β-ar

Compound 43, also known as β-AR antagonist 2, is an antagonist of β-AR with an IC50 of 0.17 μM. It inhibits the growth of mouse A549 xenograft tumors and demonstrates cardioprotective efficacy against DOX-induced heart failure in C57 mice [1].

MK-0773 (PF-05314882) is a selective androgen receptor modulator that binds to AR (IC50: 6.6 nM) for the study of diseases caused by endocrine abnormalities.

6-Methoxytricin, a flavonoid isolated from Centella asiatica, is an inhibitor of aldose reductase (AR) and advanced glycosylation end-products (AGE), and inhibits T-cell proliferation and activation in biologic cells.

Ridazolol HCl (CAS 413) is a novel β-adrenoceptor (β-AR) blocker with α-adrenerolytic activity.

Ritobegron (KUC-7483), an effective and selective β3-adrenergic receptor agonist, shows effective β(3)-AR agonist activity on transfected human β-AR and has an effect on the bladder of rats Shows high selectivity with other organs.

Synephrine hydrochloride (Oxedrine hydrochloride) is an agonist that acts on sympathomimetic α-adrenergic receptor (AR).

Ritobegron (also known as KUC-7483) is a potent and selective β3-adrenergic receptor agonist. In studies involving transfected human β-AR, Ritobegron exhibits significant and selective agonistic activity towards β(3)-AR. In rats, it shows high selectivity for the bladder over other organs. In anesthetized rats, Ritobegron effectively reduces bladder pressure with minimal impact on the cardiovascular system. It holds potential as a compound for treating overactive bladder.

O-Desmethylcarvedilol (Desmethylcarvedilol) is an active metabolite of Carvedilol, a non-selective β-adrenergic receptor (β-AR) antagonist. This compound inhibits store overload-induced calcium release in HEK293 cells expressing the RyR2 R4496C mutation (IC50= 7.62 µM). Additionally, O-Desmethylcarvedilol slows the increase in heart rate and prevents diastolic pressure reduction induced by Isoproterenol in conscious rabbits (ED50s = 32 and 5 µg kg).

PROTAC AR Degrader-9 (Compound c6) is a PROTAC-based degrader specifically targeting the androgen receptor. It effectively degrades the androgen receptor in human dermal papilla cells (HDPC) with a DC50 of 262.38 nM. Additionally, this compound enhances the expression of paracrine factors, such as TGF-β1 and β-catenin, thereby promoting hair regeneration in mouse models. [Pink: ligand for target protein AR ligand-38; Black: linker; Blue: ligand for E3 ligase Cereblon]

Zilpaterol hydrochloride is a agonist of β-adrenergic receptor (AR). It is used to increase the feeding efficiency and the size of cattle.

Alprenolol (Alpheprol) is a non-selective β-adrenergic receptor (β-AR) antagonist that is also an antagonist of the serotonin (5-HT) receptor subtypes 5-HT1A and 5-HT1B.

Dobutamine, a synthetic catecholamine, increases cardiac output and corrects hypoperfusion. It acts on α1-AR, β1-AR, and β2-AR (α-1, β-1, and β-2 adrenoceptors) with selective agonist activity on β1-AR and relatively weak activity at α1-AR and β2-AR. [1] [2] [3] [4].

Bopindolol ((±)-Bopindolol) fumarate is an orally active β-adrenoceptor (ARs) antagonist with partial agonist activity, non-selective for β1- and β2-ARs, and with low affinity for the β3-AR subtype. It is a precursor to Pindolol and is used to study primary and renal vascular hypertension.

GRK2 Inhibitor 2 (Compound 8h), with an IC50 of 19 nM for GRK2 and 137 nM for Aurora-A, enhances β-AR-mediated cAMP accumulation in GRK2-overexpressing HEK293 cells. It is utilized in congestive heart failure (HF) research [1].

Dobutamine hydrochloride (Dobutamine (hydrochloride)) is a catecholamine that acts as a β-adrenergic receptor agonist with potent positive inotropic effects.

Azenosertib (ZN-c3) is an orally active, specific GPR119 agonist. Azenosertib (ZN-c3) stimulates cell proliferation and improves pancreatic β-cell function. [1]

Bopindolol is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol is a prodrug of pindolol and can be rapidly metabolized to an active hydrolyzed form. Bopindolol can be used for essential and renovascular hypertension research [1] [2].