目录号
产品名
应用
产品描述
文献引用
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AMPK activator
Acadesine 是一种在肝细胞和脂肪细胞中选择性激活 AMPK 的物质。- R. Lim, .et al. , Placenta, 2015, Apr;36(4):454-62 PMID: 25659498
- Stella Liong, .et al. , J Physiol Biochem, 2015, Dec;71(4):703-17 PMID: 26407807
- 芦荟大黄素是一种存在于芦荟乳液中的蒽醌,芦荟乳液是从芦荟植物中分泌出的物质。它具有强烈的刺激性泻药作用。
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PARP inhibitor
Olaparib (AZD2281) 是一种抑制剂,针对的是参与 DNA 修复的酶——聚ADP核糖聚合酶(PARP)。- Yuki Yoshino, .et al. , Biochem Biophys Res Commun, 2025, Jan:742:151153 PMID: 39672008
- Saptarshi Sinha, .et al. , Med Oncol, 2024, Jan 6;41(2):49 PMID: 38184505
- Erika Nakatsuka, .et al. , Transl Oncol, 2024, Sep 12:50:102119 PMID: 39270525
- Callum G Jones, .et al. , Cancers (Basel), 2024, Feb 21;16(5):863 PMID: 38473223
- Aurelie Vanderlinden, .et al. , Br J Cancer, 2023, Nov;129(11):1829-1840 PMID: 37777579
- Saptarshi Sinha, .et al. , Exp Cell Res, 2022, Nov 1;420(1):113338 PMID: 36075449
- Subhajit Chatterjee, .et al. , J Cancer Res Clin Oncol, 2022, Dec;148(12):3521-3535 PMID: 35962813
- Yuki Uchihara, .et al. , Mol Cell, 2022, Jul 21;82(14):2557-2570 PMID: 35594857
- Ji-Ye Kim, .et al. , Cell Death Dis, 2022, Mar 15;13(3):239 PMID: 35293383
- Emad Matanes, .et al. , Front Oncol, 2021, Oct 27;11:745981 PMID: 34778062
- Shino Endo, .et al. , Cancer Res Commun, 2021, 1(2): 90-105
- Yan Baglo, .et al. , Transl Oncol, 2021, Nov;14(11):101198 PMID: 34418731
- Joseph M Gozgit, .et al. , Cancer cell, 2021, Jul 22;S1535-6108(21)00340-8 PMID: 34375612
- Sefinew Molla, .et al. , DNA Repair (Amst), 2021, Jun 10;105:103157 PMID: 34144488
- Jianming Wang, .et al. , Cell Rep, 2021, Feb 16;34(7):108759 PMID: 33596418
- Ai Ito, .et al. , Biogerontology, 2021, Feb;22(1):119-131 PMID: 33216250
- Tim J Wigle, .et al. , Cell Chem Biol, 2020, Jul 16;27(7):877-887 PMID: 32679093
- Ali Divan, .et al. , Pharmacol Res Perspect, 2020, Apr; 8(2): e00586 PMID: 32342655
- Jianwei Dou, .et al. , J Sep Sci, 2020, Dec 4 PMID: 33275824
- Sai Dimple Manavitha Gullipalli, .et al. , Int. J. Adv. Pharm. Biotech, 2020, 6(2) 01-08
- Chao Zhang, .et al. , J Atheroscler Thromb, 2020, Sep 25 PMID: 32981917
- Wigle TJ, .et al. , SLAS Discov, 2019, Dec 19:2472555219883623 PMID: 31855104
- Wang Q, .et al. , Cancer Med, 2019, Dec 21 PMID: 31863638
- Molla S, .et al. , Pathol Oncol Res, 2019, Nov 25 PMID: 31768967
- Alvin Z.Lu, .et al. , Biochem Pharmacol, 2019, May 7. pii: S0006-2952(19)30171-6 PMID: 31075269
- Bian C, .et al. , Nat Commun, 2019, Feb 11;10(1):693 PMID: 30741937
- HC de Silva, .et al. , Cell Mol Life Sci, 2019, 1-16 PMID: 30725116
- Kamada Y, .et al. , Fitoterapia, 2018, Sep;129:94-101 PMID: 29928967
