MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 532481 | Name: PSB1115
Featured

Description:

WARNING: This product is for research use only, not for human or veterinary use.

PSB1115 is a highly selective, water-soluble, human A2B adenosine receptor antagonist. PSB1115 has Ki values are 53.4, > 10000 and > 10000 nM at human A2B, A1 and A3 receptors respectively. PSB1115 produces potent analgesic effects in vivo. Administration of PSB1115 abolished cupping's beneficial effects in LPS-induced ALI.

Chemical Structure

PSB1115
PSB1115
CAS#152529-79-8 (acid)

Theoretical Analysis

MedKoo Cat#: 532481

Name: PSB1115

CAS#: 152529-79-8 (acid)

Chemical Formula: C14H14N4O5S

Exact Mass: 350.0685

Molecular Weight: 350.35

Elemental Analysis: C, 48.00; H, 4.03; N, 15.99; O, 22.83; S, 9.15

Price and Availability

Size Price Availability Quantity
10mg USD 325.00
50mg USD 1,150.00
Bulk Inquiry
Buy Now
Add to Cart
Related CAS #
409344-71-4 (potassium) 152529-79-8 (acid)
Synonym
PSB1115; PSB 1115; PSB-1115.
IUPAC/Chemical Name
4-(2,6-dioxo-1-propyl-1,2,3,6-tetrahydropurin-8-yl)benzene-1-sulfonic acid
InChi Key
UYDRRQPGDSIMNU-UHFFFAOYSA-N
InChi Code
InChI=1S/C14H14N4O5S/c1-2-7-18-13(19)10-12(17-14(18)20)16-11(15-10)8-3-5-9(6-4-8)24(21,22)23/h3-6H,2,7H2,1H3,(H,15,16)(H,17,20)(H,21,22,23)
SMILES Code
O=S(C1=CC=C(C(N2)=NC(NC(N3CCC)=O)=C2C3=O)C=C1)(O)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO and water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
PSB1115 has Ki values are 53.4, > 10000 and > 10000 nM at human A2B, A1 and A3 receptors respectively. It produces potent analgesic effects in vivo.
In vitro activity:
In human embryonic kidney cells, AMP579 induced phosphorylation could be blocked by PSB1115. Reference: https://pubmed.ncbi.nlm.nih.gov/19730798/
In vivo activity:
PSB1115 increased the effectiveness of anti-aascular endothelial growth factor treatment. The pharmacological blockade of A2B receptor with PSB1115 significantly reduced tumor growth by inhibiting tumor angiogenesis and increasing T cells numbers within the tumor microenvironment. Reference: Oncotarget. 2015 Sep 29;6(29):27478-89. https://pubmed.ncbi.nlm.nih.gov/26317647/
Solvent mg/mL mM
Solubility
DMSO 38.8 100.00
Water 7.8 20.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 350.35 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Liu Y, Yang X, Yang XM, Walker S, Förster K, Cohen MV, Krieg T, Downey JM. AMP579 is revealed to be a potent A2b-adenosine receptor agonist in human 293 cells and rabbit hearts. Basic Res Cardiol. 2010 Jan;105(1):129-37. doi: 10.1007/s00395-009-0056-9. PMID: 19730798; PMCID: PMC2828901. 2. Sorrentino C, Miele L, Porta A, Pinto A, Morello S. Activation of the A2B adenosine receptor in B16 melanomas induces CXCL12 expression in FAP-positive tumor stromal cells, enhancing tumor progression. Oncotarget. 2016 Sep 27;7(39):64274-64288. doi: 10.18632/oncotarget.11729. PMID: 27590504; PMCID: PMC5325441. 3. Sorrentino C, Miele L, Porta A, Pinto A, Morello S. Myeloid-derived suppressor cells contribute to A2B adenosine receptor-induced VEGF production and angiogenesis in a mouse melanoma model. Oncotarget. 2015 Sep 29;6(29):27478-89. doi: 10.18632/oncotarget.4393. PMID: 26317647; PMCID: PMC4695003.
In vitro protocol:
1. Liu Y, Yang X, Yang XM, Walker S, Förster K, Cohen MV, Krieg T, Downey JM. AMP579 is revealed to be a potent A2b-adenosine receptor agonist in human 293 cells and rabbit hearts. Basic Res Cardiol. 2010 Jan;105(1):129-37. doi: 10.1007/s00395-009-0056-9. PMID: 19730798; PMCID: PMC2828901.
