VU0467485
Based on 1 Customer Validation
VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.29%
- CAS No.: 1451994-10-7
- Formule: C17H17FN4O2S
- Masse moléculaire:360.41
-
Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Activité biologique
|
mAChR4 |
VU0467485 (3 mg/kg; p.o.) treatment displays that the Cmax, AUCo-inf and elimination t1/2 were 1.2 μM, 3.8 μM h and 4.2 hours, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Sprague Dawley rats (amphetamine-induced hyperlocomotion rat model) [1]
-
Dosage:1, 3, 10 mg/kg
-
Administration:Oral administration
-
Result:Dose-dependently reverses AHL.
-
Animal Model:Male sprague Dawley rats[1]
-
Dosage:Oral administration (Pharmacokinetic Analysis)
-
Administration:3 mg/kg
-
Result:The Cmax, AUCo-inf and elimination t1/2 were 1.2 μM, 3.8 μM•h and 4.2 hours, respectively.
Chemical Information
-
CAS No. 1451994-10-7
-
Appearance Solid
-
Masse moléculaire 360.41
-
Formule C17H17FN4O2S
-
Color Light yellow to yellow
-
SMILES
O=C(C1=C(N)C2=C(C)C(C)=NN=C2S1)NCC3=CC=C(OC)C(F)=C3
-
Synonyms
AZ13713945
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 20 mg/mL (55.49 mM; ultrasonic and warming 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
-
Fiche technique (274 KB)
-
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)
-
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 | 2.7746 mL | 13.8731 mL | 27.7462 mL | 69.3654 mL |
| 5 mM | 0.5549 mL | 2.7746 mL | 5.5492 mL | 13.8731 mL | |
| 10 mM | 0.2775 mL | 1.3873 mL | 2.7746 mL | 6.9365 mL | |
| 15 mM | 0.1850 mL | 0.9249 mL | 1.8497 mL | 4.6244 mL | |
| 20 mM | 0.1387 mL | 0.6937 mL | 1.3873 mL | 3.4683 mL | |
| 25 mM | 0.1110 mL | 0.5549 mL | 1.1098 mL | 2.7746 mL | |
| 30 mM | 0.0925 mL | 0.4624 mL | 0.9249 mL | 2.3122 mL | |
| 40 mM | 0.0694 mL | 0.3468 mL | 0.6937 mL | 1.7341 mL | |
| 50 mM | 0.0555 mL | 0.2775 mL | 0.5549 mL | 1.3873 mL |