ar-a 2

AR-A 2 is a selective 5-HT1B receptor antagonist, with a high affinity to guinea pig cortex 5HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki: 0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki: 5 nM).

Mirosamicin is a macrolide antibiotic, it has antimicrobial effect against gram-positive bacteria, some gram-negative bacteria and mycoplasma.

AR antagonist 2 (compound 58) is a potent inhibitor of the androgen receptor (AR) (IC50: 0.95 μM).

β3-AR agonist 2 is a potent and selective agonist of β3-adrenergic receptor (β3-AR with an EC50 of 8 nM).

The compound is an a1/a3 adenosine receptor antagonist, which helps to treat (neurological) inflammatory diseases.

Finerenone (BAY-948862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist with IC50 of 18 nM for the treatment of chronic heart failure. Finerenone (BAY-948862) displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold).

GS-9667, a selective and partial agonist of the A(1) adenosine receptor (AR), represents an effective therapy for Type 2 diabetes (T2DM) and dyslipidemia via lowering of free fatty acids (FFA).

Norepinephrine (Levophed) can stimulate apoptosis in adult rat ventricular myocytes by activation of the β-adrenergic pathway. It can up-regulate the expression of vascular endothelial growth factor, matrix metalloproteinase (MMP)-2, and MMP-9 in nasopharyngeal carcinoma tumour cells.

Brimonidine Tartrate (AGN190342 tartrate) is a quinoxaline derivative and adrenergic α-2 receptor agonist (EC50: 0.45 nM) that is used to manage intraocular pressure associated with open-angle glaucoma or ocular hypertension.

Gliquidone (AR-DF 26) is a potent, second-generation sulfonylurea with antihyperglycemic activity. Like other second-generation compounds, gliquidone exerts greater binding affinity to SUR1 and increased potency compared to first-generation compounds. In addition, this agent exerts peroxisome proliferator-activated receptor (PPAR) gamma agonistic activity.

ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities[1][2][3]. ar-Turmerone ((+)-ar-Turmerone) exerts positive modulation on murine DCs, induces NSC proliferation.

AR-C141990 hydrochloride is a potent inhibitor of lactate transporters known as monocarboxylate transporters (MCTs). It has pK i values of 7.6 and 6.6 for MCT-1 and MCT-2, respectively. Additionally, this compound exhibits immunosuppressive properties and effectively inhibits the graft versus host response.

Guanfacine-13C,15N3is intended for us as an internal standard for the quantification of guanfacine by GC- or LC-MS. Guanfacine is an α2-adrenergic receptor (α2-AR) agonist with Kivalues of 93, 1,380, and 3,890 nM for α2A-, α2B-, and α2C-ARs, respectively, in a radioligand binding assay.1It has EC50values of 52, 288, and 602 nM for α2A-, α2B-, and α2C-ARs, respectively, for stimulated [35S]GTPγS binding. It also binds to imidazoline receptor 1 (Ki= 19 nM in a radioligand binding assay).2Guanfacine (0.3-5 mg/kg) binds to adrenergic receptors in the central nervous system and lowers blood pressure in hypertensive rats in a dose-dependent manner.3It also improves spatial working memory deficits induced by hypobaric hypoxia in rats.4Formulations containing guanfacine are used in the treatment of high blood pressure and attention deficit hyperactivity disorder (ADHD). 1.Jasper, J.R., Lesnick, J.D., Chang, L.K., et al.Ligand efficacy and potency at recombinant α2 adrenergic receptors: Agonist-mediated [35S]GTPγS bindingBiochem. Pharmacol.55(7)1035-1043(1998) 2.Nikolic, K., Filipic, S., and Agbaba, D.QSAR study of imidazoline antihypertensive drugsBioorg. Med. Chem.16(15)7134-7140(2008) 3.Scholtysik, G.Pharmacology of guanfacineBr. J. Clin. Pharmacol.10(Suppl 1)21S-24S(1980) 4.Kauser, H., Sahu, S., Kumar, S., et al.Guanfacine is an effective countermeasure for hypobaric hypoxia-induced cognitive declineNeuroscience254110-119(2013)

Tosatoxumab (AR-301; KBSA301), a human immunoglobulin G1 monoclonal antibody, specifically targets and neutralizes S. aureus alpha-toxin (alpha-hemolysin; Hla) by binding to its N-terminal epitope. This interaction blocks the toxin's ability to form functional pore oligomers, crucial for its pathogenic activity. As a result, Tosatoxumab offers promising potential as an adjunctive passive immunotherapy alongside conventional antibiotics for S. aureus pneumonia [1] [2].

