An antagonist of GPR35
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CID-2745687

Item No. 12046

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-(2,4-difluorophenyl)-5-[[2-[[(1,1-dimethylethyl)amino]thioxomethyl]hydrazinylidene]methyl]-1H-pyrazole-4-carboxylic acid, methyl ester
CAS Number
264233-05-8
Synonyms
  • ML-194
Molecular Formula
C17H19F2N5O2S
Formula Weight
395.4
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 10 mg/ml
λmax
242, 338 nm
SMILES
O=C(OC)C1=C(/C=N/NC(NC(C)(C)C)=S)N(C2=CC=C(F)C=C2F)N=C1
InChi Code
InChI=1S/C17H19F2N5O2S/c1-17(2,3)22-16(27)23-20-9-14-11(15(25)26-4)8-21-24(14)13-6-5-10(18)7-12(13)19/h5-9H,1-4H3,(H2,22,23,27)/b20-9+
InChi Key
CYNLZIBKERMMOA-AWQFTUOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $103

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    10 mg

    $153

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    25 mg

    $354

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    50 mg

    $653

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    Product Description

    CID-2745687 is a reversible, competitive antagonist of GPR35, blocking activation by the synthetic agonist pamoic acid with a Ki value of 12.8 nM.1 It less potently blocks activation of GPR35 by zaprinast (Item No. 10010421) (IC50 = 160 nM).2 It shows ~57-fold selectivity for GPR35 over the related receptor GPR55 (IC50 = 9.08 µM).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhao, P., Sharir, H., Kapur, A., et al. Targeting of the orphan receptor GPR35 by pamoic acid: A potent activator of extracellular signal-regulated kinase and β-arrestin2 with antinociceptive activity. Mol. Pharmacol. 78(4), 560-568 (2010).

    2. Heynen-Genel, S., Dahl, R., Shi, S., et al. Selective GPR35 antagonists: Antagonists for the orphan receptor GPR35. Probe 3, 1-18 (2011).