PDE10A-IN-2 hydrochloride
Based on 1 Customer Validation
PDE10A-IN-2 hydrochloride is a potent, highly selective and orally active phosphodiesterase 10A (PDE10A) inhibitor with an IC50 of 2.8 nM. PDE10A-IN-2 hydrochloride shows selectivity of >3500-fold against other PDE subtypes. PDE10A-IN-2 hydrochloride can be used for pulmonary arterial hypertension (PAH) research.
For research use only. We do not sell to patients.
- Purity : 98.43%
- Formula: C33H38Cl3N5O
- Molecular Weight:627.05
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PDE10A 2.8 nM (IC50) |
In Vivo
In Sprague-Dawley rats, the pharmacokinetic study of PDE10A-IN-2 hydrochloride (compound 14 3HCL; 10 mg/kg) shows the oral bioavailability up to ～50%, and the T1/2 is 5.2 hours (p.o.), and the Cmax is 272 ng/mL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wister rats (6 weeks, 160-180 g) injected with Monocrotaline[1]
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Dosage:2.5 mg/kg
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Administration:Oral administration; daily; for 3 weeks
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Result:Decreased symptoms of the pulmonary arterial hypertension (PAH) rats.
Chemical Information
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Appearance Solid
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Molecular Weight 627.05
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Formula C33H38Cl3N5O
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Color White to yellow
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SMILES
CN1CCN(CCCOC2=CC(N3C(/C=C/C4=C5N=CC=CC5=CC=C4)=NC6=CC(C)=CC=C36)=CC=C2)CC1.[H]Cl.[H]Cl.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (159.48 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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 (sealed storage, away from moisture). 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 | 1.5948 mL | 7.9738 mL | 15.9477 mL | 39.8692 mL |
| 5 mM | 0.3190 mL | 1.5948 mL | 3.1895 mL | 7.9738 mL | |
| 10 mM | 0.1595 mL | 0.7974 mL | 1.5948 mL | 3.9869 mL | |
| 15 mM | 0.1063 mL | 0.5316 mL | 1.0632 mL | 2.6579 mL | |
| 20 mM | 0.0797 mL | 0.3987 mL | 0.7974 mL | 1.9935 mL | |
| 25 mM | 0.0638 mL | 0.3190 mL | 0.6379 mL | 1.5948 mL | |
| 30 mM | 0.0532 mL | 0.2658 mL | 0.5316 mL | 1.3290 mL | |
| 40 mM | 0.0399 mL | 0.1993 mL | 0.3987 mL | 0.9967 mL | |
| 50 mM | 0.0319 mL | 0.1595 mL | 0.3190 mL | 0.7974 mL | |
| 60 mM | 0.0266 mL | 0.1329 mL | 0.2658 mL | 0.6645 mL | |
| 80 mM | 0.0199 mL | 0.0997 mL | 0.1993 mL | 0.4984 mL | |
| 100 mM | 0.0159 mL | 0.0797 mL | 0.1595 mL | 0.3987 mL |
PDE10A-IN-2 hydrochloride Related Classifications
HY-131973 Related Classifications
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