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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.54%
- CAS 番号: 1337918-83-8
- 分子式: C36H46N8O3
- 分子量:638.80
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保管条件:
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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Vazegepant
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生物活性
製品説明
体外実験
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.
体内実験
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.
化学情報
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CAS 番号 1337918-83-8
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性状 Solid
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分子量 638.80
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分子式 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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別名
Zavegepant; BHV-3500
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
溶剤 & 溶解度
体外:
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
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 関連分類
HY-134992 関連分類
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