SML1983

Sigma-Aldrich

PSB-603

≥98% (HPLC)

Sinónimos:
8-(4-(4-(4-Chlorophenyl)piperazide-1-sulfonyl)phenyl)-1-propylxanthine, PSB 603, PSB603, 8-[4-[[4-(4-Chlorophenyl)-1-piperazinyl]sulfonyl]phenyl]-3,9-dihydro-1-propyl-1H-purine-2,6-dione
Empirical Formula (Hill Notation):
C24H25ClN6O4S
Número de CAS:
Peso molecular:
529.01
NACRES:
NA.77
En este momento no podemos mostrarle ni los precios ni la disponibilidad

assay

≥98% (HPLC)

form

powder

color

white to brownish

solubility

DMSO: 2 mg/mL to clear

shipped in

ambient

storage temp.

2-8°C

SMILES string

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

Biochem/physiol Actions

PSB-603 is known to modify cellular metabolism and enhance cellular sensitivity for chemotherapy. Thus, PSB-603 is recognized to possess anticancer action, which has been studied in colorectal cancer.
PSB-603 is an adenosine receptor A2b antagonist (IC50 = 1.13 nM against 10 μM A2bR agonist NECA-induced calcium response in Jurkat T cells in the presence of 200 nM A2aR antagonist MSX-2) that targets A2bR with high affinity (KD = 0.403 nM/human, 0.457 nM/rat, 4.09 nM/mouse A2bR; Ki against 0.3 nM [3H]PSB-603 = 0.553 nM/human, 0.355 nM/rat, 0.265 nM/mouse A2bR) and selectivity, exhibiting little affinity toward A1, A2a, or A3 adenosine receptors by competition binding assay (Ki >10 μM against 0.4 nM [3H]DPCPX for human/rat A1R, 1 nM [3H]MSX-2 for human/mouse/rat A2aR, 10 nM [3H]NECA for human/mouse/rat A3R) with the exception of mouse A1R (Ki = 42.2 nM against 0.4 nM [3H]DPCPX).

pictograms

Exclamation mark

signalword

Warning

hcodes

RIDADR

NONH for all modes of transport

WGK Germany

WGK 3

Flash Point F

Not applicable

Flash Point C

Not applicable

Mohamad Wessam Alnouri et al.
Purinergic signalling, 11(3), 389-407 (2015-07-02)
Adenosine receptors (ARs) have emerged as new drug targets. The majority of data on affinity/potency and selectivity of AR ligands described in the literature has been obtained for the human species. However, preclinical studies are mostly performed in mouse or...
Christina Mølck et al.
Cancer letters, 383(1), 135-143 (2016-10-30)
Adenosine is a multifaceted regulator of tumor progression. It modulates immune cell activity as well as acting directly on tumor cells. The A The A PSB-603 alters cellular metabolism in colorectal cancer cells and increases their sensitivity to chemotherapy. Although...
The A2b adenosine receptor antagonist PSB-603 promotes oxidative phosphorylation and ROS production in colorectal cancer cells via adenosine receptor-independent mechanism.
M?lck C, et al.
Cancer Letters, 383(1), 135-143 (2016)
Thomas Borrmann et al.
Journal of medicinal chemistry, 52(13), 3994-4006 (2009-07-03)
A new series of 1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines was designed, synthesized, and characterized in radioligand binding and functional assays at A(2B) adenosine receptors. A(2B) antagonists with subnanomolar affinity and high selectivity were discovered. The most potent compounds were 1-ethyl-8-(4-(4-(4-trifluoromethylbenzyl)piperazine-1-sulfonyl)phenyl)xanthine (24, PSB-09120, K(i) (human...

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