Vadimezan (ASA404)

For research use only. Not for use in humans.

目录号:S1537 别名: NSC 640488, DMXAA 中文名称:2,5-己酮可可碱

Vadimezan (ASA404) Chemical Structure

CAS No. 117570-53-3

Vadimezan (ASA404, NSC 640488, DMXAA)是一种vascular disrupting agents (VDA),也是一种DT-diaphorase的竞争性抑制剂,无细胞试验中Ki为20 μM ,IC50为62.5 μM。DMXAA (Vadimezan) 也是一种STING 激动剂,具有潜在的抗肿瘤活性。DMXAA (Vadimezan) 在体外可有效诱导 IFN-βTNF-α 的表达,但对 TNF-α 影响相对较低。DMXAA (Vadimezan)具有抗病毒活性。Phase 3。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1138.26 现货
RMB 991.09 现货
RMB 3029.34 现货
RMB 7922.67 现货
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客户使用Selleck生产的Vadimezan (ASA404)发表文献14篇:

客户使用该产品的5个实验数据:

  • (B and C) sh-scrambled or sh-ck2a–transducted L929 cells (B) and Raw cells (C) were stimulated by DMXAA (100 μg/ml) for various times. Cytosolic and nuclear extracts were prepared as described in Materials and Methods. Five percent of the cytosolic proteins and 20% of the nuclear proteins were resolved by 10% SDS-PAGE. Subsequently, immunoblotting was conducted by indicated Abs. The amounts of Tubulin and Lamin B1 in cytosol versus nuclei detected by respective Abs were used as internal control for fractionation.

    J Immunol, 2015, 194:4477-4488. Vadimezan (ASA404) purchased from Selleck.

  • (E) WT and ASC−/− macrophages were stimulated with 1 μg/ml of tumor-derived DNA in the presence of lipofectamine or 50 μg/ml of DMXAA at different time points. Whole cell extracts were analysed with antibodies against pTBK1, total TBK1, pIRF3, total IRF3 and GAPDH.

    J Immunol, 2016, 196(7):3191-8. Vadimezan (ASA404) purchased from Selleck.

  • (B and C) sh-scrambled or sh-ck2α–transducted L929 cells (B) and Raw cells (C) were stimulated by DMXAA (100 μg/ml) for various times. Cytosolic and nuclear extracts were prepared as described in Materials and Methods. Five percent of the cytosolic proteins and 20% of the nuclear proteins were resolved by 10% SDS-PAGE. Subsequently, immunoblotting was conducted by indicated Abs. The amounts of Tubulin and Lamin B1 in cytosol versus nuclei detected by respective Abs were used as internal control for fractionation.

    J Immunol, 2015, 194(9):4477-88. Vadimezan (ASA404) purchased from Selleck.

  • (b-e) HEK293T cells were transiently transfected with empty vector (b), plasmids encoding hSTING(H232) (c), hSTING(R232) (d), or mSTING (e) together with IFNβ-luciferase reporter. After 24 h, cells were transfected with 2′,3′‐cGAMP (2 μg/mL) or stimulated with CMA (50 μg/mL), DMXAA (50 μM) and α-mangostin. Luciferase activity was measured 24 h after stimulation. Error bars represent the SD of independent experiments (n=3); *P<0.05, **P<0.01, ***P<0.001 (Student's t-test).

    ChemMedChem, 2018, 13(19):2057-2064. Vadimezan (ASA404) purchased from Selleck.

  • (A) 24 h after incubation of co-culture of B16.F10 cells and TAMs with different concentrations of DMXAA; (B) 24 h after incubation of co-culture of B16.F10 cells and TAMs with different concentrations of SIM administered alone or in combination with 100 μM DMXAA; (C) 24 h after incubation of mono-cultured B16.F10 cells with 100 μM DMXAA administered alone and with different concentrations of SIM administered alone or in combination with 100 μM DMXAA. Data are shown as mean ± SD of triplicate measurements; DMXAA: cells incubated with different concentrations of DMXAA; SIM: cells incubated with different concentrations of SIM; SIM+ 100 μM DMXAA: cells incubated with different concentrations of SIM administered in combination with 100 μM DMXAA; The two-way ANOVA Multiple Comparison Test with Bonferroni post-tests was used to compare overall effects of different drug concentrations (*, P<0.05; **, P<0.01; ***, P<0.001).

