A TRPM8 antagonist
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AMG 2850

Item No. 42906

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5,8R-dihydro-N-[(1S)-2,2,2-trifluoro-1-methylethyl]-8-[4-(trifluoromethyl)phenyl]-1,7-naphthyridine-7(6H)-carboxamide
CAS Number
1470018-52-0
Molecular Formula
C19H17F6N3O
Formula Weight
417.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
FC(F)(F)[C@H](C)NC(N1[C@H](C2=CC=C(C=C2)C(F)(F)F)C3=NC=CC=C3CC1)=O
InChi Code
InChI=1S/C19H17F6N3O/c1-11(18(20,21)22)27-17(29)28-10-8-12-3-2-9-26-15(12)16(28)13-4-6-14(7-5-13)19(23,24)25/h2-7,9,11,16H,8,10H2,1H3,(H,27,29)/t11-,16+/m0/s1
InChi Key
DDBWYSSPWMXBIY-MEDUHNTESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

    1 mg

    $75

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    5 mg

    $356

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    10 mg

    $599

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    25 mg

    $1,060

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    Product Description

    AMG 2850 is an antagonist of transient receptor potential melastatin 8 (TRPM8).1 It inhibits menthol- or cold-induced intracellular calcium release in CHO cells expressing rat TRPM8 (IC50s = 7.3 and 150 nM, respectively). AMG 2850 is selective for TRPM8 over transient receptor potential ankyrin 1 (TRPA1), transient receptor potential vanilloid 1 (TRPV1), TRPV3, and TRPV4 (IC50s = >20, >10, >10, and >10 µM, respectively). In vivo, AMG 2850 (100 mg/kg) decreases body temperature in rats and mice. It also inhibits wet-dog shakes induced by icilin (Item No. 10137) in rats when administered at a dose of 10 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gavva, N.R., Davis, C., Lehto, S.G., et al. Transient receptor potential melastatin 8 (TRPM8) channels are involved in body temperature regulation. Mol. Pain. 8, 36 (2012).

    2. Lehto, S.G., Weyer, A.D., Zhang, M., et al. AMG2850, a potent and selective TRPM8 antagonist, is not effective in rat models of inflammatory mechanical hypersensitivity and neuropathic tactile allodynia. Naunyn Schmiedebergs Arch. Pharmacol. 388(4), 465-476 (2015).