PSB603 | CAS#1092351-10-4 | A(2B)R antagonist

MedKoo Cat#: 532482 | Name: PSB-603

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Description:

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

PSB-603 is a adenosine A(2B) receptor antagonist which suppresses tumor growth and metastasis by inhibiting induction of regulatory T cells. PSB-603 was used to study the impact of A2BAR activation or inhibition on trafficking.

Chemical Structure

PSB-603

CAS#1092351-10-4

Theoretical Analysis

MedKoo Cat#: 532482

Name: PSB-603

CAS#: 1092351-10-4

Chemical Formula: C24H25ClN6O4S

Exact Mass: 528.1347

Molecular Weight: 529.01

Elemental Analysis: C, 54.49; H, 4.76; Cl, 6.70; N, 15.89; O, 12.10; S, 6.06

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 350.00	2 Weeks
10mg	USD 550.00	2 Weeks

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Synonym

PSB603; PSB 603; PSB-603.

IUPAC/Chemical Name

8-{4-[4-(4-chlorophenyl)piperazine-1-sulfonyl]phenyl}-1-propyl-2,3,6,7-tetrahydro-1H-purine-2,6-dione

InChi Key

OVHCTHHFOHMNFV-UHFFFAOYSA-N

InChi Code

InChI=1S/C24H25ClN6O4S/c1-2-11-31-23(32)20-22(28-24(31)33)27-21(26-20)16-3-9-19(10-4-16)36(34,35)30-14-12-29(13-15-30)18-7-5-17(25)6-8-18/h3-10H,2,11-15H2,1H3,(H,26,27)(H,28,33)

SMILES Code

O=C(N1CCC)NC2=C(NC(C3=CC=C(S(=O)(N4CCN(C5=CC=C(Cl)C=C5)CC4)=O)C=C3)=N2)C1=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

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:

PSB-603 is an adenosine A2B receptor antagonist that displays > 17000-fold selectivity over other adenosine receptors (Ki values are 0.553, > 10000, > 10000 and > 10000 nM for A2B, A1, A2A and A3 receptors respectively).

In vitro activity:

In HNSCC cells, PSB-603 led to inhibition of cell proliferation, transmigration, and VEGFA secretion. These effects were associated with cell cycle arrest and the induction of the apoptotic pathway. Reference: Int J Cancer. 2020 Jul 1;147(1):202-217. https://pubmed.ncbi.nlm.nih.gov/31846065/

In vivo activity:

This study investigated the link between body weight reduction, glucose homeostasis, and anti-inflammatory activity induced by PSB-603. PSB-603 significantly reduced body weight in obese mice and significantly reduced triglycerides and total cholesterol blood levels. Reference: Int J Mol Sci. 2022 Nov 3;23(21):13439. https://pubmed.ncbi.nlm.nih.gov/36362227/

	Solvent	mg/mL	mM
Solubility
	DMSO	26.5	50.00

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 529.01 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.

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. Wilkat M, Bast H, Drees R, Dünser J, Mahr A, Azoitei N, Marienfeld R, Frank F, Brhel M, Ushmorov A, Greve J, Goldberg-Bockhorn E, Theodoraki MN, Doescher J, Laban S, Schuler PJ, Hoffmann TK, Brunner C. Adenosine receptor 2B activity promotes autonomous growth, migration as well as vascularization of head and neck squamous cell carcinoma cells. Int J Cancer. 2020 Jul 1;147(1):202-217. doi: 10.1002/ijc.32835. Epub 2020 Jan 9. PMID: 31846065. 2. Vecchio EA, Tan CY, Gregory KJ, Christopoulos A, White PJ, May LT. Ligand-Independent Adenosine A2B Receptor Constitutive Activity as a Promoter of Prostate Cancer Cell Proliferation. J Pharmacol Exp Ther. 2016 Apr;357(1):36-44. doi: 10.1124/jpet.115.230003. Epub 2016 Jan 20. PMID: 26791603. 3. Kotańska M, Dziubina A, Szafarz M, Mika K, Bednarski M, Nicosia N, Temirak A, Müller CE, Kieć-Kononowicz K. Preliminary Evidence of the Potent and Selective Adenosine A2B Receptor Antagonist PSB-603 in Reducing Obesity and Some of Its Associated Metabolic Disorders in Mice. Int J Mol Sci. 2022 Nov 3;23(21):13439. doi: 10.3390/ijms232113439. PMID: 36362227; PMCID: PMC9656786. 4. Kotańska M, Szafarz M, Mika K, Dziubina A, Bednarski M, Müller CE, Sapa J, Kieć-Kononowicz K. PSB 603 - a known selective adenosine A2B receptor antagonist - has anti-inflammatory activity in mice. Biomed Pharmacother. 2021 Mar;135:111164. doi: 10.1016/j.biopha.2020.111164. Epub 2020 Dec 29. PMID: 33385856.

