An M4 muscarinic receptor PAM
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Emraclidine

Item No. 42125

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-(5,7-dihydro-2,4-dimethyl-6H-pyrrolo[3,4-b]pyridin-6-yl)-2-[1-[2-(trifluoromethyl)-4-pyridinyl]-3-azetidinyl]-ethanone
CAS Number
2170722-84-4
Synonyms
  • CVL-231
  • PF-06852231
Molecular Formula
C20H21F3N4O
Formula Weight
390.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(CC1CN(C1)C2=CC(C(F)(F)F)=NC=C2)N3CC4=NC(C)=CC(C)=C4C3
InChi Code
InChI=1S/C20H21F3N4O/c1-12-5-13(2)25-17-11-27(10-16(12)17)19(28)6-14-8-26(9-14)15-3-4-24-18(7-15)20(21,22)23/h3-5,7,14H,6,8-11H2,1-2H3
InChi Key
DTCZNKWBDTXEBS-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $413

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    10 mg

    $660

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    50 mg

    $1,032

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    100 mg

    $1,445

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    Product Description

    Emraclidine is a positive allosteric modulator (PAM) of M4 muscarinic acetylcholine receptors (mAChRs).1 It is selective for M4 mAChRs over a panel of 59 receptors, ion channels, transporters, and enzymes at 10 µM. Emraclidine selectively potentiates ACh-induced activation of the M4 mAChR over M1-M3 and M5 mAChRs in cells expressing the human receptors (EC50s = 12.3, 4,798, >10,000, >10,000, and >10,000 nM, respectively). In vivo, emraclidine (3.2 mg/kg) inhibits amphetamine-induced locomotor activity in mice and prepulse inhibition deficits in rats.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Butler, C.R., Popiolek, M., McAllister, L.A., et al. Design and synthesis of clinical candidate PF-06852231 (CVL-231): A brain penetrant, selective, positive allosteric modulator of the M4 muscarinic acetylcholine receptor. J. Med. Chem. 67(13), 10831-10847 (2024).