urotensin receptor

Urotensin-II receptor antagonist-1 (compound 1) is a human Urotensin II receptor antagonist with low oral bioavailability (F=0-3% in rats) and a Ki of 16 nM in HEK293 cells expressing human recombinant UT receptors. It inhibits cytochrome P450 enzymes (IC50=0.75 μM for CYP2D6; 1.4 μM for CYP3A4), suppresses κ opioid receptors (EC50=3.2 μM), and targets cardiac sodium channels (Ki=2.5 μM).

[Orn5]-URP acetate is an effective and selective Urotensin-II receptor (UT) antagonist (pEC50 = 7.24). [Orn5]-URP exhibits no agonist activity.

Palosuran (ACT-058362) (ACT-058362) is a new potent and specific antagonist of the human UT receptor.

SB 611812 is an antagonist of urotensin-II (UT) and can be used in studies about the treatment of cardiovascular disease.

Meclinertant (SR 48692) is a neurotensin receptor-1 (NT1) antagonist that blocks neurotensin-induced excitation and can be used to study neurological disorders.

FL104 is a potent agonist of small-molecule urotensin II receptor, pEC50= 7.11.

NTRC-844 is a selective rat neurotensin receptor type 2 (NTS2) antagonist that shows analgesic activity in animal models of pain.

Urotensin II, mouse acetate (9047-55-6 free base) is an endogenous ligand for the orphan GPR14 or SENR. It is a potent vasoconstrictor.

SB-657510 is a urotensin II (UII) receptor (UT) antagonist. The Ki values of UT for human, monkey, cat, rat and mouse were 61, 17, 30, 65 and 56 nM, respectively. SB-657510 plays an anti-inflammatory role by inhibiting UII-induced inflammatory mediators, such as adhesion molecules, in human vascular endothelial cells and upregulation of cytokines and tissue factors. SB 657510 has a therapeutic effect on diabetes-related atherosclerotic disease in diabetic mouse models.

(±)-AC 7954 hydrochloride is a urotensin-II (UT) receptor activator.

[Orn8]-Urotensin II acetate is a Urotensin receptor ligand and a partial agonist at Urotensin receptors.

Palosuran hydrochloride 540769-28-6(free base)(ACT-058362 hydrochloride) is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6±0.2 nM.

Urotensin II (114-124), human acetate is an 11-amino acid residue peptide, is a potent vasoconstrictor and agonist for the orphan receptor GPR14.

UFP 803 acetate is a potent ligand of urotensin-II (UT) receptor. UFP-803 displays the activity of a lower residual agonist.

Urantide acetate is a selective and competitive urotensin-II (UT) receptor antagonist (pKB = 8.3). Blocks hU-II induced contractions in thoracic aorta ex vivo. Exhibits no effect on noradrenaline or endothelin 1-induced contraction or on acetylcholine-ind

LM11A-31 dihydrochloride is a water-soluble, non-peptide with high blood-brain barrier permeability.LM11A-31 dihydrochloride, a p75NTR (neurotrophin receptor p75) Ligand, is a potent proNGF (nerve growth factor) antagonist.

AF40431 is the first reported small-molecule ligand of sortilin (IC50: 4.4 µM; Kd: 0.7 µM). AF40431 is bound in the neurotensin-binding site of sortilin.

NTRC-824 is >150-fold selectivity for NTS2 over NTS1 (Ki >30 μM). NTRC-824 is an effective, selective, and neurotensin-like nonpeptide neurotensin receptor type 2 (NTS2) antagonist (IC50: 38 nM and a Ki : 202 nM).

SBI-553 is an effective and brain penetrant NTR1 allosteric modulator (EC50: 0.34 μM).

SORT1-IN-2 (compound 6) is an inhibitor of SORT1.

PROTAC SMARCA2 degrader-29 (Example 87) is a potent PROTAC SMARCA2 (BRM) degrading agent with a DC50 ranging between 10-100 nM (BRM) and over 1 μM (BRG1, also known as SMARCA2).

EGFR-IN-132 (Compound 23) is an EGFR inhibitor effective against various EGFR mutations including the wild-type, L858R/T790M, d19/T790M, L858R/T790M/C797S, and d19/T790M/C797S with IC50 values of 1.6, 0.025, 0.019, 0.022, and 0.029 nM, respectively. This compound demonstrates favorable pharmacokinetics with high oral bioavailability.

SORT1-IN-5 (compound 3) is a SORT1 inhibitor capable of crossing the blood-brain barrier. The MSOH salt form of SORT1-IN-5 exhibits a certain degree of oral bioavailability.

SBI-810 is a functional selective β-arrestin-biased allosteric modulator of the neurotensin receptor 1 (NTSR1). In the presence of the endogenous ligand neurotensin (NT), SBI-810 regulates NTSR1 signaling through a G protein-specific mechanism. It fully antagonizes NT-induced Gq activation and partially antagonizes NT-induced Gi1 activation, allowing NTSR1 to activate GoA and G12.