2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. THPP-1

THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species.

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THPP-1

THPP-1 Estructura química

No. CAS : 1257051-63-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO En stock
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Based on 1 publication(s) in Google Scholar

THPP-1 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE THPP-1

Ver todos los productos específicos de isoformas Phosphodiesterase (PDE):

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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Descripciòn

THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species[1].

IC50 & Target

PDE10

 

In Vivo

THPP-1 (0.1-1.0 mg/kg, p.o.) shows novel object recognition in rats[1].
THPP-1 (p.o., 1-30 mg/kg) dose-dependently increases phosphorylation of GluR1 S845 in the rat striatum whereas the total levels of GluR1 in the striatum are not affected. Administration of THPP-1 also results in an associated increase in the pGluR1/GluR1 ratios at all doses examined in this study[1].
THPP-1 (1, 3, 10 mg/kg, p.o.) significantly attenuated the stimulant effects in stimulant-induced motor activity (SIMA) in monkey[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Wistar Hannover rats ranging from 200 to 300 g[1].
Dosage: 0.1-1.0 mg/kg.
Administration: P.O.
Result: Showed novel object recognition.
Animal Model: Eleven monkeyswere surgically implanted with subcutaneous telemetric devices to permit the simultaneous recording of electrocorticogram (ECoG), electrooculogram (EOG), and electromyogram (EMG) activit
Dosage: 1, 3, 10 mg/kg.
Administration: P.O.
Result: Significantly attenuated the stimulant effects in SIMA.
Animal Model: Male Wistar Hannover rats ranging from 200 to 300 g[1].
Dosage: 1-30 mg/kg.
Administration: P.O. (10% Tween 80/90% water) 2 h prior to tissue collection (Pharmacokinetic Analysis).
Result: Dose-dependently increases phosphorylation of GluR1 S845.
Peso molecular

464.90

Fòrmula

C23H21ClN6O3
No. CAS
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=C2C=CC=CN2C=N1)N3CCC4=NC(C5=CC=C(N=C5)Cl)=NC(OCCOC)=C4C3
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvente y solubilidad
In Vitro: 

DMSO : 31.25 mg/mL (67.22 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 2.1510 mL 10.7550 mL 21.5100 mL
5 mM 0.4302 mL 2.1510 mL 4.3020 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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  • Calculadora de dilución

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
Pureza y Documentación
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1510 mL 10.7550 mL 21.5100 mL 53.7750 mL
5 mM 0.4302 mL 2.1510 mL 4.3020 mL 10.7550 mL
10 mM 0.2151 mL 1.0755 mL 2.1510 mL 5.3775 mL
15 mM 0.1434 mL 0.7170 mL 1.4340 mL 3.5850 mL
20 mM 0.1076 mL 0.5378 mL 1.0755 mL 2.6888 mL
25 mM 0.0860 mL 0.4302 mL 0.8604 mL 2.1510 mL
30 mM 0.0717 mL 0.3585 mL 0.7170 mL 1.7925 mL
40 mM 0.0538 mL 0.2689 mL 0.5378 mL 1.3444 mL
50 mM 0.0430 mL 0.2151 mL 0.4302 mL 1.0755 mL
60 mM 0.0359 mL 0.1793 mL 0.3585 mL 0.8963 mL
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THPP-1 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:

THPP-11257051-63-0THPP1THPP 1Phosphodiesterase (PDE)SIMAPDE10AnovelobjectrecognitionInhibitorinhibitorinhibit

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Nombre del producto:
THPP-1
Cat. No.:
HY-117604
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