Trk Receptor Antagonist

Tanezumab (RN-624) is a humanized anti-NGF mAb with high affinity and specificity. Tanezumab blocks NGF binding to its receptors, p75 and TrkA, in the peripheral nervous system. Tanezumab can be used in studies of acute and chronic pain such as osteoarthritis, knee and neuralgia, as well as post-herpetic neuralgia.

ALE-0540, a nonpeptidic small molecule, is a nerve growth factor receptor antagonist. ALE-0540 inhibits the binding of NGF to tyrosine kinase (Trk) A or both p75 and TrkA with IC₅₀ values of 5.88 μM and 3.72 μM, respectively. ALE-0540 can be used to examine mechanisms leading to the development of agents for the study of pain.

Pegcantratinib (CT327) is a potent and selective TRKA antagonist with activity against TRKB and TRKC. Pegcantratinib can be used for research of CYLD cutaneous syndrome (CCS) and inflammatory dermatoses, such as psoriasis and concomitant pruritus.

ANA-12 (Standard) is an analytical standard of ANA-12 (HY-12479). This product is intended for research and analytical applications. ANA-12 is a brain-penetrant, selective TrkB antagonist with IC₅₀ values of 45.6 nM and 41.1 μM, and K_d values of 10 nM and 12 μM, for high- and low-affinity sites, respectively. ANA-12 specifically inhibits BDNF-induced TrkB receptor activation and its downstream signaling cascades by directly and non-competitively binding to the TrkB receptor, without affecting the functions of TrkA and TrkC. ANA-12 is used in research concerning neuropsychiatric disorders (such as depression and anxiety), acute and chronic pain, neuroimmune inflammation, and the mechanisms of learning and memory.