):35. PMID: 35260079 -
Cell Rep
SETDB2-mediated transcriptional repression of IDE in sensory neurons promotes migraine-like pain behaviors in mice. [Abstract]2026 Mar 24;45(4):117201. PMID: 41880325 -
Cell Rep
ILC2-derived CGRP triggers acute inflammation and nociceptive responses in bacterial cystitis. [Abstract]2024 Oct 15;43(10):114859. PMID: 39412984 -
Br J Pharmacol
Naringenin relieves paclitaxel-induced pain by suppressing calcitonin gene-related peptide signalling and enhances the anti-tumour action of paclitaxel. [Abstract]2024 Sep;181(17):3136-3159. PMID: 38715438 -
J Invest Dermatol
Thromboxane-Induced α-CGRP Release from Peripheral Neurons Is an Essential Positive Feedback Loop in Capsaicin-Induced Neurogenic Inflammation. [Abstract]2019 Mar;139(3):656-664. PMID: 30612974 -
Biochem Pharmacol
Calcitonin gene-related peptide/protein kinase A: A novel pathway to regulate patency of ductus arteriosus. [Abstract]2026 Jun:248:117840. PMID: 41724283 -
Cell Mol Life Sci
Sensory nerves drive migration of dental pulp stem cells via the CGRP-Ramp1 axis in pulp repair. [Abstract]2024 Aug 28;81(1):373. PMID: 39196292 -
Int Endod J
Sensory nerves, but not sympathetic nerves, promote reparative dentine formation after dentine injury via CGRP-mediated angiogenesis: An in vivo study. [Abstract]2024 Jan;57(1):37-49. PMID: 37874659 -
Cephalalgia
Sex differences in CGRP-induced vasodilation of human middle meningeal arteries but not human coronary arteries: implications for migraine. [Abstract]2024 Jul;44(7):3331024241254088. PMID: 39043230 -
Cephalalgia
No additive effect of combining sumatriptan and olcegepant in the GTN mouse model of migraine. [Abstract]2021 Mar;41(3):329-339. PMID: 33059476 -
Cephalalgia
2020 Aug;40(9):924-934. PMID: 32223300 -
Cephalalgia
Targeting CGRP via receptor antagonism and antibody neutralisation in two distinct rodent models of migraine-like pain. [Abstract]2019 Dec;39(14):1827-1837. PMID: 31288556 -
Int Immunopharmacol
Calcitonin gene-related peptide-modulated macrophage phenotypic alteration regulates angiogenesis in early bone healing. [Abstract]2024 Mar 30:130:111766. PMID: 38452411 -
Int J Mol Sci
CGRP Signaling via CALCRL Increases Chemotherapy Resistance and Stem Cell Properties in Acute Myeloid Leukemia. [Abstract]2019 Nov 20;20(23):5826. PMID: 31756985 -
Invest Ophthalmol Vis Sci
Corneal Nerves Promote Alkali Burn Repair by Modulating Macrophages and Neutrophils via Calcitonin Gene-Related Peptide. [Abstract]2026 Apr 1;67(4):60. PMID: 42041175 -
Invest Ophthalmol Vis Sci
CGRP/TSP1 Signaling Dampens Corneal Inflammation and Fibrosis by Targeting A2M During Corneal Stromal Wound Healing. [Abstract]2026 Jan 5;67(1):10. PMID: 41533912 -
Sci Rep
Peripheral N-methyl-D-aspartate receptor activation contributes to monosodium glutamate-induced headache but not nausea behaviours in rats. [Abstract]2022 Aug 16;12(1):13894. PMID: 35974090 -
Sci Rep
Cortical spreading depolarisation-induced facial hyperalgesia, photophobia and hypomotility are ameliorated by sumatriptan and olcegepant. [Abstract]2020 Jul 10;10(1):11408. PMID: 32651400 -
Sci Rep
A unique inbred rat strain with sustained cephalic hypersensitivity as a model of chronic migraine-like pain. [Abstract]2018 Jan 30;8(1):1836. PMID: 29382888 -
Front Cell Neurosci
Paralogs of the Calcium-Dependent Activator Protein for Secretion Differentially Regulate Synaptic Transmission and Peptide Secretion in Sensory Neurons. [Abstract]2018 Sep 11:12:304. PMID: 30254567 -
Korean J Pain
Anti-nociceptive effects of dual neuropeptide antagonist therapy in mouse model of neuropathic and inflammatory pain. [Abstract]2022 Apr 1;35(2):173-182. PMID: 35354680 -
Vascul Pharmacol
Binding and functional pharmacological characteristics of gepant-type antagonists in rat brain and mesenteric arteries. [Abstract]2017 Mar:90:36-43. PMID: 28192258 -
Peptides
Neuronal calcitonin gene-related peptide promotes prostate tumor growth in the bone microenvironment. [Abstract]2021 Jan:135:170423. PMID: 33086087 -
Tissue Cell
Sensory neuron TRPV1-mediated macrophage polarization and immune response regulate dental implant osseointegration. [Abstract]2026 Apr:99:103243. PMID: 41297248 -
Biomed Res Int
Neural Peptide α-CGRP Coregulated Angiogenesis and Osteogenesis via Promoting the Cross-Talk between Mesenchymal Stem Cells and Endothelial Cells. [Abstract]2022 Jun 16;2022:1585840. PMID: 35757476 -
Orthop J Sports Med
Calcitonin Gene-Related Peptide Influences Bone-Tendon Interface Healing Through Osteogenesis: Investigation in a Rabbit Partial Patellectomy Model. [Abstract]2021 Jul 13;9(7):23259671211003982. PMID: 34345631 -
Neuropeptides
Periodontal CGRP contributes to orofacial pain following experimental tooth movement in rats. [Abstract]2015 Aug:52:31-7. PMID: 26164378 -