In vitro protocol:

In vivo protocol:

1. Kotańska M, Dziubina A, Szafarz M, Mika K, Bednarski M, Nicosia N, Temirak A, Müller CE, Kieć-Kononowicz K. Preliminary Evidence of the Potent and Selective Adenosine A2B Receptor Antagonist PSB-603 in Reducing Obesity and Some of Its Associated Metabolic Disorders in Mice. Int J Mol Sci. 2022 Nov 3;23(21):13439. doi: 10.3390/ijms232113439. PMID: 36362227; PMCID: PMC9656786. 2. Kotańska M, Szafarz M, Mika K, Dziubina A, Bednarski M, Müller CE, Sapa J, Kieć-Kononowicz K. PSB 603 - a known selective adenosine A2B receptor antagonist - has anti-inflammatory activity in mice. Biomed Pharmacother. 2021 Mar;135:111164. doi: 10.1016/j.biopha.2020.111164. Epub 2020 Dec 29. PMID: 33385856.

1: Cherchi F, Venturini M, Magni G, Frulloni L, Chieca M, Buonvicino D, Santalmasi C, Rossi F, De Logu F, Coppi E, Pugliese AM. Adenosine A2B receptors differently modulate oligodendrogliogenesis and myelination depending on their cellular localization. Glia. 2024 Jul 30. doi: 10.1002/glia.24593. Epub ahead of print. PMID: 39077799. 2: Sanchez-Guerrero G, Umbaugh DS, Ramachandran AA, Artigues A, Jaeschke H, Ramachandran A. Translocation of Adenosine A2B Receptor to Mitochondria Influences Cytochrome P450 2E1 Activity after Acetaminophen Overdose. Livers. 2024 Mar;4(1):15-30. doi: 10.3390/livers4010002. Epub 2023 Dec 26. PMID: 39007013; PMCID: PMC11245301. 3: Gong X, Zheng C, Cai Y, Zhang W, Zhu B, Rong R, Kong Y, Zhang Y, Wang J, Li Y, Zhang P. Adenosine-modulating synthetic high-density lipoprotein for chemoimmunotherapy of triple-negative breast cancer. J Control Release. 2024 Mar;367:637-648. doi: 10.1016/j.jconrel.2024.01.064. Epub 2024 Feb 8. PMID: 38295994. 4: Wang Y, Chang J, Qiao S, Yang Y, Yun C, Li Y, Wang F. Salvianolic acid B attenuates diabetic nephropathy through alleviating ADORA2B, NALP3 in flammasome, and NFκB activity. Can J Physiol Pharmacol. 2024 May 1;102(5):318-330. doi: 10.1139/cjpp-2023-0089. Epub 2023 Dec 9. PMID: 38070193. 5: Marco-Bonilla M, Herencia R, Fresnadillo M, Huete-Toral F, Carracedo G, Largo R, Herrero-Beaumont G, Mediero A. Dipyridamole activates adenosine A2B receptor and AMPK/cAMP signaling and promotes myogenic differentiation of myoblastic C2C12 cells. Front Pharmacol. 2023 Sep 12;14:1247664. doi: 10.3389/fphar.2023.1247664. PMID: 37771723; PMCID: PMC10522837. 6: Kubacka M, Mogilski S, Bednarski M, Pociecha K, Świerczek A, Nicosia N, Schabikowski J, Załuski M, Chłoń-Rzepa G, Hockemeyer J, Müller CE, Kieć- Kononowicz K, Kotańska M. Antiplatelet Effects of Selected Xanthine-Based Adenosine A2A and A2B Receptor Antagonists Determined in Rat Blood. Int J Mol Sci. 2023 Aug 29;24(17):13378. doi: 10.3390/ijms241713378. PMID: 37686188; PMCID: PMC10487961. 7: Wang H, Tan F, Xu Y, Ma Y, Li Y, Xiao H. Adenosine Receptor A2B Antagonist Inhibits the Metastasis of Gastric Cancer Cells and Enhances the Efficacy of Cisplatin. Technol Cancer Res Treat. 2023 Jan-Dec;22:15330338221150318. doi: 10.1177/15330338221150318. PMID: 36786018; PMCID: PMC9929921. 8: Haddad M, Alsalem M, Aldossary SA, Kalbouneh H, Jaffal SM, Alshawabkeh Q, Al Hayek S, Abdelhai O, Barakat NA, El-Salem K. The role of adenosine receptor ligands on inflammatory pain: possible modulation of TRPV1 receptor function. Inflammopharmacology. 2023 Feb;31(1):337-347. doi: 10.1007/s10787-022-01127-3. Epub 2022 Dec 29. PMID: 36580157. 9: Kotańska M, Dziubina A, Szafarz M, Mika K, Bednarski M, Nicosia N, Temirak A, Müller CE, Kieć-Kononowicz K. Preliminary Evidence of the Potent and Selective Adenosine A2B Receptor Antagonist PSB-603 in Reducing Obesity and Some of Its Associated Metabolic Disorders in Mice. Int J Mol Sci. 2022 Nov 3;23(21):13439. doi: 10.3390/ijms232113439. PMID: 36362227; PMCID: PMC9656786. 