ar a 2

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

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).

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

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.

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, exhibits analgesic activity, and can be used in the study of HCV.

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

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

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

ar-Turmerone ((+)-ar-Turmerone) is a major bioactive compound of the herb Curcuma longa with anti-tumorigenesis and anti-inflammatory activities[1][2][3]. It positively modulates murine DCs, induces NSC proliferation, and constitutes a promising therapeutic agent for various neurologic disorders[4][5]. It also activates apoptotic proteins in human lymphoma U937 cells[3].

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).

YT 6-2-PEG3-C2-NH2 is a conjugate of the autophagy-targeting ligand (ATL) targeting p62 SQSTM1 and an AUTOTAC linker. It is used in the synthesis of the AUTOTAC degrader ATC-324 for the androgen receptor (AR). ATC-324 induces the formation of the AR p62 complex, leading to autophagy-lysosomal degradation of AR. This action reduces nuclear AR levels and downregulates target gene expression of AR and AR-v7, effectively degrading common AR mutants found in prostate cancer (PCa).

BMY 7378 (free base) is a selective antagonist for the α1D adrenergic receptor (α1D-AR). It exhibits a membrane-binding affinity for cloned rat α1D-AR (Ki=2 nM) that is over 100 times stronger than its affinity for cloned rat α1A-AR (Ki=800 nM) or hamster α1B-AR (Ki=600 nM). Additionally, BMY 7378 (free base) acts as a partial agonist at the 5-HT1A receptor.

Antibioticadjuvant 2 (compound 5q) is a potent antibiotic adjuvant that enhances the efficacy of polymyxins and exhibits low toxicity in mammals. The minimum resensitization concentration of Antibioticadjuvant 2 for Escherichia coli AR-0493 is 0.125 μg/mL.

AR Degrader-1 (Compound ML 2-9) is a monovalent degrader of androgen receptors (AR) categorized under molecular glues. In LNCaP prostate cancer cells, it facilitates AR degradation through DCAF16 (E3 ligase) while exhibiting minimal cytotoxicity.

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].

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].

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

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

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

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)

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

A1AR antagonist 2 (compound 18h) is a potent antagonist of the A1 adenosine receptor (AR) with Ki values of 1.49, 10.2, and 50.1 nM for hA1, hA2A, and hA2B, respectively [1].

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].

Adenosine receptor inhibitor 2 (compound 14b) is a potent inhibitor of AR (adenosine receptor), exhibiting dual affinity towards A1/A2A ARs with higher affinity for A1- than A2A AR, and Ki values of 52.2 nM for A1 AR and 167 nM for A2A AR.