AE9C90CB
AE9C90CB is an M3 muscarinic receptor (mAChR) antagonist and M2 muscarinic receptor ligand (human pKi values of 9.9 and 8.6, respectively). AE9C90CB binds to the M3 receptor and produces an insurmountable antagonism of Carbamoylcholine chloride (HY-B1208)-induced bladder strip contraction, thereby inhibiting the elevation of intravesical pressure and salivation, and exhibits functional selectivity for the bladder relative to the salivary glands. AE9C90CB can be used in the study of overactive bladder.
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- CAS No.: 893426-98-7
- Formule: C21H25ClN2O2
- Masse moléculaire:372.89
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
mAChR3 9.9 (pKi) |
mAChR2 8.6 (pKi) |
In Vitro
AE9C90CB (3 h) exhibits high affinity for human recombinant muscarinic M3 receptors (pKi 9.9) with moderate selectivity for M3 over M2 receptors in CHO cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Urethane (1.5 g/kg, i.v.)-anaesthetized rabbit model with bladder catheterization and intravesical pressure recording, challenged with carbachol (1.5 μg/kg, i.a.)[1]
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Dosage:3 μg/kg
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Administration:Intravenous (i.v.) bolus; each dose separated by a 30-min interval
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Result:Effectively inhibited the Carbachol-induced increase in intravesical pressure, with an ED50 of 3 μg/kg; ED50 for salivation = 16 μg/kg; bladder versus salivary gland selectivity = 5.4.
Chemical Information
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CAS No. 893426-98-7
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Masse moléculaire 372.89
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Formule C21H25ClN2O2
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SMILES
[H][C@@]1(CNC2)[C@@]2([H])[C@H]1CN(C)C(C(C3=CC=CC=C3)(C4=CC=CC=C4)O)=O.Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AE9C90CB Related Classifications
HY-134971 Related Classifications
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