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Biological Activity
High affinity, selective muscarinic M2 receptor antagonist (pKi values are 8.3, 7.7 and 6.82 for M2, M1 and M3 receptors, respectively). Displays cardioselectivity in vivo, over intestinal, tracheal and bladder muscarinic receptors; inhibits vagally and agonist-induced bradycardia.
Compound Libraries
AQ-RA 741 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
M. Wt | 463.62 |
Formula | C27H37N5O2 |
Storage | Store at RT |
Purity | ≥99% (HPLC) |
CAS Number | 123548-16-3 |
PubChem ID | 129989 |
InChI Key | BCUGCHZRMKTPMU-UHFFFAOYSA-N |
Smiles | CCN(CC)CCCCC1CCN(CC(=O)N2C3=CC=CC=C3C(=O)NC3=C2N=CC=C3)CC1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
1eq. HCl | 46.36 | 100 | |
DMSO | 46.36 | 100 | |
ethanol | 46.36 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 463.62. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 2.16 mL | 10.78 mL | 21.57 mL |
5 mM | 0.43 mL | 2.16 mL | 4.31 mL |
10 mM | 0.22 mL | 1.08 mL | 2.16 mL |
50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Doods et al (1991) Cardioselectivity of AQ-RA 741, a novel tricyclic antimuscarinic drug. Eur.J.Pharmacol. 192 147 PMID: 2040358
Dorje et al (1991) Antagonist binding profiles of five cloned human muscarinic receptor subtypes. J.Pharmacol.Exp.Ther. 256 727 PMID: 1994002
Doods et al (1994) Pharmacological profile of selective muscarinic receptor antagonists on guinea-pig ileal smooth muscle. Eur.J.Pharmacol. 253 275 PMID: 8200421
Keywords: AQ-RA 741, supplier, Selective, high, affinity, M2, antagonists, Muscarinic, Receptors, Acetylcholine, ACh, AQRA741, M2, Receptors, M2, Receptors, Tocris Bioscience