A TRPM8 antagonist
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AMG 333

Item No. 36825

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-[[[(S)-(3-fluoro-2-pyridinyl)[3-fluoro-4-(trifluoromethoxy)phenyl]methyl]amino]carbonyl]-3-pyridinecarboxylic acid
CAS Number
1416799-28-4
Molecular Formula
C20H12F5N3O4
Formula Weight
453.3
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
218, 268 nm
SMILES
O=C(C1=CC=C(C=N1)C(O)=O)N[C@H](C2=C(C=CC=N2)F)C3=CC(F)=C(C=C3)OC(F)(F)F
InChi Code
InChI=1S/C20H12F5N3O4/c21-12-2-1-7-26-17(12)16(10-4-6-15(13(22)8-10)32-20(23,24)25)28-18(29)14-5-3-11(9-27-14)19(30)31/h1-9,16H,(H,28,29)(H,30,31)/t16-/m0/s1
InChi Key
QEBYISWYMFIXOZ-INIZCTEOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $35

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    10 mg

    $65

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    25 mg

    $152

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    50 mg

    $268

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    Product Description

    AMG 333 is an antagonist of transient receptor potential melastatin 8 (TRPM8; IC50s = 13 and 20 for the human and rat channels, respectively).1 It is selective for TRPM8 over TRP vanilloid 1 (TRPV1), TRPV3, TRPV4, and TRP ankyrin 1 (TRPA1; IC50s = >20, >20, >20, and >40 µM, respectively), as well as a panel of 100 kinases and 144 additional targets at 1 and 10 µM, respectively. AMG 333 (0.6-3 mg/kg) decreases wet-dog shakes, a behavioral marker of cold sensation, induced by the TRPM8 agonist icilin (Item No. 10137) in rats.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Horne, D.B., Biswas, K., Brown, J., et al. Discovery of TRPM8 antagonist (S)-6-(((3-fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic acid (AMG 333), a clinical candidate for the treatment of migraine. J. Med. Chem. 61(18), 8186-8201 (2018).