Vazegepant
Based on 1 publication(s) in Google Scholar
Vazegepant (Zavegepant; BHV-3500) is an orally active calcitonin gene-related peptide (CGRP) receptor antagonist with a Ki of 23 pM for human CGRP receptor and an EC50 of 880 pM for reversing CGRP-induced vasodilation in human intracranial arteries. Vazegepant can block CGRP-mediated vasodilation in the trigeminal vascular system and inhibit neuronal circuit sensitization. Vazegepant can be used in migraine-related research.
For research use only. We do not sell to patients.
- Purity: 99.54%
- CAS No.: 1337918-83-8
- Formula: C36H46N8O3
- Molecular Weight:638.80
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Vazegepant
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Biological Activity
Description
In Vitro
Vazegepant (Zavegepant) exhibits fully competitive binding activity to the human CGRP receptor expressed endogenously in the SKN-MC cell membrane, with a Ki of 23 pM, which is more than 10,000 times more selective than the adrenal medullary receptor 1/2, calcitonin receptor, and amyloid receptor 1/3; and can strongly and completely reverse the vasodilatory effect induced by CGRP in isolated human intracranial arterial tissue, with an EC50 of 880 pM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Vazegepant exhibited low oral bioavailability in monkey (F = 0.3%), mouse (F = 1.4%), and rat (F = 1.7%) animal models[1].
Vazegepant (nasal administration) was rapidly absorbed in a rabbit model, with a Tmax of 15-20 min[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1337918-83-8
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Appearance Solid
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Molecular Weight 638.80
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Formula C36H46N8O3
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Color White to off-white
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SMILES
O=C(N1CCC(C2=CC3=C(NC2=O)C=CC=C3)CC1)N[C@H](CC4=CC5=C(NN=C5)C(C)=C4)C(N6CCN(C7CCN(C)CC7)CC6)=O
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Synonyms
Zavegepant; BHV-3500
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (78.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (protect from light). 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (284 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)
References
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 (protect from light). 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 | 1 mM | 1.5654 mL | 7.8272 mL | 15.6544 mL | 39.1359 mL |
| 5 mM | 0.3131 mL | 1.5654 mL | 3.1309 mL | 7.8272 mL | |
| 10 mM | 0.1565 mL | 0.7827 mL | 1.5654 mL | 3.9136 mL | |
| 15 mM | 0.1044 mL | 0.5218 mL | 1.0436 mL | 2.6091 mL | |
| 20 mM | 0.0783 mL | 0.3914 mL | 0.7827 mL | 1.9568 mL | |
| 25 mM | 0.0626 mL | 0.3131 mL | 0.6262 mL | 1.5654 mL | |
| 30 mM | 0.0522 mL | 0.2609 mL | 0.5218 mL | 1.3045 mL | |
| 40 mM | 0.0391 mL | 0.1957 mL | 0.3914 mL | 0.9784 mL | |
| 50 mM | 0.0313 mL | 0.1565 mL | 0.3131 mL | 0.7827 mL | |
| 60 mM | 0.0261 mL | 0.1305 mL | 0.2609 mL | 0.6523 mL |
Vazegepant Related Classifications
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