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Description: High affinity and selective M2 antagonist
Chemical Name: 11-[[4-[4-(Diethylamino)butyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one
Purity: ≥99% (HPLC)
Biological Activity for AQ-RA 741
AQ-RA 741 is a 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 for AQ-RA 741
AQ-RA 741 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for AQ-RA 741
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for AQ-RA 741
| 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 for AQ-RA 741
The following data is based on the product molecular weight 463.62. 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 | 2.16 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 for AQ-RA 741
References for AQ-RA 741
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for AQ-RA 741, please let us know.
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Keywords: AQ-RA 741, AQ-RA 741 supplier, Selective, high, affinity, M2, antagonists, Muscarinic, Receptors, Acetylcholine, ACh, AQRA741, 2292, Tocris Bioscience
Citations for AQ-RA 741
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