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PD-102807

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Catalog No. T23124Cas No. 23062-91-1

PD-102807 is a selective and competitive M4 muscarinic receptor antagonist (IC50 = 90.7 nM), with IC50 values of 950–7412 nM for M1, M2, M3, and M5 receptors, and can be used for Parkinson's disease research, as well as to inhibit airway smooth muscle (ASM) contraction.

PD-102807

PD-102807

🥰Excellent
Purity: 98.90%
Catalog No. T23124Cas No. 23062-91-1
PD-102807 is a selective and competitive M4 muscarinic receptor antagonist (IC50 = 90.7 nM), with IC50 values of 950–7412 nM for M1, M2, M3, and M5 receptors, and can be used for Parkinson's disease research, as well as to inhibit airway smooth muscle (ASM) contraction.
Pack SizePriceAvailabilityQuantity
1 mg$52In Stock
5 mg$123In Stock
10 mg$197In Stock
25 mg$332In Stock
50 mg$496In Stock
100 mg$693In Stock
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Purity:98.90%
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Product Introduction

Bioactivity
Description
PD-102807 is a selective and competitive M4 muscarinic receptor antagonist (IC50 = 90.7 nM), with IC50 values of 950–7412 nM for M1, M2, M3, and M5 receptors, and can be used for Parkinson's disease research, as well as to inhibit airway smooth muscle (ASM) contraction.
In vitro
Methods:
To evaluate the antagonistic selectivity of PD-102807 toward different subtypes of muscarinic receptors, [^35S]-GTPγS binding assays were performed to measure its inhibitory effect on agonist-induced G protein activation at M1, M2, M3, and M4 receptors. The pK_B values for each receptor subtype were determined to assess its antagonistic potency and selectivity.[1]
Results:
PD-102807 significantly inhibited M4 receptor-mediated G protein activation, with a pK_B value of 7.40, which was substantially higher than its potency at M1 (5.60), M2 (5.88), and M3 (6.39) receptors, indicating strong selectivity for the M4 receptor.
In vivo
Methods:
To evaluate the effects of PD-102807 on L-DOPA-induced abnormal involuntary movements (AIMs) and neurotransmitter release, male Sprague-Dawley rats were used. A 3 μM concentration of PD-102807 was perfused starting 40 minutes before administration of L-DOPA and benserazide, and microdialysis was used to measure GABA and glutamate (Glu) levels in the substantia nigra pars reticulata (SNr) and striatum.[2]
Results:
PD-102807 significantly inhibited the L-DOPA-induced increases in GABA and Glu levels in the SNr and striatum, and reduced the axial-limb-orolingual (ALO) AIMs score from 70.75 ± 5.64 to 25.38 ± 6.64, effectively alleviating abnormal involuntary movements.
Chemical Properties
Molecular Weight392.45
FormulaC23H24N2O4
Cas No.23062-91-1
SmilesO=C(OCC)C=1C=2C(=CC=C3OC4C5=CC=C(OC)C=C5CCN4CC32)NC1C
Relative Density.1.34 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 120 mg/mL (305.77 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.5481 mL12.7405 mL25.4810 mL127.4048 mL
5 mM0.5096 mL2.5481 mL5.0962 mL25.4810 mL
10 mM0.2548 mL1.2740 mL2.5481 mL12.7405 mL
20 mM0.1274 mL0.6370 mL1.2740 mL6.3702 mL
50 mM0.0510 mL0.2548 mL0.5096 mL2.5481 mL
100 mM0.0255 mL0.1274 mL0.2548 mL1.2740 mL

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