    PLoS One, 2018, 13(8):e0202827. Vadimezan (ASA404) purchased from Selleck.

产品安全说明书

VDA抑制剂选择性比较

生物活性

产品描述 Vadimezan (ASA404, NSC 640488, DMXAA)是一种vascular disrupting agents (VDA),也是一种DT-diaphorase的竞争性抑制剂,无细胞试验中Ki为20 μM ,IC50为62.5 μM。DMXAA (Vadimezan) 也是一种STING 激动剂,具有潜在的抗肿瘤活性。DMXAA (Vadimezan) 在体外可有效诱导 IFN-βTNF-α 的表达,但对 TNF-α 影响相对较低。DMXAA (Vadimezan)具有抗病毒活性。Phase 3。
特性 DMXAA(ASA404)是DT-心肌黄酶竞争性抑制剂。
靶点
DT-diaphorase [1]
(Cell-free assay)
DT-diaphorase [1]
(Cell-free assay)
20 μM(Ki) 20 μM(Ki)
体外研究

在体外, DMXAA(ASA404)抑制纯化的DT-心肌黄酶,IC50为62.5 μM,Ki为20 μM。DMXAA(ASA404)作用于DLD-1人结肠癌细胞, 抑制DT-心肌黄酶活性,IC50为 49.6 μM,而对细胞色素 b5 还原酶和细胞色素P450还原酶没有显著作用效果。[1] DMXAA(ASA404)为抗病毒药物,作用于RAW 264.7巨噬细胞,抑制VSV-诱导的细胞毒性,也抑制流感病毒复制。[2] 最新研究显示DMXAA(ASA404)作用于VEGFR几种激酶成员,如人人脐静脉内皮细胞中的VEGFR2信号,具有非免疫调节的抑制效果。[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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MDA-MB-231 M{TiS2Z2dmO2aX;uJIF{e2G7 MoexNlQhfG9iOU[geW0> MkPKOFghcHK| NXrHcYR{TGWlcnXhd4UhcW5iTVTNNkBt\X[nbDDpckBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHH0JFI1KHSxIEm2JJVOKGGodHXyJFQ5KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? NVnJRW03RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizO|Y{PzJpPkK4N|c3Ozd{PD;hQi=>
HepG2 MWHD[YxtKGO7Y3zlJIFzemW|dDDhd5NigQ>? M4fESFAvOiC3TR?= MXGyOEBpenN? M2HzZ2NmdGxiY4njcIUh[XK{ZYP0JIlvKGi3bXHuJGhmeEd{IHPlcIx{KGG|c3Xzd4VlKGG|IHHjZ5VufWyjdHnvckBifCCVIIDoZZNmKGG2IECuNkB2VSCjZoTldkAzPCCqcoOgZpkheHKxcHnkbZVuKGmxZHnk[UB{fGGrbnnu[{1j[XOnZDDmcI94KGO7dH;t[ZRzcWNibXX0bI9lKHKnbHH0bZZmKHSxIHPvcpRzd2x? NGG3SVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGyPVUyOSd-MkmxNlk2OTF:L3G+
HepG2 MXLD[YxtKGO7Y3zlJIFzemW|dDDhd5NigQ>? M2rjcVI1KGi{cx?= NEDoN|FE\WyuIHP5Z4xmKGG{cnXzeEBqdiCqdX3hckBJ\XCJMjDj[YxteyCjc4Pld5Nm\CCjczDhZ4N2dXWuYYTpc44h[XRiUzDwbIF{\SClbz30doVifGWmIIfpeIgheHm{YX7vfIFvfGixbnWgZZQhOTpzIH3vcIFzKHKjdHnvJIFnfGW{IEK0JIhzeyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKG[ub4egZ5l1d22ndILpZ{Bu\XSqb3S= MnXMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzMkm1NVEoRjJ7MUK5OVEyRC:jPh?=
HepG2 NHjoW2hCeG:ydH;zbZMh[XO|YYm= Ml;kNE4zKHWP M2fnTVI1KGi{cx?= MYPJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEincFeyJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGOuZXH2[YQh[2G|cHHz[U0{KGyndnXsd{BifCByLkKgeW0h[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfCCvZYToc4Q> MofCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjlzMkm1NVEoRjJ7MUK5OVEyRC:jPh?=
HepG2 M1PvPGFxd3C2b4Ppd{Bie3OjeR?= MmXWNE4zKHWP NYm4SIxZOjRiaILz MnvOTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiClbHXheoVlKGOjc4Dhd4UuQSCuZY\lcJMh[XRiMD6yJJVOKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RibXX0bI9l MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF{OUWxNUc,OjlzMkm1NVE9N2F-
