LRRC8C Inhibitors
LRRC8C inhibitors encompass a variety of chemical entities that attenuate the functional activity of LRRC8C, a component of the volume-regulated anion channels (VRACs). Verapamil, a calcium channel blocker, indirectly inhibits LRRC8C by reducing intracellular calcium levels, a key regulator of VRAC activity, thus leading to diminished chloride ion conduction through LRRC8C. Similarly, DCPIB, a specific VRAC inhibitor, directlyhalts the chloride ion flow that LRRC8C mediates, significantly decreasing its functional channel activity. Bumetanide and Glibenclamide, although primarily acting on ion co-transporters and potassium channels respectively, can alter ionic gradients and cellular ionic homeostasis, which could indirectly impact the conduction properties of LRRC8C. Phloretin and Niflumic Acid, by their inhibition of various chloride channels, including VRACs, contribute to the reduction of LRRC8C's activity in chloride transport, suggesting a multi-target approach to diminishing LRRC8C function.
Further contributing to the inhibition of LRRC8C are compounds like Tamoxifen, Flufenamic Acid, and Gallotannin, which have been reported to inhibit VRACs, thereby decreasing LRRC8C's contribution to chloride ion transport across the cell membrane. The anion channel blockers DIDS and Dicamba (IAA-94) target anion exchange and chloride channels, respectively, curtailing the chloride ion flow integral to LRRC8C function. Moreover, Clofibric Acid, while known for its agonistic action on PPARs, also impedes VRAC activity, further repressing LRRC8C's role in anion conduction. Collectively, these inhibitors leverage the interconnected nature of cellular ion channels and transporters to mitigate the activity of LRRC8C, capitalizing on the sensitivity of VRACs to the ionic milieu and signaling modalities within the cell.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Verapamil | 52-53-9 | sc-507373 | 1 g | $374.00 | ||
Verapamil is a calcium channel blocker that reduces intracellular calcium levels. Since LRRC8C is part of the volume-regulated anion channels (VRAC) that are sensitive to cytosolic Ca2+ levels, verapamil can diminish LRRC8C-mediated chloride ion conduction. | ||||||
Bumetanide (Ro 10-6338) | 28395-03-1 | sc-200727 sc-200727A | 1 g 5 g | $109.00 $228.00 | 9 | |
Bumetanide is a loop diuretic inhibiting the Na+-K+-2Cl- co-transporter. By disrupting ionic gradients, bumetanide can indirectly affect the ionic balance across the cell membrane, thus potentially diminishing LRRC8C function as part of VRAC. | ||||||
Tamoxifen | 10540-29-1 | sc-208414 | 2.5 g | $272.00 | 18 | |
Tamoxifen is a selective estrogen receptor modulator that has been shown to inhibit VRAC. Given that LRRC8C forms part of the VRAC complex, tamoxifen can decrease the functional activity of LRRC8C by inhibiting the channel's conductance. | ||||||
Phloretin | 60-82-2 | sc-3548 sc-3548A | 200 mg 1 g | $64.00 $255.00 | 13 | |
Phloretin is a dihydrochalcone that inhibits various chloride channels, including VRACs. As LRRC8C is part of the VRAC complex, the inhibition by phloretin can lead to a decrease in LRRC8C-mediated chloride transport. | ||||||
Niflumic acid | 4394-00-7 | sc-204820 | 5 g | $32.00 | 3 | |
Niflumic acid is a nonsteroidal anti-inflammatory drug that blocks chloride channels. By blocking these channels, niflumic acid can indirectly lead to the diminishment of LRRC8C activity as it is part of the VRAC. | ||||||
Gallotannin | 1401-55-4 | sc-202619 sc-202619A sc-202619B sc-202619C sc-202619D sc-202619E sc-202619F | 1 g 10 g 100 g 250 g 1 kg 2.5 kg 5 kg | $26.00 $37.00 $67.00 $78.00 $234.00 $536.00 $983.00 | 12 | |
Gallotannin is a polyphenol with various biological effects, including the inhibition of chloride channels. By inhibiting VRACs, Gallotannin can decrease the functional activity of LRRC8C. | ||||||
Flufenamic acid | 530-78-9 | sc-205699 sc-205699A sc-205699B sc-205699C | 10 g 50 g 100 g 250 g | $27.00 $79.00 $154.00 $309.00 | 1 | |
Flufenamic acid is a nonsteroidal anti-inflammatory drug that acts as a blocker of chloride channels. Its inhibitory effect on VRACs can lead to the diminishment of LRRC8C activity, reducing chloride ion conduction. | ||||||
DIDS, Disodium Salt | 67483-13-0 | sc-203919A sc-203919B sc-203919 sc-203919C | 25 mg 100 mg 250 mg 1 g | $51.00 $163.00 $286.00 $683.00 | 6 | |
DIDS (4,4'-Diisothiocyanatostilbene-2,2'-disulfonic acid) is an inhibitor of anion exchangers and chloride channels, including VRACs. This inhibition can lead to reduced LRRC8C function as it impedes chloride ion transport through the channel complex. | ||||||
Glyburide (Glibenclamide) | 10238-21-8 | sc-200982 sc-200982A sc-200982D sc-200982B sc-200982C | 1 g 5 g 25 g 100 g 500 g | $46.00 $61.00 $117.00 $173.00 $530.00 | 36 | |
Glibenclamide is a sulfonylurea compound that inhibits ATP-sensitive potassium channels. By altering cellular ionic homeostasis, it can indirectly affect LRRC8C activity since potassium ion distribution can influence chloride channel activity as part of VRAC. | ||||||
Clofibric acid | 882-09-7 | sc-203000 sc-203000A | 10 g 50 g | $24.00 $40.00 | 1 | |
Clofibric acid is a peroxisome proliferator-activated receptor (PPAR) agonist, but it also exhibits inhibitory effects on chloride channels including VRACs. Its inhibition can therefore lead to reduced functional activity of LRRC8C within the channel complex. | ||||||