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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.52%
- CAS No.: 2649803-05-2
- Formule: C23H27F3N4O
- Masse moléculaire:432.48
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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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.
Chemical Information
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CAS No. 2649803-05-2
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Appearance Solid
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Masse moléculaire 432.48
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2659 KB)
Références
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 Related Classifications
HY-141711 Related Classifications
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