PSB-603
Based on 3 publication(s) in Google Scholar
PSB-603 is a potent and highly selective A2B adenosine receptor antagonist exhibiting a Ki value of 0.553 nM and virtually no affinity for the human and rat A1 and A2A and the human A3 receptors up to a concentration of 10 μM.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.38%
- CAS 番号: 1092351-10-4
- 分子式: C24H25ClN6O4S
- 分子量:529.01
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 PSB-603
More-
Cell Proliferation/Viability Assay
-
Cell Proliferation/Viability Assay
-
In Vivo Efficacy Study
-
In Vivo Efficacy Study
Adenosine Receptor アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| Jurkat | IC50 |
1.13 nM
Compound: 35
|
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
Antagonist activity at adenosine A2B receptor in human Jurkat T cells assessed as inhibition of NECA-induced increase in intracellular calcium concentration by fluorimetric measurement in presence of MSX-2
|
[PMID: 19569717] |
体外実験
PSB-603 is a potent and selective adenosine A2B receptor antagonist exhibiting a Ki value of 0.553 nM at the human A2B receptor and virtually no affinity for the human and rat A1 and A2A and the human A3 receptors up to a concentration of 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
-
Cell Line:Peripheral T cells
-
Concentration:100 nM
-
Incubation Time:24 hours
-
Result:Significantly inhibited NECA stimulated IL-6 release ≈3-fold.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Adult male Albino Swiss mice, CD-1, weighing 25-30 g[4]
-
Dosage:1, 5 or 10 mg/kg
-
Administration:Administered intraperitoneally (ip), prior to carrageenan injection
-
Result:Carrageenan-induced edema model. The increase in paw oedema was significantly inhibited in all groups receiving PSB-603. The dose of 5 mg/kg turned out to be the most active.
化学情報
-
CAS 番号 1092351-10-4
-
性状 Solid
-
分子量 529.01
-
分子式 C24H25ClN6O4S
-
Color Off-white to light brown
-
SMILES
O=C(N1CCC)NC2=C(N=C(C3=CC=C(S(=O)(N4CCN(C5=CC=C(Cl)C=C5)CC4)=O)C=C3)N2)C1=O
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
-
Journal Impact Factor
-
Most Recent
-
Cell Metab
Stress triggers irritable bowel syndrome with diarrhea through a spermidine-mediated decline in type I interferon. [Abstract]2025 Jan 7;37(1):87-103.e10. PMID: 39366386
PSB-603 purchased from MedChemExpress. Usage Cited in: Cell Metab. 2025 Jan 7;37(1):87-103.e10. [Abstract]
ES-exposed mice were i.p. injected with the A2B inhibitor PSB603 (PSB-603) (5 mg/kg; i.p.; once every 2 days for 3 times), followed by detection of visceral sensitivity (n = 4).
-
Br J Cancer
2024 May;130(9):1542-1551. PMID: 38461171
PSB-603 purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2024 May;130(9):1542-1551. [Abstract]
The effects of A2BR antagonist on CD39-mediated promotion of tumor metastasis. Each group of mice was injected intravenously with 5×105 vector or CD39-expressing CT-26 cells. Meanwhile, tumor-bearing mice were treated with PSB-603 (5 mg/kg, i.p.) or vehicle every other day. The lungs were removed and photographed after 12 days (n=5).
-
Sci Rep
Synergistic effects of HDAC inhibitor tucidinostat and ENT inhibitor dipyridamole in T-cell malignancies. [Abstract]2026 Mar 15. PMID: 41833979
PSB-603 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2026 Mar 15. [Abstract]
MT-1 cells were pretreated for 2 h with the indicated concentrations of selective adenosine receptor antagonists: PSB-603 (100-800 nM) for A2b, followed by treatment with dipyridamole (Dip; 16 µM), tucidinostat (Tuc; 360 nM), or their combination for 48 h. Cell viability was assessed by CCK-8 assay.
PSB-603 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2026 Mar 15. [Abstract]
ATN-1 cells were pretreated for 2 h with PSB-603 (100-800 nM) for A2b followed by treatment with dipyridamole (Dip; 16 µM), tucidinostat (Tuc; 360 nM), or their combination for 48 h. Cell viability was measured using the CCK-8 assay.
溶剤 & 溶解度
体外:
DMSO : 32.5 mg/mL (61.44 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 1.67 mg/mL (3.16 mM); Suspended solution; Need ultrasonic and warming and heat to 42°C
純度とドキュメンテーション
-
データシート (273 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Thomas Borrmann, et al. 1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity. J Med Chem. 2009 Jul 9;52(13):3994-4006. [Content Brief]
[2]. Mohamad Wessam Alnouri, et al. Selectivity is species-dependent: Characterization of standard agonists and antagonists at human, rat, and mouse adenosine receptors. Purinergic Signal. 2015 Sep;11(3):389-407. [Content Brief]
[3]. Nadine Borg, et al. CD73 on T Cells Orchestrates Cardiac Wound Healing After Myocardial Infarction by Purinergic Metabolic Reprogramming. Circulation. 2017 Jul 18;136(3):297-313. [Content Brief]
[4]. Magdalena Kotańska, et al. PSB 603 - a known selective adenosine A2B receptor antagonist-has anti-inflammatory activity in mice. Biomed Pharmacother. 2021 Mar;135:111164. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8903 mL | 9.4516 mL | 18.9032 mL | 47.2581 mL |
| 5 mM | 0.3781 mL | 1.8903 mL | 3.7806 mL | 9.4516 mL | |
| 10 mM | 0.1890 mL | 0.9452 mL | 1.8903 mL | 4.7258 mL | |
| 15 mM | 0.1260 mL | 0.6301 mL | 1.2602 mL | 3.1505 mL | |
| 20 mM | 0.0945 mL | 0.4726 mL | 0.9452 mL | 2.3629 mL | |
| 25 mM | 0.0756 mL | 0.3781 mL | 0.7561 mL | 1.8903 mL | |
| 30 mM | 0.0630 mL | 0.3151 mL | 0.6301 mL | 1.5753 mL | |
| 40 mM | 0.0473 mL | 0.2363 mL | 0.4726 mL | 1.1815 mL | |
| 50 mM | 0.0378 mL | 0.1890 mL | 0.3781 mL | 0.9452 mL | |
| 60 mM | 0.0315 mL | 0.1575 mL | 0.3151 mL | 0.7876 mL |