PSB 0777 ammonium hydrate 

PSB 0777 ammonium hydrate is a potent and selective adenosine A_2A receptor full agonist with K_i values of 44.4 nM, 360 nM for rat and human A_2A receptors, respectively. PSB 0777 ammonium hydrate has K_i values of ≥10000 nM, 541 nM for rat and human A₁ receptors, respectively. PSB 0777 ammonium hydrate shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium hydrate has the potential for inflammatory bowel disease (IBS) research research^[1][2][3].

Ki: 44.4 nM (rat A_2A), 360 nM (human A_2A), ≥10000 nM (rat A₁) and 541 nM (human A₁)^[1]

PSB 0777 ammonium hydrate (compound 7) shows high selectivity for the A_2AAR (>225-fold) versus the other AR subtypes (K_i values of >10000 nM and ≫10000 for human A_2B receptor and A₃ receptor, respectively). PSB 0777 ammonium hydrate acts as an full agonist at A_2AAR with an EC₅₀ value of 117 nM in CHO-K1 cells^[1].
PSB-0777 ammonium binds human β1 (K_i=4.4 μM) and β3 (K_i=3.3 μM) adrenergic receptors^[2].
PSB 0777 ammonium hydrate (0.1 µM, 1 µM, 10 µM) increases concentration-dependently Acetylcholine (Ach, 1 mM) contractions in untreated and inflamed rat ileum/jejunum preparations in ex vivo experiments^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PSB 0777 ammonium hydrate (0.4 mg/kg/day; oral gavage; from the day 5 to 10) causes a marked reduction of inflammatory cell infiltration and an amelioration of colonic mucosal architecture^[3].
PSB 0777 ammonium hydrate (0.03, 0.3, 3 mg/kg; i.p.) causes dose-dependent hypothermia and hypoactivity in C57BL/6J mice^[2].
PSB 0777 ammonium hydrate cannot be absorbed systemically by the digestive mucosa once administered by the oral route. PSB 0777 ammonium hydrate (0.4 mg/kg/day; PO) has very low plasma concentrations in rats at 30 min (below 5 nM), and there is no plasma concentrations at 60 min after administration. PSB 0777 ammonium hydrate (0.4 mg/kg/day; IP) makes plasma concentrations well evident at 30 min, and decreases after 60 min, and is not detectable at 120 and 240 min^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

532.09

C₁₈H₂₀N₅O₇S₂.NH₄.1.75H₂O

Solid

White to off-white

OC[C@@H]1[C@H]([C@H]([C@H](N2C=NC3=C(N=C(SCCC4=CC=C(S(=O)([O-])=O)C=C4)N=C32)N)O1)O)O.[NH4+].[1.75].O

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Ali El-Tayeb, et al. Development of Polar Adenosine A2A Receptor Agonists for Inflammatory Bowel Disease: Synergism with A2B Antagonists. ACS Med Chem Lett. 2011 Oct 10;2(12):890-5.  [Content Brief]

  [2]. Jesse Lea Carlin, et al.Activation of adenosine A 2A or A 2B receptors causes hypothermia in mice. Neuropharmacology. 2018 Sep 1;139:268-278.  [Content Brief]

  [3]. L Antonioli, et al. Anti-inflammatory effect of a novel locally acting A 2A receptor agonist in a rat model of oxazolone-induced colitis. Purinergic Signal. 2018 Mar;14(1):27-36.  [Content Brief]