AMG 9810

Product details

• Chemical name: (2E)-N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-3-[4-(1,1-dimethylethyl)phenyl]-2-propenamide.
• CAS number: 545395-94-6
• Molecular formula: C21H23NO3.
• Purity: >96% (HPLC)
• Concentration: 0.5 nM - 50 µM.
• Form: Lyophilized powder.
• Solubility: Ethanol 50 mM. Centrifuge all product preparations before use (10 000 x g for 1 min).
• Reconstitution: Ethanol 50 mM. Centrifuge all product preparations before use (10 000 x g for 1 min).
• Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
• Target: TRPV1 channels
• Source: Synthetic
• Activity: AMG 9810 blocks TRPV1 with IC50 ~0.01 µM1.

Scientific background

AMG 9810 (E)-3-(4-t-butylphenyl)-N-(2, 3- dihydrobenzo [b] [1,4] dioxin-6-yl) acrylamide is a potent, non-vanilloid, competitive antagonist of the vanilloid receptor 1 (TRPV1) with IC50 values for human TRPV1 of 24.5 nM and rat TRPV1 of 85.6 nM.Additionally, it has been shown to compete with other modes of TRPV1 activation, including protons (IC50s = 92.7 and 294 nM for human and rat, respectively), heat (IC50s = 15.8 and 21 nM for human and rat, respectively), and the endogenous ligands anandamide, N-arachidonoyl dopamine (IC50s = 8.5 and 260 nM for human and rat, respectively), and oleoyldopamine.Furthermore, AMG 9810 blocks capsaicin-induced calcitonin gene-related peptide (CGRP) release and capsaicin-evoked depolarization in rat dorsal root ganglia neurons.Finally, AMG 9810 was shown to be a potent and selective antagonist of TRPV1 that can significantly reverse thermal and mechanical hyperalgesia in an animal model of inflammatory pain1.

Lead time: 1-2 Business Days

Country of origin: Israel/IL

Applications key

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Bioassay tested: Yes

• SDS (PDF)

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