10: Campos-Contreras ADR, González-Gallardo A, Díaz-Muñoz M, Vázquez-Cuevas FG. Adenosine Receptor A2B Negatively Regulates Cell Migration in Ovarian Carcinoma Cells. Int J Mol Sci. 2022 Apr 21;23(9):4585. doi: 10.3390/ijms23094585. PMID: 35562985; PMCID: PMC9100769. 11: Ma Q, Wang D, Li Y, Yang H, Li Y, Wang J, Li J, Sun J, Liu J. Activation of A2B adenosine receptor protects against demyelination in a mouse model of schizophrenia. Exp Ther Med. 2022 Jun;23(6):396. doi: 10.3892/etm.2022.11323. Epub 2022 Apr 14. PMID: 35495590; PMCID: PMC9047022. 12: Wang J, Wang D, Zheng X, Li Y, Li Y, Ma T, Li J, Sun J, Wang Y, Ma Q. A2B adenosine receptor inhibition ameliorates hypoxic-ischemic injury in neonatal mice via PKC/Erk/Creb/HIF-1α signaling pathway. Brain Res. 2022 May 1;1782:147837. doi: 10.1016/j.brainres.2022.147837. Epub 2022 Feb 16. PMID: 35182571. 13: Habahbeh S, Imraish A, Zihlif M. The crosstalk between adenosine A2B receptor and insulin signalling in rat skeletal muscle cells. Biol Futur. 2020 Sep;71(3):283-288. doi: 10.1007/s42977-020-00035-3. Epub 2020 Jul 28. PMID: 34554511. 14: Lindemann M, Dukic-Stefanovic S, Hinz S, Deuther-Conrad W, Teodoro R, Juhl C, Steinbach J, Brust P, Müller CE, Wenzel B. Synthesis of Novel Fluorinated Xanthine Derivatives with High Adenosine A2B Receptor Binding Affinity. Pharmaceuticals (Basel). 2021 May 19;14(5):485. doi: 10.3390/ph14050485. PMID: 34069548; PMCID: PMC8161391. 15: Kotańska M, Szafarz M, Mika K, Dziubina A, Bednarski M, Müller CE, Sapa J, Kieć-Kononowicz K. PSB 603 - a known selective adenosine A2B receptor antagonist - has anti-inflammatory activity in mice. Biomed Pharmacother. 2021 Mar;135:111164. doi: 10.1016/j.biopha.2020.111164. Epub 2020 Dec 29. PMID: 33385856. 16: Wilkat M, Bast H, Drees R, Dünser J, Mahr A, Azoitei N, Marienfeld R, Frank F, Brhel M, Ushmorov A, Greve J, Goldberg-Bockhorn E, Theodoraki MN, Doescher J, Laban S, Schuler PJ, Hoffmann TK, Brunner C. Adenosine receptor 2B activity promotes autonomous growth, migration as well as vascularization of head and neck squamous cell carcinoma cells. Int J Cancer. 2020 Jul 1;147(1):202-217. doi: 10.1002/ijc.32835. Epub 2020 Jan 9. PMID: 31846065. 17: Opoka W, Piotrowska J, Krakowski A, Kryczyk A, Sałat K, Zygmunt M, Librowski T, Muszyńska B. Effect of selected drugs on zinc accumulation in teeth of laboratory animals. Pharmacol Rep. 2018 Aug;70(4):684-687. doi: 10.1016/j.pharep.2018.02.006. Epub 2018 Feb 5. PMID: 29920420. 18: Ahmad T, Shin HJ, Lee J, Shin YM, Perikamana SKM, Park SY, Jung HS, Shin H. Fabrication of in vitro 3D mineralized tissue by fusion of composite spheroids incorporating biomineral-coated nanofibers and human adipose-derived stem cells. Acta Biomater. 2018 Jul 1;74:464-477. doi: 10.1016/j.actbio.2018.05.035. Epub 2018 May 23. PMID: 29803004. 19: Hinz S, Alnouri WM, Pleiss U, Müller CE. Tritium-labeled agonists as tools for studying adenosine A2B receptors. Purinergic Signal. 2018 Sep;14(3):223-233. doi: 10.1007/s11302-018-9608-5. Epub 2018 May 11. PMID: 29752618; PMCID: PMC6107469. 20: Goulding J, May LT, Hill SJ. Characterisation of endogenous A2A and A2B receptor-mediated cyclic AMP responses in HEK 293 cells using the GloSensor™ biosensor: Evidence for an allosteric mechanism of action for the A2B-selective antagonist PSB 603. Biochem Pharmacol. 2018 Jan;147:55-66. doi: 10.1016/j.bcp.2017.10.013. Epub 2017 Oct 26. PMID: 29106905; PMCID: PMC5770336.