SML1983
PSB-603
≥98% (HPLC)
동의어(들):
8-(4-(4-(4-Chlorophenyl)piperazide-1-sulfonyl)phenyl)-1-propylxanthine, 8-[4-[[4-(4-Chlorophenyl)-1-piperazinyl]sulfonyl]phenyl]-3,9-dihydro-1-propyl-1H-purine-2,6-dione, PSB 603, PSB603
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모든 사진(1)
About This Item
실험식(Hill 표기법):
C24H25ClN6O4S
CAS Number:
Molecular Weight:
529.01
UNSPSC 코드:
12352200
NACRES:
NA.77
추천 제품
분석
≥98% (HPLC)
양식
powder
색상
white to brownish
solubility
DMSO: 2 mg/mL to clear
배송 상태
ambient
저장 온도
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
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)
InChI key
OVHCTHHFOHMNFV-UHFFFAOYSA-N
생화학적/생리학적 작용
A high-affinity, selective antagonist against A2b adenosine receptor (A2b-AR, A2bR).
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).
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.
신호어
Warning
유해 및 위험 성명서
Hazard Classifications
Skin Irrit. 2
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
가장 최신 버전 중 하나를 선택하세요:
이미 열람한 고객
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
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
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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