1. GPCR/G Protein
  2. Adenosine Receptor
  3. PSB 0777 ammonium

PSB 0777 ammonium 

Cat. No.: HY-136233
Handling Instructions

PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research.

For research use only. We do not sell to patients.

PSB 0777 ammonium Chemical Structure

PSB 0777 ammonium Chemical Structure

CAS No. : 2122196-16-9

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research[1][2][3].

IC50 & Target

Ki: 44.4 nM (rat A2A), 360 nM (human A2A), ≥10000 nM (rat A1) and 541 nM (human A1)[1]

In Vitro

PSB 0777 ammonium (compound 7) shows high selectivity for the A2AAR (>225-fold) versus the other AR subtypes (Ki values of >10000 nM and ≫10000 for human A2B receptor and A3 receptor, respectively). PSB 0777 ammonium acts as an full agonist at A2AAR with an EC50 value of 117 nM in CHO-K1 cells[1].
PSB-0777 ammonium binds human β1 (Ki=4.4 μM) and β3 (Ki=3.3 μM) adrenergic receptors[2].
PSB 0777 ammonium (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].

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

In Vivo

PSB 0777 ammonium (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 (0.03, 0.3, 3 mg/kg; i.p.) causes dose-dependent hypothermia and hypoactivity in C57BL/6J mice[2].
PSB 0777 ammonium cannot be absorbed systemically by the digestive mucosa once administered by the oral route. PSB 0777 ammonium (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 (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].

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

Animal Model: Albino male Sprague-Dawley rats of 200 g with Oxazolone-induced colitis[3]
Dosage: 0.4 mg/kg
Administration: Oral gavage; daily; from the day 5 to 10
Result: Caused a marked reduction of inflammatory cell infiltration and an amelioration of colonic mucosal architecture alone or in combination with Dexamethasone (1 mg/kg/day).
Counteracted significantly the increment of colonic myeloperoxidase (MPO) levels associated with colitis.
Molecular Weight

500.55

Formula

C₁₈H₂₄N₆O₇S₂

CAS No.

2122196-16-9

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

PSB 0777PSB0777PSB-0777Adenosine ReceptorP1 receptorA2AA1brainpenetrantinflammatoryboweldiseaseIBSA2BA3β1β3AcetylcholineInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PSB 0777 ammonium
Cat. No.:
HY-136233
Quantity:
MCE Japan Authorized Agent: