T1519

Rimonabant hydrochloride (SR 141716A) is a cannabinoid receptor antagonist, binding selectively to central cannabinoid receptors (CB1) with high affinity.

Edasalonexent (CAT-1004) is an orally available NF-κB inhibitor designed to improve Duchenne muscular dystrophy.

Rimonabant (SR141716) is an inverse agonist for the cannabinoid receptor CB1. It is an anorectic anti-obesity drug produced and marketed by Sanofi-Aventis. Its main avenue of effect is a reduction in appetite. Rimonabant is the first selective CB1 receptor blocker to be approved for use anywhere in the world. Rimonabant is approved in 38 countries including the E.U., Mexico, and Brazil. It was rejected for approval for use in the United States.

(S, R, S)-AHPC-PEG4-NH2 hydrochloride is a chemically synthesized conjugate consisting of an E3 ligase ligand-linker, incorporating the VHL ligand based on (S, R, S)-AHPC, and a 4-unit PEG linker, which are specifically designed for use in PROTAC technology.

(S,R,S)-AHPC-PEG4-NH2 (VHL Ligand-Linker Conjugates 4) is a synthetic E3 ligase ligand-linker conjugate, consisting of a VHL ligand based on (S,R,S)-AHPC combined with a 4-unit PEG linker.

PROTAC ERRα ligand 1 is an estrogen-related receptor α (ERRα) antagonist with IC50 values of 0.04 μM for ERRα and 2.8 μM for ERRγ.

Eact is a selective and potent TMEM16A activator that directly activates the TRPV1 channels in sensory nociceptors, thereby producing itch, acute nociception, and thermal hypersensitivity (brackets).

EBI-1051 is a highly potent and orally efficacious inhibitor of MEK [IC50: 3.9 nM].

EBI-2511 is a highly potent, orally active inhibitor of EZH2, with an IC50 of 6 nM in Pfeffiera cell lines.

Ebrotidine (FI3542) is a competitive H2-receptor antagonist with Ki of 127.5 nM. Ebrotidine has a potent antisecretory activity and evidenced gastroprotection.

EC23 (AGN 190205) is a stable synthetic retinoid analogue that induces neuronal differentiation.

Echinomycin (Quinomycin A) is an antitumor antibiotic secondary metabolite isolated from Streptomyces, a quinoxaline antibiotic, a DNA doubly intercalating peptide, and inhibits hypoxia-inducible factor-1 (HIF-1) DNA binding activity. Echinomycin has potential anticancer activity and can be used to study triple-negative breast cancer.

Edicotinib (JNJ-527) is a blood-brain-penetrating, orally active, selective CSF-1R inhibitor (IC50 value is 3.2 nM), with less inhibitory effects on KIT (IC50 value is 20 nM) and FLT3 (IC50 value is 190 nM). Edicotinib (JNJ-527) can block microglial proliferation and attenuate neurodegeneration, and can be used to study Alzheimer's disease and rheumatoid arthritis.

XMT-1519 conjugate-1 (compound 31) serves as a linker for the HER-2 monoclonal antibody XMT-1519, facilitating the synthesis of antibody-drug conjugates (ADCs) to enhance antitumor activity [1].

ΧΜΤ-1519 conjugate-1 (compound 31) TFA is the linker for the HER-2 monoclonal antibody XMT-1519, used in the synthesis of antibody-drug conjugates (ADCs) to enhance anti-tumor activity.