An inhibitor of Nav1.7 channels
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Nav1.7 Blocker 52

Item No. 34477

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-methyl-3-[[4-[4-[[4-(trifluoromethoxy)phenyl]methoxy]-1-piperidinyl]-1,3,5-triazin-2-yl]amino]phenyl]-acetamide
CAS Number
1211866-85-1
Synonyms
  • TC-N 1752
  • Voltage-gated Sodium Channel 1.7
Molecular Formula
C25H27F3N6O3
Formula Weight
516.5
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 30 mg/ml
SMILES
O=C(C)NC1=C(C)C(NC2=NC(N3CCC(CC3)OCC4=CC=C(C=C4)OC(F)(F)F)=NC=N2)=CC=C1
InChi Code
InChI=1S/C25H27F3N6O3/c1-16-21(31-17(2)35)4-3-5-22(16)32-23-29-15-30-24(33-23)34-12-10-19(11-13-34)36-14-18-6-8-20(9-7-18)37-25(26,27)28/h3-9,15,19H,10-14H2,1-2H3,(H,31,35)(H,29,30,32,33)
InChi Key
QLKAFHZJICDACE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $109

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    10 mg

    $207

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    25 mg

    $436

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    Product Description

    Nav1.7 blocker 52 is an inhibitor of voltage-gated sodium channel 1.7 (Nav1.7; IC50 = 0.17 µM).1 It is selective for Nav1.7 over human-ether-a-go-go (hERG), also known as Kv11.1, Nav1.5, and Nav1.8 (IC50s = >10, 1.1, and 2.2 µM, respectively) but does inhibit Nav1.3 and Nav1.4 (IC50s = 0.3 and 0.4 µM, respectively). Nav1.7 blocker 52 (20 and 30 mg/kg) inhibits formalin-induced flinching in a rat model of persistent pain. It also increases the latency to paw withdrawal in a hot plate test in a mouse model of inflammatory pain induced by complete Freund’s adjuvant (CFA).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bregman, H., Berry, L., Buchanan, J.L., et al. Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain. J. Med. Chem. 54(13), 4427-4445 (2011).

    2. Matson, D.J., Hamamoto, D.T., Bregman, H., et al. Inhibition of inactive states of tetrodotoxin-sensitive sodium channels reduces spontaneous firing of C-fiber nociceptors and produces analgesia in formalin and complete Freund’s adjuvant models of pain. PLoS One 10(9), e0138140 (2015).