HepG2 NEL2fFdCeG:ydH;zbZMh[XO|YYm= NI\uOXEzPCCqcoO= NX3QbVZ4UW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnPy[YF{\SCrbjDjcIVifmWmIGDBVnAhdGW4ZXzzJINwNXS{ZXH0[YQhf2m2aDDwfZJidm:6YX70bI9v\SCjdDCxPlEhdW:uYYKgdoF1cW9iYX\0[ZIhOjRiaILzJIJ6KFenc4Tldo4h[myxdDDt[ZRpd2R? MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF{OUWxNUc,OjlzMkm1NVE9N2F-
HepG2 Mn;LRZBweHSxc3nzJIF{e2G7 NUHndYJFOC5{IIXN M4rQWVI1KGi{cx?= MVPJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEincFeyJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGOuZXH2[YQhWEGUUDDs[ZZmdHNiYYSgNE4zKHWPIHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4SgcYV1cG:m MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF{OUWxNUc,OjlzMkm1NVE9N2F-
HepG2 NYe0UXpXSXCxcITvd4l{KGG|c3H5 NIiwVFkzPCCqcoO= MVnJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEincFeyJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGOuZXH2[YQh[2G|cHHz[U0{KGyndnXsd{Bkdy22cnXheIVlKHerdHigdJlz[W6xeHHueIhwdmViYYSgNVoyKG2xbHHyJJJifGmxIHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4SgcYV1cG:m NFPh[3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUGyPVUyOSd-MkmxNlk2OTF:L3G+
HepG2 NHHlZoRCeG:ydH;zbZMh[XO|YYm= MVKyOEBpenN? NEW0bmpKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KGmwY4LlZZNmKGmwIHPs[YF3\WRiY3HzdIF{\S17IHzleoVteyClbz30doVifGWmIIfpeIgheHm{YX7vfIFvfGixbnWgZZQhOTpzIH3vcIFzKHKjdHnvJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5QhdWW2aH;k M{XFU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUK5OVEyLz5{OUGyPVUyOTxxYU6=
HepG2 M4O2[WFxd3C2b4Ppd{Bie3OjeR?= NYH1O41OOjRiaILz NWThTYhbUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCmb4fudoVofWyjdHnvckBw\iCEY3ytfGwh\XiycnXzd4lwdiClbz30doVifGWmIIfpeIgheHm{YX7vfIFvfGixbnWgZZQhOTpzIH3vcIFzKHKjdHnvJIFnfGW{IEK0JIhzeyCkeTDX[ZN1\XKwIHLsc5QhdWW2aH;k M2q3cVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUK5OVEyLz5{OUGyPVUyOTxxYU6=
HepG2 NF3rV5BCeG:ydH;zbZMh[XO|YYm= MYOyOEBpenN? M{XwT2lv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMhfXC{ZXf1cIF1cW:wIH;mJGJq\CCneIDy[ZN{cW:wIHPvMZRz\WG2ZXSge4l1cCCyeYLhco95[W62aH;u[UBifCBzOkGgcY9t[XJicnH0bY8h[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfCCvZYToc4Q> MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTF{OUWxNUc,OjlzMkm1NVE9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-p38 / p38 ; 

PubMed: 21819972     


Mouse macrophages (MHS) were stimulated with 20 µg/ml DMXAA in culture. At various time points, the culture supernatants and the cells were collected and assayed for amount of p38 phosphorylation with immunoblots. 

p-MK2 / pERK / p-JNK ; 

PubMed: 21819972     


Mouse macrophages (MHS) were pre-exposed to IFN-γ, followed by DMXAA treatment at 20 µg/ml. The cells also extracted to determine the effect of IFN-γ priming on DMXAA-induced MAPK pathways activation.

