PSB-1115 (potassium salt)是一种选择性A2B腺苷受体拮抗剂。
Cas No.:409344-71-4
Sample solution is provided at 25 µL, 10mM.
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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.
PSB-1115 (potassium salt)是一种选择性A2B腺苷受体拮抗剂[1]。PSB-1115 (potassium salt)通过抑制TRPV1基因表达，减少钙离子内流，从而调节动物的感觉过敏和疼痛相关行为[2]。PSB-1115 (potassium salt)已广泛应用于大脑中动脉闭塞小鼠模型中以减少梗死面积[3]。
在体外，PSB-1115 (potassium salt)处理15分钟可显著抑制腺苷（100μM）诱导的T84细胞内cAMP升高，IC50值为84nM[4]。使用1µM的PSB-1115 (potassium salt)处理MDA-MB-231细胞24小时，能显著提高p-JNK1/2和JNK1/2的表达水平[5]。
在体内，连续4天每日瘤周注射1mg/kg剂量的PSB-1115 (potassium salt)，可显著抑制黑色素瘤小鼠模型的肿瘤生长，并显著减少肿瘤组织中CD11b+ Gr1+肿瘤浸润细胞的数量[6]。单次静脉注射10mg/kg剂量的PSB-1115 (potassium salt) 10分钟，能显著抑制由A1受体双位点配体VCP746引起的大鼠心动过速及肾脏和肠系膜血管扩张[7]。在携带B16.F10肿瘤的小鼠中连续一周每日腹腔注射1mg/kg剂量的PSB-1115 (potassium salt)，可显著降低肿瘤组织中VEGF表达水平和微血管密度[8]。
| 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 | |
| 别名 | 1-丙基-8-(4-磺酸基苯基)黄嘌呤钾盐水合物 | ||
| 化学名 | 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+] | ||
| 分子式 | C14H13N4O5S•K | 分子量 | 388.4 |
| 溶解度 | DMF: 5 mg/ml,DMSO: 25 mg/ml,PBS (pH 7.2): 1 mg/ml | 储存条件 | Store at -20°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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