Free shipping on all orders over $ 500

PD 102807 

Cat. No. M29495
PD 102807  Structure
Size Price Availability Quantity
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

PD 102807 is a M4 muscarinic receptor antagonist with an IC50 of 90.7 nM. PD 102807 inhibits M1, M2, M3, M5 muscarinic receptor with IC50s of 6558.7, 3440.7, 950.0, and 7411.7 nM, respectively. Antidyskinetic effect.

Chemical Information
Molecular Weight 392.45
Formula C23H24N2O4
CAS Number 23062-91-1
Form Solid
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ikunobu Muramatsu, et al. J Neurochem. Novel regulatory systems for acetylcholine release in rat striatum and anti-Alzheimer's disease drugs

[2] Michael Marks, et al. Br Med Bull. Yaws

[3] Michael Marks, et al. Int J STD AIDS. Yaws

[4] Eric Tompkins, et al. Am J Respir Cell Mol Biol. PD 102807 Induces M3 mAChR-Dependent GRK-/Arrestin-Biased Signaling in Airway Smooth Muscle Cells

[5] M C Olianas, et al. Life Sci. PD 102807, a novel muscarinic M4 receptor antagonist, discriminates between striatal and cortical muscarinic receptors coupled to cyclic AMP

Related AChR/AChE Products
Zanapezil

Zanapezil (TAK-147) is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor, it has potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM).

Tacrine

Tacrine is a potent acetylcholinesterse (AChE) inhibitor (IC50=109 nM), also acting as a CYP1A2 substrate agent.

THRX-160209

THRX-160209 is a potent antagonist at the M(2) muscarinic acetylcholine (ACh) receptor subtype that was designed using a multivalent strategy, simultaneously targeting the orthosteric site and a nearby site known to bind allosteric ligands.

Catestatin

Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide.

α-Conotoxin MII

α-Conotoxin MII (α-CTxMII), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM.

  Catalog
Abmole Inhibitor Catalog




Keywords: PD 102807  supplier, AChR/AChE, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.