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Submit ReviewPD 102807
Description: Selective M4 antagonist
Chemical Name: 3,6a,11,14-Tetrahydro-9-methoxy-2-methyl-(12H)-isoquino[1,2-b]pyrrolo[3,2-f][1,3]benzoxazine-1-carboxylic acid, ethyl ester
Purity: ≥98% (HPLC)
Biological Activity
Selective M4 muscarinic receptor antagonist. IC50 values are 91, 6559, 3441, 950 and 7412 nM for human M4, M1, M2, M3, and M5 receptors respectively. Promotes self-renewal of erythroid progenitors.
Compound Libraries
PD 102807 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 392.45 |
| Formula | C23H24N2O4 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 23062-91-1 |
| PubChem ID | 4995951 |
| InChI Key | VDDUJINYXKGZLV-UHFFFAOYSA-N |
| Smiles | CCOC(=O)C1=C(C)NC2=CC=C3OC4N(CCC5=CC(OC)=CC=C45)CC3=C12 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 39.24 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 392.45. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.55 mL | 12.74 mL | 25.48 mL |
| 5 mM | 0.51 mL | 2.55 mL | 5.1 mL |
| 10 mM | 0.25 mL | 1.27 mL | 2.55 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.51 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Augelli-Szafran et al (1998) Identification and characterization of m4 selective muscarinic antagonists. Bioorg.Med.Chem.Lett. 8 1991 PMID: 9873472
Bohme et al (2002) Synthesis and pharmacology of benzoxazines as highly selective antagonists at M4 muscarinic receptors. J.Med.Chem. 45 3094 PMID: 12086495
Kitaichi et al (1999) A novel muscarinic M4 receptor antagonist provides further evidence of an autoreceptor role for the muscarinic M2 receptor sub-type. Eur.J.Pharmacol. 383 53 PMID: 10556681
Trivedi et al (2019) Muscarinic acetylcholine receptor regulates self-renewal of early erythroid progenitors. Sci.Transl.Med. 11 PMID: 31554738
If you know of a relevant reference for PD 102807, please let us know.
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Keywords: PD 102807, PD 102807 supplier, Selective, M4, antagonists, antagonism, Muscarinic, Receptors, Acetylcholine, ACh, PD102807, expansion, self-renewal, hematopoietic, progenitors, burst-forming, units, erythroid, BFU-E, mAChR4, Stem, Cell, Proliferation, 1671, Tocris Bioscience
4 Citations for PD 102807
Citations are publications that use Tocris products. Selected citations for PD 102807 include:
Trivedi et al (2019) Muscarinic acetylcholine receptor regulates self-renewal of early erythroid progenitors. Sci.Transl.Med. 11 PMID: 31554738
Solanki et al (2007) Cholinergic innervation of the guinea-pig isolated vas deferens. Naunyn Schmiedebergs Arch Pharmacol 376 265 PMID: 17992517
Zhu et al (2017) Impairments of spatial memory in an Alzheimer's disease model via degeneration of hippocampal cholinergic synapses. Nat Commun 8 1676 PMID: 29162816
Thomson et al (2017) Cell-Type-Specific Translation Profiling Reveals a Novel Strategy for Treating Fragile X Syndrome. Neuron 95 550 PMID: 28772121
Do you know of a great paper that uses PD 102807 from Tocris? Please let us know.
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