An antagonist of the EP2 receptor
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TG6-129

Item No. 19085

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2E)-N-[[[4-[[(5-ethyl-1,3,4-thiadiazol-2-yl)amino]sulfonyl]phenyl]amino]thioxomethyl]-3-(4-fluorophenyl)-2-propenamide
CAS Number
1164464-14-5
Synonyms
  • SID 17503974
Molecular Formula
C20H18FN5O3S3
Formula Weight
491.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 8 mg/mlDMSO: 10 mg/ml
λmax
224, 310 nm
SMILES
FC1=CC=C(/C=C/C(NC(NC2=CC=C(S(NC3=NN=C(CC)S3)(=O)=O)C=C2)=S)=O)C=C1
InChi Code
InChI=1S/C20H18FN5O3S3/c1-2-18-24-25-20(31-18)26-32(28,29)16-10-8-15(9-11-16)22-19(30)23-17(27)12-5-13-3-6-14(21)7-4-13/h3-12H,2H2,1H3,(H,25,26)(H2,22,23,27,30)/b12-5+
InChi Key
SYSMVOANBVDZNG-LFYBBSHMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $49

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    1 mg

    $86

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    5 mg

    $376

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    Product Description

    TG6-129 is an antagonist of the EP2 receptor, suppressing PGE2-induced elevation of cAMP in cells expressing EP2 with an IC50 value of 1.6 µM.1 It is without effect on EP4, DP1, IP, and β2-adrenergic receptors. TG6-129 reduces the expression of COX-2, IL-1β, IL-12, IL-23, IL-6, and TNF-α induced by the EP2-selective agonist butaprost (Item No. 13740) in P388D1 macrophages.1 It has low cell cytotoxicity (CC50 = 326 µM), prolonged plasma half-life, and does not cross the blood-brain barrier.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ganesh, T., Jiang, J., Shashidharamurthy, R., et al. Discovery and characterization of carbamothioylacrylamides as EP2 selective antagonists. ACS Med. Chem. Lett. 4(7), 616-621 (2013).