- 2018, .et al. , FEBS Open Bio, 2018, Jun; 8(6): 1001-1012 PMID: 29928579
- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
- Hiro Sato, .et al. , Nat Commun, 2017, 8: 1751 PMID: 29170499
- Charles-André Philip, .et al. , BMC Cancer, 2017, 17: 638 PMID: 28886696
- Rulina AV, .et al. , Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
- 氯化小檗碱最近被发现对心血管系统具有多种有益效果,并具有显著的抗炎活性。小檗碱能有效降低LPS刺激的巨噬细胞内的超氧化物水平。小檗碱通过选择性抑制gp91phox表达和增强SOD活性,从而恢复细胞的氧化还原平衡。
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
- Celastrol 是一种从中国的雷公藤(T. wilfordii)中提取的三萜类抗氧化化合物。在一项关于大鼠肝脏脂质过氧化的独立实验中,celastrol 的 IC50 值为 7 微摩尔,其抗氧化能力约为 α-生育酚 的 15 倍。
- Xuechun Wang, .et al. , Int J Mol Sci, 2023, Mar 8;24(6):5204 PMID: 36982279
- R. San Gil, .et al. , bioRxiv, 2020, Jan
- Abdin AA, .et al. , Eur J Pharmacol., 2014, 742:102-12 PMID: 25218987
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Bcl-2 Inhibitor
ABT-737 是一种广谱 Bcl-2 抑制剂。IC50 值从 192 nM(前B细胞系 Hal-01)到小于 10 μM(Nalm-6、K562 和 HL-60)。- Jung Mo Lee, .et al. , Yonsei Med J, 2022, Jan;63(1):16-25 PMID: 34913280
- AidaVarela-Moreira, .et al. , Int J Pharm, 2022, Apr 25;618:121638 PMID: 35257802
- Daniel F R Boehmer, .et al. , Sci Immunol, 2021, Jul 16;6(61) PMID: 34272227
- Shivani Arora, .et al. , Med, 2021, 2,1-13
- Ying Ji, .et al. , Nat Commun, 2020, Aug 25;11(1):4249 PMID: 32843618
- Birgit Ritschka, .et al. , Genes Dev, 2020, Apr 1;34(7-8):489-494 PMID: 32139422
- Hiroki Akiyama, .et al. , Cancers, 2020, 12 (2) PMID: 32050632
- Hsu CC, .et al. , Arch Oral Biol, 2020, Mar;111:104653 PMID: 31935534
- Gupta VK, .et al. , Apoptosis, 2020, Feb;25(1-2):135-150 PMID: 31867678
- Meikle V, .et al. , Antimicrob Agents Chemother, 2018, Nov 12. pii: AAC.01846-18 PMID: 30420480
- Chauhan D, .et al. , Cell Rep, 2018, Nov 27;25(9):2354-2368.e5 PMID: 30485805
- Jose Mario Gonzalez-Meljem, .et al. , Nat Commun, 2017, 8: 1819 PMID: 29180744
- Zhang C, .et al. , J Biol Chem, 2017, Sep 8;292(36):15105-15120 PMID: 28673964
- Eun Young Kim, .et al. , Neoplasia, 2017, Apr; 19(4): 354-363 PMID: 28319809
- Masayoshi Toge, .et al. , Int J Oncol., 2015, Apr;46(4):1844-8 PMID: 25647738
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glucocorticoid receptor agonist
地塞米松是一种强效的合成糖皮质激素类固醇药物。它具有抗炎和免疫抑制作用。其效力约为天然激素氢化可的松的20-30倍,以及强的松的4-5倍。- Ken Kobayashi, .et al. , Cell Tissue Res, 2022, Sep;389(3):501-515 PMID: 35748981
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Emodin 是一种泻药树脂,来源于大黄、鼠李和日本虎杖(Fallopia japonica)。它属于一类名为蒽醌的化合物,这些化合物显示出抗炎和抗癌效果。
- Sakanashi M, .et al. , Circ J. , 2013, 77(7):1827-37. PMID: 23615023
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Topoisomerase II inhibitor
