AM12

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AM12 inhibits Lanthanide-evoked TRPC5 activity with an IC₅₀ of 0.28 μM.

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AM12 Chemical Structure

CAS No. : 2387510-84-9

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TRPC TRPM TRPV TRPA TRPML

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References
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Description

AM12 inhibits Lanthanide-evoked TRPC5 activity with an IC₅₀ of 0.28 μM^[1].

IC₅₀ & Target

IC50: 0.28 μM (TRPC5)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.28 μM Compound: 20; AM12	Inhibition of human TRPC5 expressed in HEK293 cells assessed as reduction in gadolinium-induced calcium entry after 30 mins by fura-2 dye based fluorescence assay Inhibition of human TRPC5 expressed in HEK293 cells assessed as reduction in gadolinium-induced calcium entry after 30 mins by fura-2 dye based fluorescence assay	[PMID: 30943030]

In Vitro

AM12 also inhibits TRPC5 activity evoked by the agonist (-)-Englerin A^[1].
AM12 also inhibits TRPC4 channels similarly. AM12 inhibits TRPC5 and TRPC4 channels via a site accessible from the extracellular face of the membrane, acting directly on either the channel or a site closely associated with it^[1].
AM12 also inhibits Ca²⁺ entry evoked by Gd³⁺. AM12 inhibits the Gd³⁺-evoked Ca²⁺ signal with an IC₅₀ of 0.28 μM. AM12 is slightly more potent than the natural product Galangin as an inhibitor of the Gd³⁺-evoked signal^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

349.13

Formula

C₁₅H₉BrO₅

CAS No.

2387510-84-9

SMILES

O=C1C(O)=C(C2=CC=CC=C2Br)OC3=C1C(O)=CC(O)=C3

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Naylor J, et al. Natural and synthetic flavonoid modulation of TRPC5 channels. Br J Pharmacol. 2016 Feb;173(3):562-74. [Content Brief]

AM12 Related Classifications

Cardiovascular Disease

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AM122387510-84-9AM 12AM-12TRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

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