Drug intelligence / Profile preview

MRS1845

Development stage
Preclinical
Lead developer
National Institutes of Health
Modality
Small Molecules
Administration
Parenteral
01

Overview

MRS1845 (N-propargylnitrendipine) is a small molecule inhibitor of Orai1, the pore-forming subunit of the store-operated calcium entry (SOCE) channel. It is primarily utilized as a pharmacological research tool to investigate the role of calcium signaling in various cellular processes, particularly in immune cell function and oncology. In preclinical research concerning multiple myeloma, MRS1845 has been used to demonstrate that Orai1-mediated calcium influx is essential for the cytotoxic activity of natural killer (NK) cells. Specifically, studies have shown that butyrate can reverse daratumumab resistance by epigenetically upregulating Orai1 expression, an effect that is abolished by the administration of MRS1845, thereby confirming the critical role of the Orai1-mediated calcium signaling axis in overcoming treatment resistance.

Other names
N-propargylnitrendipine
02

Targets

LTCC (Voltage-gated calcium channel (L-type))ORAI1 (Calcium release–activated calcium channel protein 1)

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