依托泊苷与DNA和拓扑异构酶II(帮助DNA解旋)形成三元复合物,阻止DNA链的重新连接,并因此导致DNA链断裂。因此,这会导致DNA合成出错,并促进癌细胞的凋亡。- Bageshri Naimish Nanavati, .et al. , Curr Biol, 2024, Sep 9;34(17):4081-4090 PMID: 39153481
- Wan J Gan, .et al. , Cytoskeleton (Hoboken), 2024, Jul 10 PMID: 38984538
- Wan J. Gan, .et al. , bioRxiv, 2024, March 10
- Zoya Mann, .et al. , Mol Biol Cell, 2024, Jan 1; 35(1) PMID: 37903230
- Bageshri Naimish Nanavati, .et al. , bioRxiv, 2023, Feb 23 PMID: 36865131
- Sibei Wang, .et al. , Molecules, 2023, Jan 19;28(3):1016 PMID: 36770683
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Chen JC, .et al. , Biomolecules, 2019, Sep 9;9(9) PMID: 31505885
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Calhelha RC, .et al. , Analyst, 2017, Oct 23;142(21):4124-4141 PMID: 28991301
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ERRα and ERRγ inverse agonist
Kaempferol 被发现能够抑制牛主动脉肌球蛋白轻链激酶,其抑制常数 Ki 为 0.3-0.5 微米。此外,Kaempferol 还能通过一条新的 ERK-NFκB-cMyc-p21 通路抑制 VEGF 表达和体外血管生成。- Asmaa R. Abdel-Hamed, .et al. , J Med Chem Sci, 2023, 6: 250-268
- A O Hamouda, .et al. , Eur Rev Med Pharmacol Sci, 2022, Dec;26(23):8644-8659 PMID: 36524484
- 盐酸二甲双胍是一种大鸟嘌呤类降糖药,用于治疗不对饮食调整做出反应的非胰岛素依赖型糖尿病。
- Matthew A Schaller, .et al. , JCI Insight, 2021, Sep 22;6(18):e148003 PMID: 34357881
- Matthew A. Schaller, .et al. , bioRxiv, 2021, January 21
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ALK Inhibitor
TAE684 是一种 ALK 抑制剂,同时也是 LRRK2 激酶活性的强效抑制剂(对野生型 LRRK2 的 IC(50) 为 7.8nM,对 G2019S 突变体的 IC(50) 为 6.1nM)。- Yue Guo, .et al. , Cell Biosci, 2022, Dec 30;12(1):210 PMID: 36585695
- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Li T, .et al. , Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
- Parthenolide((-)-Parthenolide)是一种天然存在于小白菊(Tanacetum parthenium)中的倍半萜内酯。
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HMG-CoA reductase inhibitor
Pitavastatin Calcium 是一种与酶 HMGCR (HMG-CoA reductase) 竞争的抑制剂,能够减少 LDL cholesterol 的合成。- Weizhen Chen, .et al. , Biomaterials, 2021, 280:121260 PMID: 34823885
- Karis Tutuska, .et al. , Cell Death Dis, 2020, Apr; 11(4): 274 PMID: 32332697
- D Jarmuzek, .et al. , J Photochem Photobiol A Chem, 2019, November
- Marwan Ibrahim Abdullah, .et al. , Sci Rep, 2017, 7: 8090 PMID: 28808351
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PLA inhibitor
Polydatin 通过改善微循环和抑制血小板聚集,保护脑细胞免受缺血性损伤。此外,polydatin 抑制内皮细胞在脂多糖刺激下的 ICAM-1 表达;它还减轻了白细胞与内皮细胞之间的粘附。- Darshika Pathiraja, .et al. , Food Chem, 2023, May 1;407:135145 PMID: 36521391
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mTOR Inhibitor
PP242 是一种强效且选择性的 mTOR 抑制剂,能够抑制 mTORC1 和 mTORC2。- Nobuyuki Kondo, .et al. , JCI Insight, 2023, Dec 22;8(24):e173688 PMID: 37917191
