DRAinh-A250 is a specific inhibitor of Cl-/anion exchanger SLC26A3 (DRA), fully and reversibly inhibits SLC26A3-mediated Cl- exchange with HCO3-, I-, and thiocyanate (SCN-) with IC50 of ~0.2 uM; does not inhibit the homologous anion exchangers SLC26A4 (pendrin) or SLC26A6 (PAT-1), as well as other related proteins or intestinal ion channels; blocked fluid absorption in closed colonic loops but not in jejunal loops in mice, while the NHE3 (SLC9A3) inhibitor tenapanor blocked absorption only in the jejunum; reduces signs of constipation in loperamide-treated mice after oral treatment.
CLP257 (CLP-257) is a potent, selective K+-Cl- cotransporter KCC2 activator with EC50 of 616 nM; displays selectivity for KCC2 over other KCC family members, NKCC1 and GABAA receptors, and a panel of 55 other receptors; restores impaired Cl(-) transport in neurons, rescues KCC2 plasma membrane expression; renormalizes stimulus-evoked responses in spinal nociceptive pathways in a rat model of neuropathic pain.
Join with Us
Product Use Citations
Pharmacological Glossary Abbreviations
How to Order
Terms & Conditions
Credit Card Payment
Shipping Rates & Policies