21819972
Growth inhibition assay
Cell proliferation ; 

PubMed: 30138430     


24 h after incubation of co-culture of B16.F10 cells and TAMs with different concentrations of DMXAA; 

30138430
体内研究 DMXAA(ASA404)显著延迟化学致癌物诱导的细胞生长, 提高肿瘤倍增时间,且提高从治疗到安乐死的时间。DMXAA(ASA404)处理携带肿瘤的动物后, 平均肿瘤倍增时间,平均肿瘤变三倍时间,及从治疗到安乐死的平均时间分别提高4.4-, 1.8- 2.7-倍。[4] DMXAA(ASA404)处理显著保护感染200 p.f.u.小鼠适应的H1N1流感 PR8病毒的C57BL/6J小鼠,使存活率达60%, 而对照组存活率只为20%。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

DT-心肌黄酶活性和酶抑制动力学分析:

通过在Beckman DU 650分光光度计上检测细胞色素 c 在 550 nm处减少量而测定纯化的DT-心肌黄酶活性。每组实验含细胞色素c(70 μM), NADH(多种浓度), 纯化的DT-心肌黄酶(0.032 μg),及溶于含0.14% BSA终体积为1 mL Tris–HCl buffer(50 mM, pH 7.4)的维生素K(多种浓度)。加入NADH开始反应。根据反应曲线初始部分(30秒)计算减少率, 结果表示为μmol 减少的细胞色素/min/mg 蛋白,使用21 mM−1 cm−1 摩尔消光系数表示减少的细胞色素c。在室温下进行酶反应,所有反应做三次平行。反应中含有的DMXAA(ASA404) (不同浓度) 用来表示纯化的 DT-心肌黄酶抑制活性,通过改变NADH (维生素K不变)维生素K (NADH不变) 的浓度测定抑制特性。获得Ki值。通过测量对Dicumarol敏感的DCPIP在 600 nm处的减少量而测定DT-心肌黄酶作用于DLD-1细胞的活性收集处于指数生长中期的DLD-1细胞,置于冰冻buffer (Tris–HCl, 25 mM, pH 7.4和 250 mM蔗糖),然后在冰上进行超声处理。酶反应条件为2 mM NADH, 40 μM DCPIP, 溶于含BSA (0.7 mg/mL)终体积为1 mL Tris–HCl (25 mM, pH 7.4) 的 20 μL Dicumarol。使用21 mM−1 cm−1 的摩尔消光系数表示对Dicumarol敏感的 DCPIP减少量。通过 Bradford检测测定蛋白水平。
细胞实验: [1]
- 合并
  • Cell lines: DLD-1和 H460
  • Concentrations: 0 到2 mM
  • Incubation Time: 96 小时
  • Method: DLD-1人结肠癌和H460人非小细胞肺癌细胞单层培养在RPMI 1640培养基中,培养基中补充胎牛血清 (10%), 丙酮酸钠(2 mM), 青霉素/链霉亲和素 (50 IU mL−1/50 μg mL-1) 及l-谷氨酰胺(2 mM)。在有氧条件下进行MTT 实验和所有其他实验,检测药物敏感性。细胞接种在96孔板上,然后在含5% CO2的环境下温育过夜。完全移除培养基,使用含多种药物浓度的培养基替代。在只有维生素K时,药物处理时间为1小时,然后细胞在Hanks’平衡盐溶液中冲洗两次,然后在每孔中加入200 μL 新鲜RPMI 1640培养基。 在只有DMXAA(ASA404) 存在时,药物处理时间为3小时。 随后温育4天,使用MTT检测测定细胞存活情况。为了DMXAA(ASA404)和维生素K联用,初步建立细胞 ,选择非毒性(细胞存活率>95%)浓度的DMXAA(ASA404)。细胞使用DMXAA(ASA404) (2 mM)先处理2小时,随后移除培养基,使用含抑制剂 (DMXAA(ASA404),持续浓度为2 mM)和维生素K(多种浓度)的培养基更换。再温育7小时,使用Hanks’平衡盐溶液冲洗细胞,再加入生长培养基。
    (Only for Reference)
动物实验: [4]
- 合并
  • Animal Models: 注射化学致癌物 (NMU)的雌性 Wistar大鼠
  • Dosages: ≤300 mg/kg
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 7 mg/mL (24.79 mM)
Water Insoluble
Ethanol Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 282.29
化学式

C17H14O4

CAS号 117570-53-3
储存条件 粉状
溶于溶剂
别名 NSC 640488, DMXAA

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00856336 Completed Drug: DMXAA Refractory Tumors Antisoma Research May 2003 Phase 1
NCT00863733 Completed Drug: DMXAA Solid Tumors Cancer Research UK|Cancer Society Auckland May 1996 Phase 1

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在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

VDA Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID