A TRPV1 antagonist
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A-784168

Item No. 32855

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3,6-dihydro-3′-(trifluoromethyl)-N-[4-[(trifluoromethyl)sulfonyl]phenyl]-[1(2H),2′-bipyridine]-4-carboxamide
CAS Number
824982-41-4
Molecular Formula
C19H15F6N3O3S
Formula Weight
479.4
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
O=C(C1=CCN(C2=NC=CC=C2C(F)(F)F)CC1)NC3=CC=C(S(=O)(C(F)(F)F)=O)C=C3
InChi Code
InChI=1S/C19H15F6N3O3S/c20-18(21,22)15-2-1-9-26-16(15)28-10-7-12(8-11-28)17(29)27-13-3-5-14(6-4-13)32(30,31)19(23,24)25/h1-7,9H,8,10-11H2,(H,27,29)
InChi Key
SDUAWRFBHRAFBM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $190

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    10 mg

    $283

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    25 mg

    $587

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    Product Description

    A-784168 is a transient receptor potential vanilloid 1 (TRPV1) competitive antagonist.1 It inhibits capsaicin-induced activation of TRPV1 in 1321N1 cells expressing TRPV1 (IC50 = 25 nM for the human receptor). A-784168 is selective for TRPV1 over a panel of 74 neurotransmitter receptors, ion channels, and other TRP channels at 50 μM but does act as an antagonist at TRP melastatin 8 (TRPM8; IC50 = 20.8 μM). It also inhibits TRPV1 activation induced by mildly acidic conditions, N-arachidonoyl dopamine (NADA; Item No. 90057), or anandamide (Item No. 90050) in HEK293 cells (IC50s = 14, 33.7, and 35.1 nM, respectively). It inhibits capsaicin-induced currents in primary rat dorsal root ganglion neurons (IC50 = 10 nM). A-784168 (200 μmol/kg) inhibits thermal hypersensitivity and mechanical hypersensitivity induced by NGF in rats.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cui, M., Honore, P., Zhong, C., et al. TRPV1 receptors in the CNS play a key role in broad-spectrum analgesia of TRPV1 antagonists. J. Neurosci. 26(37), 9385-9393 (2006).

    2. Mills, C.D., Nguyen, T., Tanga, F.Y., et al. Characterization of nerve growth factor-induced mechanical and thermal hypersensitivity in rats. Eur. J. Pain 17(4), 469-479 (2012).