KVA-D-88
Based on 1 Customer Validation
KVA-D-88 is a blood-brain barrier-permeable PDE4 inhibitor with IC50 values of 140 and 880 nM for PDE4B and PDE4D, respectively. KVA-D-88 induces cAMP accumulation and inhibits neuroactive substance-mediated hyperlocomotion, locomotor sensitization. KVA-D-88 can be used for the research of drug addiction.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.81%
- No. CAS: 2410550-31-9
- Fòrmula: C17H11Cl2F2N3O
- Peso molecular:382.19
-
Almacenamiento:Powder -20°C, 3 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]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
PDE4B 140 nM (IC50) |
PDE4D 880 nM (IC50) |
In Vitro
KVA-D-88 preferentially inhibits the PDE4B isoform over PDE4D in vitro, with an IC50 of 140 nM for PDE4B and 880 nM for PDE4D[1].
KVA-D-88 (1-100000 nM; overnight) induces cAMP accumulation in PDE4B1-transfected HEK293 cells with an EC50 of 0.5 μM in vitro[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6J (male and female; 3 months old for acute locomotion, 10-12 weeks old for self-administration)[1]
-
Dosage:0.5 mg/kg; 1 mg/kg; 2 mg/kg; 2.5 mg/kg; 4 mg/kg; 5 mg/kg; 10 mg/kg
-
Administration:i.p.; single dose, 30 minutes prior to neuroactive substance exposure/sessions
-
Result:Significantly blocked hyperlocomotor activity, with no significant effect on basal locomotor activity.
Significantly blocked locomotor sensitization.
Significantly decreased the number of active nose-pokes.
Chemical Information
-
No. CAS 2410550-31-9
-
Appearance Solid
-
Peso molecular 382.19
-
Fòrmula C17H11Cl2F2N3O
-
Color White to off-white
-
SMILES
O=C(C1=CC2=CC=CN=C2N1C3=CC=C(Cl)C(Cl)=C3)N4CC(F)(F)C4
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 20 mg/mL (52.33 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. 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)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
-
Ficha de datos (277 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)
-
Instrucciones de manejo (2659 KB)
Referencias
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 | 2.6165 mL | 13.0825 mL | 26.1650 mL | 65.4125 mL |
| 5 mM | 0.5233 mL | 2.6165 mL | 5.2330 mL | 13.0825 mL | |
| 10 mM | 0.2616 mL | 1.3082 mL | 2.6165 mL | 6.5412 mL | |
| 15 mM | 0.1744 mL | 0.8722 mL | 1.7443 mL | 4.3608 mL | |
| 20 mM | 0.1308 mL | 0.6541 mL | 1.3082 mL | 3.2706 mL | |
| 25 mM | 0.1047 mL | 0.5233 mL | 1.0466 mL | 2.6165 mL | |
| 30 mM | 0.0872 mL | 0.4361 mL | 0.8722 mL | 2.1804 mL | |
| 40 mM | 0.0654 mL | 0.3271 mL | 0.6541 mL | 1.6353 mL | |
| 50 mM | 0.0523 mL | 0.2616 mL | 0.5233 mL | 1.3082 mL |
KVA-D-88 Related Classifications
HY-139178 Related Classifications
Powered by Bioz