Arformoterol Tartrate ((R,R)-Formoterol tartrate) is the tartrate salt of arformoterol. Arformoterol is a long-acting beta-2 adrenergic agonist with bronchodilator activity[2].

LL-K9-3, a selective hydrophobic tagging technology (HyT)-based degrader, specifically targets the CDK9-cyclin T1 complex, displaying DC50 values of 589 nM for cyclin T1 and 662 nM for CDK9. This compound consists of the CDK9 inhibitor, SNS 032, linked to a hydrophobic tag via a glycol linker. Notably, LL-K9-3 does not affect the degradation of other CDKs (CDK1, 2, 4, 5, 6, and 7). Tested in 22RV1 cells, it effectively reduces androgen receptor (AR) and cMyc expression by inducing the selective and synchronous degradation of CDK9 and cyclin T1.

Verosudil (AR-12286) is a highly potent Rho kinase (ROCK) inhibitor with a Ki of 2 and 2 nM against ROCK1 and ROCK2, respectively. AR-12286 reverses steroid-induced intraocular pressure in mice by decreasing intraocular pressure by increasing outflow of aqueous ether through the trabecular reticulum.

Adenosine receptor inhibitor 2 (compound 14b) is a potent inhibitor of AR (adenosine receptor). Adenosine receptor inhibitor 2 exhibits dual affinity toward A 1 /A 2A ARs with higher affinity for the A 1 - than the A 2A AR. Adenosine receptor inhibitor 2 exhibits Ki values of 52.2 nM for the A 1 AR and 167 nM for the A 2A AR.

Finerenone-d5 is a deuterated compound of Finerenone. Finerenone has a CAS number of 1050477-31-0. Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist with IC50 of 18 nM for the treatment of chronic heart failure. Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). 

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].

AR-H067637 is a rapid-binding, reversible and potent (inhibition constant K(i) = 2-4 nM), competitive inhibitor of thrombin, as well as of thrombin bound to fibrin (clot-bound thrombin) or to thrombomodulin. The total amount of free thrombin generated in

Aldose reductase-IN-2 (Compound 5f) is a potent inhibitor of aldose reductase (AR) with antioxidant properties. aldose reductase-IN-2 is a promising anti-diabetic complication drug.

2'-MeCCPA is a potent and highly selective A1 adenosine receptor (A1AR) agonist with a K-value of 1.8 nM for AR.2'-MeCCPA inhibits trichostatin-stimulated adenylate cyclase activity with an IC value of 13.1 nM.2'-MeCCPA exhibits analgesic activity and can be used in the study of HCV.

CLP-3094 (2-([2-(4-CHLOROPHENOXY)ETHYL]THIO)-1H-BE) is a potent androgen receptor BF3 (binding function 3) inhibitor. BF3-IN-1 inhibits AR transcriptional activity with IC50 of 4 μM. CLP-3094 is a selective and potent GPR142 antagonist.

AR-R17779 hydrochloride is a potent, selective full agonist of the nAChR, demonstrating K i values of 92 nM for the α7 subtype and 16,000 nM for the α4β2 subtype. It is noted for its ability to enhance learning and memory in rats, suggesting potential therapeutic applications. Additionally, this compound exhibits anxiolytic properties and can mitigate inflammation by activating anti-inflammatory cholinergic (vagal) pathways [1] [2] [4].

A1AR antagonist 2 (compound 18h) is a potent antagonist of the A1 adenosine receptor (AR). A1AR antagonist 2 has Ki values of 1.49, 10.2, and 50.1 nM for hA 1, hA 2A, and hA 2B, respectively [1].

AR-9281 (APAU) is a potent and selective inhibitor of soluble epoxide hydrolase (s-EH) potentially for the treatment of hypertension and type 2 diabetes

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].

Yohimbine is a nonselective alpha 2-adrenergic receptor (AR) antagonist(IC50 : 0.6 μM)

BMY 7378 dihydrochloride (BMY7378 HCl) , α1D-adrenergic receptor antagonist, is a weak partial agonist/antagonist of 5-HT1A receptor.

Dobutamine is a synthetic catecholamine that can increase cardiac output and correct hypoperfusion. Dobutamine acts on α1-AR, β1-AR, β2-AR (α-1, β-1 andβ-2 adrenoceptors) that is a selective agonist of β1-AR , relatively weak activity at α1-AR and β2-AR. [1] [2] [3] [4].