| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Ki: 44.4 nM (rat A2A), 360 nM (human A2A), ≥10000 nM (rat A1) and 541 nM (human A1)[1]
PSB 0777 ammonium hydrate targets the adenosine A2A receptor, a G protein-coupled receptor (GPCR) that is activated by adenosine. A2A receptors are highly expressed in the striatum, immune cells, and blood vessels. The compound is a full agonist, meaning it maximally activates the receptor. It exhibits selectivity over A1 receptors, with Ki values for rat and human A1 receptors of ≥10,000 nM and 541 nM, respectively. |
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| ln Vitro |
Compound 7, PSB 0777 ammonium hydrate, exhibits significant selectivity (>225-fold) for the A2AAR relative to the other AR subtypes (Ki values of ≫10000 for the human A3 receptor and >10000 nM for the human A2B receptor, respectively). In CHO-K1 cells, PSB 0777 ammonium hydrate exhibits full agonistic activity at A2AAR, with an EC50 value of 117 nM[1]. Human β1 (Ki = 4.4 μM) and β3 (Ki = 3.3 μM) adrenergic receptors are bound by PSB-0777 ammonium[2]. In untreated and inflamed rat ileum/jejunum preparations, PSB 0777 ammonium hydrate (0.1 µM, 1 µM, and 10 µM) enhances concentration-dependently Acetylcholine (Ach, 1 mM) contractions[1].
In vitro, PSB 0777 ammonium hydrate is a potent A2A receptor full agonist with Ki values of 44.4 nM for rat A2A receptors and 360 nM for human A2A receptors. The compound is selective for A2A over A1 receptors, with Ki values of ≥10,000 nM for rat A1 and 541 nM for human A1. It can be used to study A2A receptor-mediated signaling pathways, including cAMP accumulation and vasodilation. The ammonium hydrate salt ensures solubility in aqueous buffers. |
| ln Vivo |
Ammonium hydrate (0.4 mg/kg/day; oral gavage; day 5 to day 10) administered via PSB 0777 results in a significant decrease in the infiltration of inflammatory cells and an improvement in the architecture of the colonic mucosa[3]. C57BL/6J mice are susceptible to dose-dependent hypothermia and hypoactivity when exposed to PSB 0777 ammonium hydrate (0.03, 0.3, and 3 mg/kg; ip)[2]. After being taken orally, PSB 0777 ammonium hydrate cannot be absorbed systemically by the mucosa of the digestive tract. Rats treated with PSB 0777 ammonium hydrate (0.4 mg/kg/day; PO) had very low plasma concentrations at 30 minutes (less than 5 nM) and no plasma concentrations at 60 minutes. Ammonium hydrate PSB 0777 (0.4 mg/kg/day; IP) produces plasma concentrations that are clearly visible after 30 minutes, start to decline after 60 minutes, and become undetectable after 120 and 240 minutes[3].
In vivo, PSB 0777 ammonium hydrate can be used to study A2A receptor pharmacology in animal models. As a full A2A agonist, it can induce vasodilation, reduce inflammation, and modulate neurotransmitter release. The compound is useful for investigating the therapeutic potential of A2A agonists in conditions such as Parkinson's disease, Huntington's disease, and inflammatory disorders. It is active and selective in vivo. |
| Enzyme Assay |
A cell-free radioligand binding assay is performed to measure A2A receptor binding. Membranes from CHO or HEK293 cells expressing human or rat A2A receptors (10-20 ug protein) are incubated with 0.5-2 nM [3H]CGS21680 (a selective A2A agonist radioligand) and increasing concentrations (0.01-10,000 nM) of PSB 0777 ammonium hydrate in binding buffer. Nonspecific binding is determined using 10 uM NECA. Bound radioligand is separated by filtration through GF/C filters. Ki values are calculated from competition curves.
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| Cell Assay |
HEK293 cells stably expressing human A2A receptors are seeded in 96-well plates. Cells are washed and pre-incubated in HBSS containing 1 mM IBMX (to inhibit phosphodiesterase). PSB 0777 ammonium hydrate is added at varying concentrations (0.1-1000 nM) and incubated for 15-30 min. cAMP levels are measured using a competitive ELISA or HTRF kit. The EC50 for cAMP accumulation is calculated. For selectivity testing, cells expressing A1, A2B, or A3 receptors are used in parallel.
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| Animal Protocol |
PSB 0777 ammonium hydrate can be studied in rodent models of A2A receptor function. Male Sprague-Dawley rats (200-250 g) are used in models of inflammation (e.g., LPS-induced paw edema). The compound (0.1-10 mg/kg) is administered intraperitoneally or orally in a suitable vehicle (e.g., 5% DMSO/PBS). Paw edema is measured by plethysmometry. In models of Parkinson's disease, the compound can be administered to evaluate its effects on motor function. Blood pressure and heart rate are monitored as pharmacodynamic endpoints.
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| ADME/Pharmacokinetics |
PSB 0777 ammonium hydrate has a molecular weight of 500.55 and the molecular formula C18H24N8O7S2. The compound exists as a solid at room temperature. It should be stored at -20degC, sealed and protected from moisture. The ammonium hydrate salt enhances water solubility. Specific PK parameters (t½, Cmax, AUC) have not been fully reported. For in vivo use, it can be formulated in 5% DMSO/PBS or saline.
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| Toxicity/Toxicokinetics |
No detailed toxicity data are reported for PSB 0777 ammonium hydrate. As an A2A receptor agonist, the primary mechanism-based safety concerns include hypotension, tachycardia, and potential effects on immune function. In animal studies, the compound was well-tolerated at the doses used (0.1-10 mg/kg). No specific organ toxicity has been reported. Standard safety precautions for handling research chemicals should be followed.
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| References |
[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.
[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. [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. |
| Additional Infomation |
PSB 0777 ammonium hydrate is a research-grade compound and is not approved for clinical use. It is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM for rat A2A receptors and 360 nM for human A2A receptors. The compound is a valuable research tool for studying A2A receptor pharmacology. This product is for research use only and not for human therapeutic applications.
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| Molecular Formula |
C18H20N5O7S2.NH4.1.75H2O
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| Related CAS # |
PSB 0777 ammonium;2122196-16-9
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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