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Cat. No. Product Name CAS No. Information
PC-63492

CE-245677

717899-97-3

CE-245677 is a potent, selective, orally active, dual Tie2/Trk kinase inhibitor with IC50 of 4.7 nM, 1 nM for Tie2 and TrkA/B, respectively; displays >100-fold selectivity against a panel of angiogenic receptor tyrosine kinases (e.g. KDR, PDGFR, FGFR).

Pain

Phase 1 Clinical

PC-43281

PF-05089771 free base

1235403-62-9

PF-05089771 free base is a potent, subtype selective Nav1.7 inhibitor with IC50 of 11 nM, shows no activity against Nav 1.5 and >10-fold selectivity over other Nav isoforms; specifically interacts with the voltage-sensor domain (VSD4); blocks the majority of TTX-S current (75%) at 30 nM in human DRG neurons (IC50=8.4 nM); exhibits action potentials in spinal slice electrophysiology recordings, mouse and human DRG neurons, demonstrates in vivo efficacy mouse capsaicin-induced neurogenic flare model.

Pain

Phase 1 Discontinued

PC-43215

CNV1014802

934240-30-9

CNV1014802 (GSK-1014802, Raxatrigine, Vixotrigine, BIIB074) is a potent, selective Nav1.7 sodium channel blocker, shows analgesic effects and potential in the treatment of cognitive symptoms of schizophrenia in vivo.

Pain

Phase 2 Clinical

PC-63166

PF-05089771

1430806-04-4

PF-05089771 is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 11 nM, >1,000-fold selectivity over Nav1.3, 1.4 and Nav1.5, 1.8; interacts with the voltage-sensor domain (VSD) of domain IV, blocks all Nav1.7 splice variants with similar potency (5N11L, 5A11S, 5A11L and 5N11S, IC50s=11=33 nM); displays high selectivity over L-type calcium channels, KvLQT and hERG potassium channels; demonstrates in vivo efficacy in a mouse capsaicin-induced neurogenic flare model.

Pain

Phase 1 Discontinued

PC-61682

Oliceridine hydrochloride

1401028-24-7

Oliceridine hydrochloride (Olinvo, TRV130) is a potent, selective, and G protein biased μ opioid receptor (MOR) agonist with pEC50 of 8.1; displays 178-fold selectivity over KOR and 355-fold selectivity over DOR; elicits robust G protein signaling, with potency and efficacy similar to morphine in cell-based assays; is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine in mice and rats.

Pain

Phase 3 Clinical

PC-61681

Oliceridine

1401028-24-7

Oliceridine (Olinvo, TRV130) is a potent, selective, and G protein biased μ opioid receptor (MOR) agonist with pEC50 of 8.1; displays 178-fold selectivity over KOR and 355-fold selectivity over DOR; elicits robust G protein signaling, with potency and efficacy similar to morphine in cell-based assays; is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine in mice and rats.

Pain

Phase 3 Clinical

PC-61625

Befiradol

208110-64-9

Befiradol (F13640, NLX 112) is a highly potent, selective 5-HT1A receptor agonist with Ki of 2.7 nM; exhibits agonist efficacy greater than for (±)8-OH-DPAT or buspirone; stimulates 'total G-proteins', but unlike (±)8-OH-DPAT and buspirone, more potent for Gαo activation, in rat hippocampal membranes; dose-dependently decreases extracellular 5-HT in the hippocampus and mPFC in rats, activates both 5-HT(1A) autoreceptors and postsynaptic 5-HT(1A) receptors in prefrontal cortex with a similar potency.

Pain

Discontinued

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