PSB-1115 (potassium salt) |
Catalog No.GC44733
One-Click Copy Product Info
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PSB-1115 (potassium salt) is a selective A2B Adenosine Receptor antagonist.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 409344-71-4
Sample solution is provided at 25 µL, 10mM.
PSB-1115 (potassium salt) is a selective A2B Adenosine Receptor antagonist [1]. PSB-1115 (potassium salt) can inhibit the expression of the TRPV1 gene, reduce calcium ion influx, and thereby regulate the sensory hypersensitivity and pain-related behaviors in animals[2]. PSB-1115 (potassium salt) has been widely used in mouse models of middle cerebral artery occlusion to reduce the infarct area[3].
In vitro, PSB-1115 (potassium salt) treatment for 15 minutes significantly inhibited the increase in cAMP induced by adenosine (100μM) in T84 cells, with an IC50 value of 84nM[4]. Treatment with 1µM PSB-1115 (potassium salt) for 24 hours resulted in a significant increase in the expression levels of p-JNK1/2 and JNK1/2 in MDA-MB-231 cells[5].
In vivo, PSB-1115 (potassium salt) treatment at a dose of 1mg/kg/day via peritumoral injection for 4 consecutive days significantly inhibited tumor growth in the melanoma mouse model and led to a significant reduction in the number of tumor-infiltrating CD11b+ Gr1+ cells in the in the tumors of mice[6]. A single intravenous injection of 10mg/kg dose of PSB-1115 (potassium salt) for 10min significantly inhibited the tachycardia and the dilation of the kidneys and mesenteric blood vessels caused by A1-receptor bitopic ligand VCP746 in rats[7]. For a consecutive week, 1mg/kg dose of PSB-1115 (potassium salt) was intraperitoneally injected into mice carrying B16.F10 tumors every day, resulting in a significant decrease in VEGF expression and microvessel density in the tumor tissues[8].
References:
[1] Rüsing D, Müller C E, Verspohl E J. The impact of adenosine and A2B receptors on glucose homoeostasis[J]. Journal of Pharmacy and Pharmacology, 2006, 58(12): 1639-1645.
[2] Hu X, Adebiyi M G, Luo J, et al. Sustained elevated adenosine via ADORA2B promotes chronic pain through neuro-immune interaction[J]. Cell Reports, 2016, 16(1): 106-119.
[3] Weitzel L B, Grewal H, Herson P S, et al. Abstract T P82: The Role of the A2B Receptor in a Mouse Model Of Stroke[J]. Stroke, 2015, 46(suppl_1): ATP82-ATP82.
[4] Asano T, Noda Y, Tanaka K I, et al. A2B adenosine receptor inhibition by the dihydropyridine calcium channel blocker nifedipine involves colonic fluid secretion[J]. Scientific Reports, 2020, 10(1): 3555.
[5] Zelepuga E A, Chingizova E A, Menchinskaya E S, et al. Anticancer Activity of Triterpene Glycosides Cucumarioside A0-1 and Djakonovioside A Against MDA-MB-231 as A2B Adenosine Receptor Antagonists[J]. International Journal of Molecular Sciences, 2025, 26(21): 10327.
[6] Iannone R, Miele L, Maiolino P, et al. Blockade of A2b adenosine receptor reduces tumor growth and immune suppression mediated by myeloid-derived suppressor cells in a mouse model of melanoma[J]. Neoplasia, 2013, 15(12): 1400-IN10.
[7] Cooper S L, Wragg E, March J, et al. Effects of an Adenosine Receptor Bitopic Ligand on The Cardiovascular System[J]. The FASEB Journal, 2020, 34(S1): 1-1.
[8] Sorrentino C, Miele L, Porta A, et al. Myeloid-derived suppressor cells contribute to A2B adenosine receptor-induced VEGF production and angiogenesis in a mouse melanoma model[J]. Oncotarget, 2015, 6(29): 27478.
| Cell experiment [1]: | |
Cell lines | MDA-MB-231 cells |
Preparation Method | MDA-MB-231 cells were cultured under standard conditions (37°C, 5% CO2) in MEM medium supplemented with 10% fetal bovine serum and 1% penicillin-streptomycin. MDA-MB-231 cells were seeded in 6-well plates (5×104/ml) and cultured at 37°C, 5% CO2 for 24 hours. Then, 1μM of Cucumarioside A0-1 (Cuc A0-1), 2μM of Djakonovioside A and 1μM PSB-1115 (potassium salt) were added to the cells and cultured for 6 hours. Subsequently, RIPA lysis buffer was added for cell lysis (10,000×g, 15 minutes, 4°C). The cell lysate supernatant was collected and the cAMP level was analyzed. |
Reaction Conditions | 1μM; 6h |
Applications | PSB-1115 (potassium salt) treatment significantly reduced cAMP levels in MDA-MB-231 cells. |
| Animal experiment [2]: | |
Animal models | Female Athymic Nude-Foxn1nu mice |
Preparation Method | Female Athymic Nude-Foxn1nu mice (6-8 weeks old) were housed in an animal room of specific pathogen-free (SPF) grade. 2×105 B16-F10 cells were subcutaneously injected into the right abdomen of anesthetized mice. Ten days after tumor cell implantation, when the tumors were palpable, Bay 60-6583 (0.2mg/kg/day) or PSB-1115 (potassium salt) (1mg/kg/day) was administered by peritumoral injection to the mice for 4 consecutive days, and the mouse tumor tissues were collected for analysis. |
Dosage form | 1mg/kg/day for 4 days; peritumoral injection |
Applications | PSB-1115 (potassium salt) treatment significantly reduced the levels of tumor-infiltrating CD11b+ Gr1+ cells in the tumor tissues of B16-F10 cell-xenograft mice. |
References: | |
| Cas No. | 409344-71-4 | SDF | |
| Chemical Name | 4-(2,3,6,9-tetrahydro-2,6-dioxo-1-propyl-1H-purin-8-yl)-benzenesulfonic acid, monopotassium salt | ||
| Canonical SMILES | O=C1N(CCC)C(C(NC(C2=CC=C(S([O-])(=O)=O)C=C2)=N3)=C3N1)=O.[K+] | ||
| Formula | C14H13N4O5S•K | M.Wt | 388.4 |
| Solubility | DMF: 5 mg/ml,DMSO: 25 mg/ml,PBS (pH 7.2): 1 mg/ml | Storage | Store at -20°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5747 mL | 12.8733 mL | 25.7467 mL |
| 5 mM | 514.9 μL | 2.5747 mL | 5.1493 mL |
| 10 mM | 257.5 μL | 1.2873 mL | 2.5747 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)