A265
ARL 67156 三钠盐 水合物
≥98% (HPLC), solid, ecto-ATPase inhibitor
别名:
6-氮,氮-二乙基-& # 946;-& # 947;-二溴亚甲基-D-腺苷-5 & # 8242;三磷酸 三钠盐 水合物, FPL 67156
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关于此项目
经验公式（希尔记法）:
C15H21Br2N5Na3O12P3 · xH2O
化学文摘社编号:
分子量:
785.05 (anhydrous basis)
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
ARL 67156 三钠盐 水合物, ≥98% (HPLC), solid
solubility
H2O: >20 mg/mL
DMSO: insoluble
SMILES string
O.[Na+].[Na+].[Na+].CCN(CC)c1ncnc2n(cnc12)[C@@H]3O[C@H](COP(O)(=O)OP([O-])(=O)C(Br)(Br)P([O-])([O-])=O)[C@@H](O)[C@H]3O
InChI
1S/C15H24Br2N5O12P3.3Na.H2O/c1-3-21(4-2)12-9-13(19-6-18-12)22(7-20-9)14-11(24)10(23)8(33-14)5-32-37(30,31)34-36(28,29)15(16,17)35(25,26)27;;;;/h6-8,10-11,14,23-24H,3-5H2,1-2H3,(H,28,29)(H,30,31)(H2,25,26,27);;;;1H2/q;3*+1;/p-3/t8-,10-,11-,14-;;;;/m1..../s1
InChI key
UWMONIJVKGTUGE-OPKBHZIBSA-K
assay
≥98% (HPLC)
form
solid
color
white to off-white
storage temp.
−20°C
Quality Level
Gene Information
human ... ENTPD2(954)
Application
ARL 67156三钠盐水合物可用于：
- 在脑脊液提取时抑制ATP降解
- 在细胞质和线粒体ATP定量实验中，作为ATP酶抑制剂防止ATP降解
- 在ATP释放试验中，作为胞外ATP酶抑制剂处理癌细胞
Biochem/physiol Actions
胞外ATPase抑制剂；防止2嘌呤受体激动剂的代谢。
General description
ARL 67156，一种核苷酸/ATP类似物，CD39的竞争性抑制剂。这种胞外ATP酶抑制剂含有β,γ-二溴亚甲基桥，推测其在生物学研究中具有代谢稳定性。
ARL-67156优先抑制鼠结肠中ADP 的分解，而不是抑制ATP的分解。它常被用于抑制组织制备液中的ATP水解。
存储类别
11 - Combustible Solids
wgk
WGK 3
B E Crack et al.
British journal of pharmacology, 114(2), 475-481 (1995-01-01)
1. FPL 67156 (6-N,N-diethyl-beta, gamma-dibromomethylene-D-ATP), is a newly synthesized analogue of ATP. 2. In a rabbit isolated tracheal epithelium preparation, measuring P2U-purinoceptor-dependent chloride secretion, FPL 67156 was discovered to potentiate the responses to UTP but not those to ATP-gamma-S. UTP
A commonly used ecto-ATPase inhibitor, ARL-67156, blocks degradation of ADP more than the degradation of ATP in murine colon
Durnin L, et al.
Neurogastroenterology and Motility (2016)
S A Lévesque et al.
British journal of pharmacology, 152(1), 141-150 (2007-07-03)
ARL 67156, 6-N,N-Diethyl-D-beta-gamma-dibromomethylene adenosine triphosphate, originally named FPL 67156, is the only commercially available inhibitor of ecto-ATPases. Since the first report on this molecule, various ectonucleotidases responsible for the hydrolysis of ATP at the cell surface have been cloned and
Laura Schäkel et al.
Frontiers in pharmacology, 11, 1294-1294 (2020-10-06)
Nucleoside triphosphate diphosphohydrolase1 (NTPDase1, CD39) inhibitors have potential as novel drugs for the (immuno)therapy of cancer. They increase the extracellular concentration of immunostimulatory ATP and reduce the formation of AMP, which can be further hydrolyzed by ecto-5'-nucleotidase (CD73) to immunosuppressive
Wanfeng Xu et al.
Cell metabolism, 33(2), 424-436 (2020-12-15)
Caspase-4 is an intracellular sensor for cytosolic bacterial lipopolysaccharide (LPS) and underlies infection-elicited pyroptosis. It is unclear whether and how caspase-4 detects host-derived factors to trigger pyroptosis. Here we show that mitochondrial permeability transition (MPT) activates caspase-4 by promoting the
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