Cell Physiol Biochem
NPY and CGRP Inhibitor Influence on ERK Pathway and Macrophage Aggregation during Fracture Healing. [Abstract]2017;41(4):1457-1467. PMID: 28315869 -
Biomed Pharmacother
α6GABAA receptor positive allosteric modulators targeting trigeminal ganglia for preventing and aborting chronic periorbital allodynia and cephalic pain in both sexes: A mechanistic and comparative preclinical study. [Abstract]2025 Aug:189:118344. PMID: 40652726 -
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Lösungsmittel & Löslichkeit
DMSO : ≥ 50 mg/mL (57.49 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
1M HCl : 50 mg/mL (57.49 mM; ultrasonic and adjust pH to 1 with HCl)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 1% DMSO 99% Saline
Solubility: 0.5 mg/mL (0.57 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
125I-hCGRP is used as the radioligand. The incubation buffer contained (in mM): Tris 50, NaCl 150, MgCl25 and EDTA 1, (ethylene diamine tetra-acetic acid) pH 7.4. Membrane homogenates are incubated for 180 min at room temperature with 50 pM 125I -hCGRP and increasing concentrations of Olcegepant (BIBN4096BS). The incubation is terminated by filtration through GF/B glass fibre filters using a cell harvester. The protein-bound radioactivity is determined in a gamma counter. The nonspecific binding is defined as radioactivity bound in the presence of 1 μM CGRP. The IC50 values are obtained by non-linear regression analysis on the basis of a one binding site model [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cells are washed with phosphate-buffered saline then pre-incubated with 300 μM isobutylmethylxanthine in serum-free MEM for 30 min at 37 °C α-CGRP-(S-37) or Olcegepant (BIBN4096BS) is added and the cells are incubated for 10 min before the addition of CGRP. The incubation is continued for another 15 min, then the cells are washed with PBS and processed for cAMP determination. Maximal stimulation over basal is defined by using 100 nM CGRP. Dose–response curves are generated by using Prism[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats are treated acutely with Olcegepant (0.3, 0.6, and 0.9 mg/kg, intravenously [i.v.] in a tail vein), GR-85548A (0.1 and 0.3 mg/kg subcutaneously [s.c.]), or their respective vehicle. For combined treatment, Olcegepant (0.3 mg/kg, i.v.) is administered 30 minutes before GR-85548A (0.1 mg/kg, s.c.). The doses and routes of administration are based on previous reports.
For subchronic treatment, CCI-ION and sham-operated rats are injected twice per day for 4 days (at 10 am and 6 pm) with Olcegepant (0.6 mg/kg, i.v.) or its vehicle, starting on the 15th day after ligature. A further injection of Olcegepant (0.6 mg/kg, i.v.) or vehicle is performed at 10 am the subsequent day (19th day after ligature), just before von Frey filament testing.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (282 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Rudolf K, et al. 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]carbonyl]-D-tyrosyl]-l-lysyl]-4-(4-pyridinyl)piperazine: the first CGRP antagonist for clinical trials in acute migraine. J Med Chem. 2005 Sep 22;48(19):5921-31. [Content Brief]
[2]. Doods H, et al. Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br J Pharmacol. 2000 Feb;129(3):420-3. [Content Brief]
[3]. Edvinsson L, et al. Effect of the CGRP receptor antagonist BIBN4096BS in human cerebral, coronary and omentalarteries and in SK-N-MC cells. Eur J Pharmacol. 2002 Jan 2;434(1-2):49-53. [Content Brief]
[4]. Sixt ML, et al. Calcitonin gene-related peptide receptor antagonist Olcegepant acts in the spinal trigeminal nucleus. Brain. 2009 Nov;132(Pt 11):3134-41. [Content Brief]
[5]. Michot B, et al. Differential effects of calcitonin gene-related peptide receptor blockade by Olcegepant on mechanical allodynia induced by ligation of the infraorbital nerve vs the sciatic nerve in the rat. Pain. 2012 Sep;153(9):1939-48. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / 1M HCl | 1 mM | 1.1499 mL | 5.7494 mL | 11.4989 mL | 28.7472 mL |
| 5 mM | 0.2300 mL | 1.1499 mL | 2.2998 mL | 5.7494 mL | |
| 10 mM | 0.1150 mL | 0.5749 mL | 1.1499 mL | 2.8747 mL | |
| 15 mM | 0.0767 mL | 0.3833 mL | 0.7666 mL | 1.9165 mL | |
| 20 mM | 0.0575 mL | 0.2875 mL | 0.5749 mL | 1.4374 mL | |
| 25 mM | 0.0460 mL | 0.2300 mL | 0.4600 mL | 1.1499 mL | |
| 30 mM | 0.0383 mL | 0.1916 mL | 0.3833 mL | 0.9582 mL | |
| 40 mM | 0.0287 mL | 0.1437 mL | 0.2875 mL | 0.7187 mL | |
| 50 mM | 0.0230 mL | 0.1150 mL | 0.2300 mL | 0.5749 mL |
Olcegepant Related Classifications
HY-10095 Related Classifications
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