VU6028418
Based on 1 Customer Validation
VU6028418 is a potent, highly selective and orally bioavailable M4 mAChR antagonist with an IC50 of 4.1 nM against hM4.
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: 99.52%
- CAS 番号: 2649803-05-2
- 分子式: C23H27F3N4O
- 分子量:432.48
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
生物活性
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mAChR4 |
In Vivo PK Parameters for VU6028418[1]
| parameter | rat (SD)a |
mouse (CD-1)a |
dog (beagle)a |
| dose (mg/kg) iv/po | 1/10 | 1/3 | 1/3 |
| CLp (mL/min/kg) | 6.1 | 17 | 43 |
| Vss (L/kg) | 6.7 | 10.6 | 8.5 |
| elimination t1/2 (h) | 13 | NC | 15 |
| Cmax (ng/mL) po | 17 000 | 181 | 70 |
| Tmax (h) po | 1.5 | 6.67 | 17 |
| AUC0-inf (ng/mL•h) po | 30 000 | NC | 1100 |
| F (%) po | ≥100 | ≥100 | 86 |
| total brain/total plasma (Kp) | 6.4 | ND | ND |
| unbound brain/unbound plasma (Kp,uu) |
0.61 | ND | ND |
| CSF/plasma unbound (Kp,u) | 0.24 | ND | ND |
a Values represent means from two to three animals. ND = not determined. NC = not calculated; there was insufficient data to define the elimination phase (i.e., Cmax was one of the last three time points).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SD rat, CD-1 mouse and beagle dog[1]
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Dosage:1, 3 and 10 mg/kg
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Administration:Intravenous injection or oral administration (Pharmacokinetic Analysis)
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Result:Showed good pharmacokinetic results.
化学情報
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CAS 番号 2649803-05-2
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性状 Solid
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分子量 432.48
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分子式 C23H27F3N4O
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Color White to off-white
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SMILES
FC1=CC(F)=C(F)C(C2=CC=C(N[C@H]3C[C@@](CN(CC4CCOCC4)C5)([H])[C@@]5([H])C3)N=N2)=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 5.56 mg/mL (12.86 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 60°C; 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. 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.
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 (273 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. 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 | 2.3122 mL | 11.5612 mL | 23.1225 mL | 57.8061 mL |
| 5 mM | 0.4624 mL | 2.3122 mL | 4.6245 mL | 11.5612 mL | |
| 10 mM | 0.2312 mL | 1.1561 mL | 2.3122 mL | 5.7806 mL |
VU6028418 関連分類
HY-141711 関連分類
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