A TRPV2 inhibitor
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SET2

Item No. 40360

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(2-furanylmethyl)-3-[[4-(methylpropylamino)-6-(trifluoromethyl)-2-pyrimidinyl]thio]-propanamide
CAS Number
2313525-20-9
Molecular Formula
C17H21F3N4O2S
Formula Weight
402.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
O=C(CCSC1=NC(C(F)(F)F)=CC(N(CCC)C)=N1)NCC2=CC=CO2
InChi Code
InChI=1S/C17H21F3N4O2S/c1-3-7-24(2)14-10-13(17(18,19)20)22-16(23-14)27-9-6-15(25)21-11-12-5-4-8-26-12/h4-5,8,10H,3,6-7,9,11H2,1-2H3,(H,21,25)
InChi Key
LZHSWRWIMQRTOP-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

    $491

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    50 mg

    $872

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    Product Description

    SET2 is an inhibitor of transient receptor potential vanilloid 2 (TRPV2; IC50 = 0.46 µM).1 It selectively inhibits currents induced by the TRP channel modulator 2-APB (Item No. 64970) in a patch-clamp assay using HEK293T cells overexpressing TRPV2 at 0.3 or 1 µM over HEK293T cells overexpressing TRPV1 or TRPV3 at 3 or 10 µM. SET2 (20 µM) reduces migration induced by lysophosphatidic acid (LPA) in PC-3M prostate cancer cells to a similar extent as the LPA receptor 1 (LPA1) antagonist AM966 (Item No. 22048). It also reduces LPA-induced increases in current in a patch-clamp assay using HEK293T cells when used at a concentration of 10 µM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Chai, H., Cheng, X., Zhou, B., et al. Structure-based discovery of a subtype-selective inhibitor targeting a transient receptor potential vanilloid channel. J. Med. Chem. 62(3), 1373-1384 (2019).