tcs ox2 29

TCS-OX2-29 is a potent and selective OX2 receptor antagonist (IC50: 40 nM). It displays >250-fold selectivity for OX2 over OX1.

TCS-OX2-29 is a selective orexin-2 receptor antagonist (IC50 = 40 nM), which plays an important role in pain modulation.

VEGFR-2-IN-29 is a VEGFR2 inhibitor.

SARS-CoV-2-IN-29 disodium, a diphosphate ester featuring a benzene system and molecular tweezers architecture, demonstrates antiviral efficacy by targeting SARS-CoV-2 with half-maximal inhibitory concentrations (IC50s) of 1.5 μM for virus activity and 1.6 μM for spike pseudoparticle transduction. Additionally, it disrupts liposomal membranes, evidenced by a half-maximal effective concentration (EC50) of 3.0 μM [1].

SARS-CoV-2-IN-29, a two-armed diphosphate ester featuring a benzene system and molecular tweezers, demonstrates antiviral efficacy with IC50 values of 1.5 μM for SARS-CoV-2 activity and 1.6 μM against spike pseudoparticle transduction. Additionally, it disrupts liposomal membranes, as indicated by an EC50 of 3.0 μM [1].

Peptide agonist for galanin receptors

COX-2-IN-29 is a selective inhibitor of orally active COX-2 (IC50: 0.005 μM).

Non-selective galanin receptor agonist (Ki values are 0.98, 1.48 and 1.47 nM for GAL1, GAL2 and GAL3 respectively). Anticonvulsant; prevents the occurrence of full kindled seizures in rats.

Galanin (2-11) amide is a synthetic peptide fragment of the neuropeptide galanin and an agonist of the galanin-2 (GAL2) receptor (EC50= 9.32 nM in a fluorescence imaging plate reader assay).1It selectively binds to the GAL2receptor (IC50= 1.76 nM for the rat receptor) over the GAL1receptor (IC50= 879 nM for the human receptor) but does also bind to the GAL3receptor (Ki= 271 nM for the rat receptor).1,2Intracerebroventricular administration of galanin (2-11) amide (1 nmol/animal) decreases immobility in the forced swim test in rats.3It also reduces the hind paw mechanical pain threshold and increases the hind paw cold sensitivity threshold in rats.1

Galanin is a neuropeptide with diverse biological activities. [1][2][3][4][5] It binds to rat galanin (GAL) receptor subtypes GAL1-3 (IC50s = 0.339, 1.35, and 3.31 nM, respectively) and human GAL1-3 (IC50s = 0.288, 1.62, and 12.3 nM, respectively). [1] Galanin binds to and inhibits contraction of guinea pig gastric smooth muscle cells induced by carbachol . [2] In vivo, Galanin (6 nmol, i.c.v.) increases feeding behavior in rats and increases latency to hindpaw withdrawal in response to heat and mechanical stimulation in a rat model of carrageenin-induced inflammation when administered at a dose of 2 nmol injected into the nucleus accumbens.[3][4] Galanin (5 μg, i.c.v.) also inhibits acetylcholine release induced by scopolamine in the ventral hippocampus of freely moving rats. [5]

N-terminal galanin fragment used to mediate central cardiovascular effects