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Merck

A265

Sigma-Aldrich

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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About This Item

经验公式(希尔记法):
C15H21Br2N5Na3O12P3 · xH2O
分子量:
785.05 (anhydrous basis)
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

产品名称

ARL 67156 三钠盐 水合物, ≥98% (HPLC), solid

质量水平

方案

≥98% (HPLC)

表单

solid

颜色

white to off-white

溶解性

H2O: >20 mg/mL
DMSO: insoluble

储存温度

−20°C

SMILES字符串

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

基因信息

human ... ENTPD2(954)

一般描述

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。

应用

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

生化/生理作用

胞外ATPase抑制剂;防止2嘌呤受体激动剂的代谢。

储存分类代码

11 - Combustible Solids

WGK

WGK 3


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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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
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
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)
T D Westfall et al.
European journal of pharmacology, 329(2-3), 169-173 (1997-06-25)
The influence of enzymatic degradation on the neurotransmitter actions of ATP was studied using the ecto-ATPase inhibitor 6-N,N-diethyl-D-beta,gamma-dibromomethyleneATP (ARL 67156). Field stimulation of the parasympathetic nerves innervating guinea-pig urinary bladder muscle strips (1-8 Hz for 20 s) produced characteristic biphasic

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