Transient receptor potential (TRP) channel modulators

Transient receptor potential (TRP) channels are a superfamily of cation channels that is currently subdivided into nine families split into two groups, each containing a number of subfamilies. TRP channels are expressed ubiquitously and are activated by a wide range of stimuli.  TRP subunits assemble into homo- or heterotetramers and are often functionally associated with G-protein-coupled receptors, receptor tyrosine kinases and phospholipase C.  As TRPs are intimately linked with intracellular Ca2+ signaling, they are implicated in the control of cell cycle progression, cell migration and apoptosis.

Isca Biochemicals now offer several important peptides for TRP channel research.

TIP, or TRPV1 inhibitory peptide is a TRPV1 inhibitor corresponding to amino acids 701-709 of the TRPV1 receptor.  TIP effectively inhibits capsaicin induced calcium influx and TRPV1 activation and treatment of the immortalised human keratinocyte cell line HaCaT with TIP prevents UV induced increases of MMP-1 and pro-inflammatory cytokines. In mouse skin, TIP inhibits UV induced skin thickening and prevents UV induced expression of MMP-13 and MMP-9.

tatM2NX is a TRPM2 antagonist which prevents ligand binding and TRPM2 activation, and inhibits over 90% of human TRPM2 channel currents at concentrations as low as 2 μM.  tatM2NX is an antagonist with an IC50 of 396 nM and is neuroprotective in animal models of focal and global ischemia.

SOR-C13 is a carboxy terminal truncated peptide derived from the 54 residue paralytic peptide soricidin, found in the venom of the short-tailed shrew Blarina brevicauda. SOR-C13 is a high affinity, use dependent antagonist of human TRPV6 channels with an IC50 of 14 nM. TRPV6 is a non-voltage gated calcium channel implicated in malignancies and poor prognosis in breast cancer and in vivo, SOR-C13 reduces the growth of human ovarian xenografts.

WaTx, also known as wasabi receptor toxin, is the active component of the venom of the Australian black rock scorpion Urodacus manicatus. WaTx targets the mechanical and chemical stress sensor transient receptor potential cation channel 1 (TRPA1), which it stabilizes in an active state characterized by prolonged channel openings and low Ca2+ permeability. WaTx elicits acute pain and pain hypersensitivity, but fails to trigger efferent release of neuropeptides and neurogenic inflammation typically produced by other toxins. WaTx is a unique pharmacological probe for dissecting TRPA1 function and its contribution to acute and persistent pain.  

View all our products for TRP channel research.

All peptides are available from stock, in milligram to gram quantities. Please contact us with your requirements .