2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. PDE10A-IN-2 hydrochloride

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.

PDE10A-IN-2 hydrochloride Chemical Structure

PDE10A-IN-2 hydrochloride Chemical Structure

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Description

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[1].

IC50 & Target[1]

PDE10A

2.8 nM (IC50)

In Vivo

PDE10A-IN-2 hydrochloride (compound 14 3HCL; 2.5 mg/kg; oral administration; daily; for 3 weeks) treatment decreases the typical symptoms of PAH in rats[1].
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.

Animal Model: Wister rats (6 weeks, 160-180 g) injected with Monocrotaline[1]
Dosage: 2.5 mg/kg
Administration: Oral administration; daily; for 3 weeks
Result: Decreased symptoms of the pulmonary arterial hypertension (PAH) rats.
Molecular Weight

627.05

Formula

C33H38Cl3N5O
Appearance

Solid

Color

White to yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5948 mL 7.9738 mL 15.9477 mL
5 mM 0.3190 mL 1.5948 mL 3.1895 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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
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PDE10A-IN-2 hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PDE10A-IN-2Phosphodiesterase (PDE)PDE10APAHoralInhibitorinhibitorinhibit

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