In vivo protocol:
1. Sorrentino C, Miele L, Porta A, Pinto A, Morello S. Activation of the A2B adenosine receptor in B16 melanomas induces CXCL12 expression in FAP-positive tumor stromal cells, enhancing tumor progression. Oncotarget. 2016 Sep 27;7(39):64274-64288. doi: 10.18632/oncotarget.11729. PMID: 27590504; PMCID: PMC5325441. 2. Sorrentino C, Miele L, Porta A, Pinto A, Morello S. Myeloid-derived suppressor cells contribute to A2B adenosine receptor-induced VEGF production and angiogenesis in a mouse melanoma model. Oncotarget. 2015 Sep 29;6(29):27478-89. doi: 10.18632/oncotarget.4393. PMID: 26317647; PMCID: PMC4695003.
1: Marín-Castejón A, Marco-Bonilla M, Terencio MC, Arasa J, Carceller MC, Ferrandiz ML, Noguera MA, Andrés-Ejarque R, Montesinos MC. Adenosine A2B receptor agonist improves epidermal barrier integrity in a murine model of epidermal hyperplasia. Biomed Pharmacother. 2024 Apr;173:116401. doi: 10.1016/j.biopha.2024.116401. Epub 2024 Mar 8. PMID: 38460363. 2: Tang W, Guan M, Li Z, Pan W, Wang Z. A2BR facilitates the pathogenesis of H. pylori-associated GU by inducing oxidative stress through p38 MAPK phosphorylation. Heliyon. 2023 Oct 20;9(11):e21004. doi: 10.1016/j.heliyon.2023.e21004. PMID: 38027590; PMCID: PMC10660004. 3: Ren Y, Qi L, Zhang L, Xu J, Ma J, Lv Y, Zhang Y, Wu R. Cupping alleviates lung injury through the adenosine/A2BAR pathway. Heliyon. 2022 Dec 5;8(12):e12141. doi: 10.1016/j.heliyon.2022.e12141. PMID: 36544817; PMCID: PMC9761715. 4: Odunsi K, Qian F, Lugade AA, Yu H, Geller MA, Fling SP, Kaiser JC, Lacroix AM, D'Amico L, Ramchurren N, Morishima C, Disis ML, Dennis L, Danaher P, Warren S, Nguyen VA, Ravi S, Tsuji T, Rosario S, Zha W, Hutson A, Liu S, Lele S, Zsiros E, McGray AJR, Chiello J, Koya R, Chodon T, Morrison CD, Putluri V, Putluri N, Mager DE, Gunawan R, Cheever MA, Battaglia S, Matsuzaki J. Metabolic adaptation of ovarian tumors in patients treated with an IDO1 inhibitor constrains antitumor immune responses. Sci Transl Med. 2022 Mar 16;14(636):eabg8402. doi: 10.1126/scitranslmed.abg8402. Epub 2022 Mar 16. PMID: 35294258; PMCID: PMC9311231. 5: Cooper SL, Wragg ES, Pannucci P, Soave M, Hill SJ, Woolard J. Regionally selective cardiovascular responses to adenosine A2A and A2B receptor activation. FASEB J. 2022 Apr;36(4):e22214. doi: 10.1096/fj.202101945R. PMID: 35230706; PMCID: PMC9415116. 6: Li HX, Liang XY, Wu JH, Yuan YP, Gao Y, Cai SH. Simvastatin attenuates acute lung injury by activation of A2B adenosine receptor. Toxicol Appl Pharmacol. 2021 Jul 1;422:115460. doi: 10.1016/j.taap.2021.115460. Epub 2021 Mar 24. PMID: 33774062. 7: Huang L, Fan J, Chen YX, Wang JH. Inhibition of A2B Adenosine Receptor Attenuates Intestinal Injury in a Rat Model of Necrotizing Enterocolitis. Mediators Inflamm. 2020 Jul 3;2020:1562973. doi: 10.1155/2020/1562973. PMID: 32714089; PMCID: PMC7354672. 8: Liu Y, Chu S, Hu Y, Yang S, Li X, Zheng Q, Ai Q, Ren S, Wang H, Gong L, Xu X, Chen NH. Exogenous Adenosine Antagonizes Excitatory Amino Acid Toxicity in Primary Astrocytes. Cell Mol Neurobiol. 2021 May;41(4):687-704. doi: 10.1007/s10571-020-00876-5. Epub 2020 Jul 6. Erratum in: Cell Mol Neurobiol. 2024 Jul 11;44(1):56. doi: 10.1007/s10571-024-01490-5. PMID: 32632892. 