An inhibitor of Nav1.8 channels
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.

PF-01247324

Item No. 22111

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-amino-N-methyl-5-(2,3,5-trichlorophenyl)-2-pyridinecarboxamide
CAS Number
875051-72-2
Molecular Formula
C13H10Cl3N3O
Formula Weight
330.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:4): 0.2 mg/ml
λmax
329 nm
SMILES
ClC1=CC(Cl)=CC(C2=C(N)N=C(C(NC)=O)C=C2)=C1Cl
InChi Code
InChI=1S/C13H10Cl3N3O/c1-18-13(20)10-3-2-7(12(17)19-10)8-4-6(14)5-9(15)11(8)16/h2-5H,1H3,(H2,17,19)(H,18,20)
InChi Key
HPIUHDCRVYDAEJ-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

    1 mg

    $37

    Add

    5 mg

    $106

    Add

    10 mg

    $194

    Add

    25 mg

    $436

    Add
    Product Description

    PF-01247324 is a blocker of the tetrodotoxin-resistant (TTX-R) sodium channel Nav1.8 (IC50 = 0.19 μM for human Nav1.8).1 It is selective for Nav1.8 over Nav1.1, Nav1.2, Nav1.5, and Nav1.7 channels (IC50s = 13, 12.8, 9, and 19 μM, respectively) as well as ether-a-go-go (ERG) potassium channels (IC50 = 30 μM). PF-01247324 blocks Nav1.8 channels in a VSP-FRET assay using HEK293 cells (IC50 = 2.6 μM). In vivo, PF-01247324 (100 mg/kg) reduces phase 2 flinching in a rat model of formalin-induced persistent pain.2 It increases latency to lift the inflamed paw and latency to paw withdrawal in rat models of carrageenan-induced thermal hyperalgesia and mechanical hyperalgesia induced by complete Freund's adjuvant (CFA), respectively.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bagal, S.K., Bungay, P.J., Denton, S.M., et al. Discovery and optimization of selective Nav1.8 modulator series that demonstrate efficacy in preclinical models of pain. ACS Med. Chem. Lett. 6(6), 650-654 (2015).

    2. Payne, C.E., Brown, A.R., Theile, J.W., et al. A novel selective and orally bioavailable Nav 1.8 channel blocker, PF-01247324, attenuates nociception and sensory neuron excitability. Br. J. Pharmacol. 172(10), 2654-5670 (2015).