2. Metabolic Enzyme/Protease Neuronal Signaling GPCR/G Protein Membrane Transporter/Ion Channel
  3. Phosphodiesterase (PDE) mAChR Potassium Channel
  4. CPL500036

CPL500036 is an orally active, blood-brain barrier permeable phosphodiesterase 10A (PDE10A) inhibitor with IC50 values of 1 nM (Reference 1) and 35 nM (Reference 2). CPL500036 acts as a negative allosteric modulator of the M2 muscarinic receptor with an IC50 of 9.2 μM. CPL500036 alters cyclic nucleotide levels in basal ganglia circuits, inhibits the hydrolysis of cAMP and cGMP, and suppresses hERG potassium channel tail currents. CPL500036 induces catalepsy in rats and reverses injury-induced contralateral forelimb use impairment. CPL500036 can be used in research related to schizophrenia, Parkinson's disease, and levodopa-induced dyskinesia.

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CPL500036

CPL500036 Chemical Structure

CAS No. : 1829530-11-1

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CPL500036 Related Antibodies

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mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

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Description

CPL500036 is an orally active, blood-brain barrier permeable phosphodiesterase 10A (PDE10A) inhibitor with IC50 values of 1 nM (Reference 1) and 35 nM (Reference 2). CPL500036 acts as a negative allosteric modulator of the M2 muscarinic receptor with an IC50 of 9.2 μM. CPL500036 alters cyclic nucleotide levels in basal ganglia circuits, inhibits the hydrolysis of cAMP and cGMP, and suppresses hERG potassium channel tail currents. CPL500036 induces catalepsy in rats and reverses injury-induced contralateral forelimb use impairment. CPL500036 can be used in research related to schizophrenia, Parkinson's disease, and levodopa-induced dyskinesia[1][2].

IC50 & Target[1][2]

PDE10A

1 nM (IC50)

PDE10A

35 nM (IC50)

In Vitro

CPL500036 (0.1-10 μM; 5 min) inhibits hERG tail current in hERG-HEK-293 transfected cells with an IC25 of 3.2 μM[1].
CPL500036 (0.0457-100 μM; 14 days) does not affect key cardiac spheroid health parameters up to 100 μM, but impairs DNA structure with an IC50 of 37.4 μM in human pluripotent cell-derived 3D cardiac spheroids[1].
CPL500036 (8 nM-60 μM; 72 h) is not cytotoxic at concentrations up to 60 μM in NCI-H1299, HepG2, and SH-SY5Y cell lines[1].

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

CPL500036 Related Antibodies
Parmacokinetics
Species Dose Route Cmax Tmax (Plasma) AUC0-24 T1/2 (Plasma) Cmax (Brain) Tmax (Brain)
Rat[1] 3 mg/kg p.o. 237.8 ng/mL 5.8 h 1,618.0 ng·h/mL 6.4 h 94.3 ng/mL 6.8 h
Dog[1] 1.5 mg/kg p.o. 98.3 ng/mL 1.3 h 199.4 ng·h/mL 2.1 h / /
In Vivo

CPL500036 (0.15-2 mg/kg; p.o.; single administration) induces dose-dependent catalepsy in male Sprague-Dawley rats[1].
CPL500036 (0.1-0.3 mg/kg; p.o.; single acute administration combined with Levodopa (HY-N0304)/Benserazide (HY-121275) for 16 consecutive days) dose-dependently improves sensorimotor deficits in 6-hydroxydopamine-lesioned rats[2].

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

Animal Model: Sprague-Dawley (male, ~300 g)[1]
Dosage: 0.15 mg/kg; 0.3 mg/kg; 0.6 mg/kg; 2 mg/kg
Administration: p.o.; single dose
Result: Did not induce catalepsy at 0.15 mg/kg.
Induced a low cataleptogenic effect only at 210 min and 240 min post-administration at 0.3 mg/kg.
Induced catalepsy from 120 min to 240 min post-administration at 0.6 mg/kg, with effect less than positive control haloperidol.
Produced a strong cataleptogenic effect comparable to haloperidol at 2 mg/kg.
Confirmed minimum effective dose (MED) for catalepsy as 0.6 mg/kg via AUC data.
Animal Model: Wistar Han (male, initial body weight 270-300 g, unilateral medial forebrain bundle lesion with 6-hydroxydopamine)[2]
Dosage: 0.1 mg/kg (acute single dose; chronic daily combined with L-DOPA/benserazide); 0.3 mg/kg (acute single dose; chronic daily combined with L-DOPA/benserazide)
Administration: p.o.; single acute dose; daily for 16 days (combined with L-DOPA/benserazide)
Result: Dose-dependently reversed impaired forelimb use in the stepping test after acute administration.
Completely restored forelimb use symmetry in the cylinder test during the second post-dose testing session at 0.3 mg/kg acute dose.
Did not affect vibrissae test deficits or lesion-induced catalepsy at either acute dose.
Significantly improved impaired forelimb performance in the vibrissae test when combined acutely with L-DOPA at 0.1 mg/kg.
Reduced L-DOPA-induced contralateral rotations when combined acutely with L-DOPA at 0.3 mg/kg.
Completely reversed forelimb asymmetry in the vibrissae test after chronic combined treatment at 0.3 mg/kg.
Did not alter L-DOPA's antiparkinsonian effects in the stepping, catalepsy, or rotation tests at either chronic dose.
Significantly improved impaired forelimb use in the stepping test in the OFF phase post-chronic treatment at 0.3 mg/kg combined with L-DOPA compared to lesioned rats.
Molecular Weight

341.37

Formula

C19H15N7
CAS No.
SMILES

CC1=NC=C(C)N2N=C(C3=NC4=NC(C5=CC=CC=C5)=CN4C=C3)N=C21
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CPL500036 Related Classifications

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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:

CPL5000361829530-11-1CPL 500036CPL-500036Phosphodiesterase (PDE)mAChRPotassium ChannelMuscarinic acetylcholine receptorKcsAHepG2basal-ganglia circuitsPDE10AcAMPPhosphodiesterase 10Ahuman muscarinic M2 receptorhuman 3D cardiac spheroidshERG potassium channelcGMPNCI-H1299Inhibitorinhibitorinhibit

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