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(-)-(S)-B-973B 

Cat. No. M29417
(-)-(S)-B-973B  Structure
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Biological Activity

(-)-(S)-B-973B is a potent allosteric agonist and positive allosteric modulator of α7 nAChR, with antinociceptive activity.

Chemical Information
Molecular Weight 452.5
Formula C24H26F2N6O
CAS Number 2244989-34-0
Form Solid
Solubility (25°C) DMSO 67.5 mg/mL (ultrasonic)
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] Douglas R Miller, et al. Mol Pharmacol. Allosterically Potentiated α 7 Nicotinic Acetylcholine Receptors: Reduced Calcium Permeability and Current-Independent Control of Intracellular Calcium

[2] Roger L Papke, et al. Mol Pharmacol. Differing Activity Profiles of the Stereoisomers of 2,3,5,6TMP-TQS, a Putative Silent Allosteric Modulator of α 7 nAChR

[3] Alican Gulsevin, et al. Mol Pharmacol. Allosteric Agonism of α 7 Nicotinic Acetylcholine Receptors: Receptor Modulation Outside the Orthosteric Site

[4] Sumanta Garai, et al. ACS Med Chem Lett. B-973, a Novel α7 nAChR Ago-PAM: Racemic and Asymmetric Synthesis, Electrophysiological Studies, and in Vivo Evaluation

[5] Marta Quadri, et al. Mol Pharmacol. Macroscopic and Microscopic Activation of α 7 Nicotinic Acetylcholine Receptors by the Structurally Unrelated Allosteric Agonist-Positive Allosteric Modulators (ago-PAMs) B-973B and GAT107

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Keywords: (-)-(S)-B-973B  supplier, AChR/AChE, inhibitors, activators

 
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