9: Duan L, Woolbright BL, Jaeschke H, Ramachandran A. Late Protective Effect of Netrin-1 in the Murine Acetaminophen Hepatotoxicity Model. Toxicol Sci. 2020 Jun 1;175(2):168-181. doi: 10.1093/toxsci/kfaa041. PMID: 32207522; PMCID: PMC7253199. 10: Asano T, Noda Y, Tanaka KI, Yamakawa N, Wada M, Mashimo T, Fukunishi Y, Mizushima T, Takenaga M. A2B adenosine receptor inhibition by the dihydropyridine calcium channel blocker nifedipine involves colonic fluid secretion. Sci Rep. 2020 Feb 26;10(1):3555. doi: 10.1038/s41598-020-60147-7. PMID: 32103051; PMCID: PMC7044278. 11: Guo X, An Y. [Role of adenosine A2b receptors in pulmonary microvascular endothelial inflammation induced by lipopolysaccharide]. Zhonghua Wei Zhong Bing Ji Jiu Yi Xue. 2019 Dec;31(12):1485-1490. Chinese. doi: 10.3760/cma.j.issn.2095-4352.2019.12.010. PMID: 32029034. 12: Zhou Y, Lin J, Peng X, Li C, Zhang J, Wang Q, Zhu G, You J, Zhao G. The role of netrin-1 in the mouse cornea during Aspergillus fumigatus infection. Int Immunopharmacol. 2019 Jun;71:372-381. doi: 10.1016/j.intimp.2019.03.047. Epub 2019 Apr 2. PMID: 30952101. 13: Guo X, An Y. [Activation of A2b adenosine receptor decreases lipopolysaccharide-induced pulmonary microvascular permeability]. Zhonghua Wei Zhong Bing Ji Jiu Yi Xue. 2018 Jun;30(6):588-593. Chinese. doi: 10.3760/cma.j.issn.2095-4352.2018.06.017. PMID: 30009737. 14: Xu X, Zhu Q, Niu F, Zhang R, Wang Y, Wang W, Sun D, Wang X, Wang A. A2BAR activation attenuates acute lung injury by inhibiting alveolar epithelial cell apoptosis both in vivo and in vitro. Am J Physiol Cell Physiol. 2018 Oct 1;315(4):C558-C570. doi: 10.1152/ajpcell.00294.2017. Epub 2018 Jun 13. PMID: 29898376. 15: Figueiredo AB, Souza-Testasicca MC, Mineo TWP, Afonso LCC. Leishmania amazonensis-Induced cAMP Triggered by Adenosine A2B Receptor Is Important to Inhibit Dendritic Cell Activation and Evade Immune Response in Infected Mice. Front Immunol. 2017 Jul 25;8:849. doi: 10.3389/fimmu.2017.00849. PMID: 28791011; PMCID: PMC5524897. 16: Sorrentino C, Miele L, Porta A, Pinto A, Morello S. Activation of the A2B adenosine receptor in B16 melanomas induces CXCL12 expression in FAP-positive tumor stromal cells, enhancing tumor progression. Oncotarget. 2016 Sep 27;7(39):64274-64288. doi: 10.18632/oncotarget.11729. PMID: 27590504; PMCID: PMC5325441. 17: Sorrentino C, Miele L, Porta A, Pinto A, Morello S. Myeloid-derived suppressor cells contribute to A2B adenosine receptor-induced VEGF production and angiogenesis in a mouse melanoma model. Oncotarget. 2015 Sep 29;6(29):27478-89. doi: 10.18632/oncotarget.4393. PMID: 26317647; PMCID: PMC4695003. 18: Yang Y, Qiu Y, Wang W, Xiao W, Liang H, Zhang C, Yang H, Teitelbaum DH, Sun LH, Yang H. Adenosine A2B receptor modulates intestinal barrier function under hypoxic and ischemia/reperfusion conditions. Int J Clin Exp Pathol. 2014 Apr 15;7(5):2006-18. PMID: 24966910; PMCID: PMC4069946. 19: He J, Zhao Y, Deng W, Wang DX. Netrin-1 promotes epithelial sodium channel- mediated alveolar fluid clearance via activation of the adenosine 2B receptor in lipopolysaccharide-induced acute lung injury. Respiration. 2014;87(5):394-407. doi: 10.1159/000358066. Epub 2014 Mar 21. PMID: 24663055. 20: Ning C, Wen J, Zhang Y, Dai Y, Wang W, Zhang W, Qi L, Grenz A, Eltzschig HK, Blackburn MR, Kellems RE, Xia Y. Excess adenosine A2B receptor signaling contributes to priapism through HIF-1α mediated reduction of PDE5 gene expression. FASEB J. 2014 Jun;28(6):2725-35. doi: 10.1096/fj.13-247833. Epub 2014 Mar 10. PMID: 24614760; PMCID: PMC4021439.