An ago-PAM of α7 nAChRs
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B-973B

Item No. 38790

Technical Information
Formal Name
3,4-difluoro-N-[(1S)-1-[6-[4-(2-pyridinyl)-1-piperazinyl]-2-pyrazinyl]ethyl]-benzenepropanamide
CAS Number
2244989-34-0
Synonyms
  • (–)-(S)-B-973B
Molecular Formula
C24H26F2N6O
Formula Weight
Purity
≥98%
Formulation
A solid
Methanol: Soluble
SMILES
FC(C=C1CCC(N[C@H](C2=CN=CC(N3CCN(C4=CC=CC=N4)CC3)=N2)C)=O)=C(C=C1)F
InChi Code
InChI=1S/C24H26F2N6O/c1-17(29-24(33)8-6-18-5-7-19(25)20(26)14-18)21-15-27-16-23(30-21)32-12-10-31(11-13-32)22-4-2-3-9-28-22/h2-5,7,9,14-17H,6,8,10-13H2,1H3,(H,29,33)/t17-/m0/s1
InChi Key
WQYZERNSONBUCW-KRWDZBQOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    B-973B is an allosteric agonist and positive allosteric modulator (ago-PAM) of α7 nicotinic acetylcholine receptors (nAChRs).1,2 It enhances ACh-induced activation in a two-electrode voltage-clamp assay using Xenopus oocytes expressing the human α7 nAChR when used at a concentration of 10 µM.2 B-973B (10 mg/kg) decreases paw edema and induces antinociception in the first and second phase of the formalin test in a mouse model of inflammatory pain. It also inhibits tau aggregation induced by seeding with insoluble human tau isolated from a patient with Alzheimer’s disease in primary rat neurons in a concentration-dependent manner.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Post-Munson, D.J., Pieschl, R.L., Molski, T.F., et alB-973, a novel piperazine positive allosteric modulator of the α7 nicotinic acetylcholine receptor. Eur. J. Pharmacol. 799, 16-25 (2017).

    2. Garai, S., Raja, K.S., Papke, R.L., et alB-973, a novel α7 nAChR Ago-PAM: Racemic and asymmetric synthesis, electrophysiological studies, and in vivo evaluation. ACS Med. Chem. Lett. 9(11), 1144-1148 (2018).

    3. Gibbons, G.S., Gould, H., Lee, V.M.-Y., et alIdentification of small molecules and related targets that modulate tau pathology in a seeded primary neuron model. The Journal of Biological Chemisty 299(7), 104876 (2023).