An agonist of α7 nAChRs
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PHA-543613

Item No. 42222

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(3R)-1-azabicyclo[2.2.2]oct-3-yl-furo[2,3-c]pyridine-5-carboxamide
CAS Number
478149-53-0
Synonyms
  • PHA-543,613
Molecular Formula
C15H17N3O2
Formula Weight
271.3
Purity
≥95%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
O=C(C1=NC=C(OC=C2)C2=C1)N[C@@H]3CN4CCC3CC4
InChi Code
InChI=1S/C15H17N3O2/c19-15(12-7-11-3-6-20-14(11)8-16-12)17-13-9-18-4-1-10(13)2-5-18/h3,6-8,10,13H,1-2,4-5,9H2,(H,17,19)/t13-/m1/s1
InChi Key
IPKZCLGGYKRDES-CYBMUJFWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $138

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    10 mg

    $235

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    50 mg

    $895

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    100 mg

    $1,238

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    Product Description

    PHA-543613 is an agonist of α7 nicotinic acetylcholine receptors (nAChRs).1,2 It is selective for α7 nAChRs over α4β2-, α4β4-, α3β2-, or α3β4 subunit-containing nAChRs and the serotonin (5-HT) receptor subtype 5-HT3 (EC50s = 0.03, >100, >50, >100, >100, and 11 µM, respectively, in calcium mobilization assays).2 PHA-543613 prevents decreases in the number of retinal ganglion cells in a rat model of glaucoma when applied topically.3 It improves sensorimotor deficits and reduces brain edema in a mouse model of intracerebral hemorrhage, effects that can be reversed by methyllycaconitine (Item No. 21398) or wortmannin (Item No. 10010591).4 PHA-543613 (1 mg/kg) increases the time spent with the novel object in the novel object recognition test and reverses amphetamine-induced auditory gating deficits in rats.1 Intracerebroventricular administration of PHA-543613 (0.1 mg/animal) reduces food intake and body weight in rats.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wishka, D.G., Walker, D.P., Yates, K.M., et al. Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: Synthesis and structure--activity relationship. J. Med. Chem. 49(14), 4425-4436 (2006).

    2. Gao, B., Hierl, M., Clarkin, K., et al. Pharmacological effects of nonselective and subtype-selective nicotinic acetylcholine receptor agonists in animal models of persistent pain. Pain 149(1), 33-49 (2010).

    3. Birkholz, P.J., Gossman, C.A., Webster, M.K., et al. Prevention of glaucoma-induced retinal ganglion cell loss using alpha7 nAChR agonists. J. Ophthalmol. Vis. Sci. 1(1), 1003 (2016).

    4. Krafft, P.R., Caner, B., Klebe, D., et al. PHA-543613 preserves blood-brain barrier integrity after intracerebral hemorrhage in mice. Stroke 44(6), 1743-1747 (2013).

    5. DiBrog, A.M., Kern, K.A., Demieri, E., et al. The alpha-7 nicotinic acetylcholine receptor agonist PHA-543613 reduces food intake in male rats. Pharmacol. Biochem. Behav. 237, 173723 (2024).