An M4 muscarinic receptor PAM
Technical Support & Resources

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

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
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
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    5 mg

    $413

    Add

    10 mg

    $660

    Add

    50 mg

    $1,032

    Add

    100 mg

    $1,445

    Add
    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).