- Hiroshi Fukamachi, .et al. , J Exp Clin Cancer Res, 2019, 38:127 PMID: 30866995
- Fuse MJ, .et al. , Mol Cancer Ther, 2017, Oct;16(10):2130-2143 PMID: 28751539
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MAO-B inhibitor
Quercetin 抑制多种酶系统,包括酪氨酸蛋白激酶、磷脂酶A2、磷酸二酯酶、线粒体ATP酶、PI 3-激酶和蛋白激酶C。 -
MAO-B inhibitor
槲皮素能够抑制多种酶系统,包括酪氨酸蛋白激酶、磷脂酶A2、磷酸二酯酶、线粒体ATP酶、PI 3-激酶和蛋白激酶C。 - Resveratrol 拥有广泛的作用目标,包括环氧合酶(即 COX,IC50=1.1 μM)、脂氧合酶(LOX,IC50=2.7 μM)、激酶、sirtuins 及其他蛋白质。它具有抗癌、抗炎、降低血糖以及其他有益的心血管效果。
- Zeynep Kasap Acungil, .et al. , Mol Neurobiol, 2024, Sep 24 PMID: 39316354
- Wafa Naji Shnaikat, .et al. , Iraqi J Pharm Sci, 2023, 31(Suppl.):92-99
- Ha T. Tran, .et al. , PLoS One, 2017, 12(3): e0173373 PMID: 28278187
- Salidroside(Rhodioloside)是一种在植物红景天(Rhodiola rosea)中发现的酪醇葡萄糖苷。它被认为是该植物具有抗抑郁和抗焦虑作用的化合物之一,与rosavin一起。
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HMG-CoA reductase inhibitor
Simvastatin(MK 733)是一种与HMG-CoA还原酶具有竞争性抑制作用的药物,其Ki值为0.2 nM。 -
HDAC inhibitor
Valproic acid sodium salt (Sodium Valproate) 是一种 HDAC 抑制剂,其 IC50 在 0.5 至 2 mM 范围内,同时抑制 HDAC1(IC50,400 μM),并诱导 HDAC2 的蛋白酶体降解。 -
RTK inhibitor
舒尼替尼是一种口服的小分子多靶点受体酪氨酸激酶(RTK)抑制剂,用于治疗肾细胞癌(RCC)和对伊马替尼耐药的胃肠间质瘤(GIST)。- Sophie J. Bakri, .et al. , PLoS One, 2024, 19(6): e0304782 PMID: 38833447
- Chern Ein Oon, .et al. , World J Gastrointest Oncol, 2023, May 15;15(5):810-827 PMID: 37275453
- Rachel K Toth, .et al. , Cells, 2022, Mar 16;11(6):1006 PMID: 35326457
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Thibaut Fourniols, .et al. , Int J Pharm, 2020, Jun 30;584:119337 PMID: 32371002
- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
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CXCR4 antagonist
Plerixafor 是一种免疫刺激剂,用于增殖造血干细胞,并且它是一种 趋化因子受体-4拮抗剂,用于动员造血干细胞进行移植。- Federico Antoniciello, .et al. , Front Mol Biosci, 2023, May 11;9:887564 PMID: 35647033
- Mei Zheng, .et al. , Biomed Pharmacother, 2022, Jun;150:112996 PMID: 35462338
- Asiedu KO, .et al. , EJNMMI Res, 2018, Dec 13;8(1):109 PMID: 30547233
- Kingsley O. Asiedu, .et al. , Clin Cancer Res, 2017, Jun 1; 23(11): 2759-2768 PMID: 27965305
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MEK inhibitor
U0126-EtOH 是一种同时抑制 MEK1 和 MEK2 的抑制剂,其半抑制浓度(IC50)分别为 72 nM 和 58 nM。- Ji Wang, .et al. , Acta Pharmacol Sin, 2024, Nov 20 PMID: 39567750
- Hanna Galganska, .et al. , Cell Mol Life Sci, 2021, Dec;78(24):8229-8242 PMID: 34741187
- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
- Byungki Jang, .et al. , Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
- Choe YJ, .et al. , Int J Oncol., 2014, 44(3):761-8. PMID: 24366007
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HDAC inhibitor
Vorinostat 是一种 HDACs 抑制剂,它抑制去乙酰化作用,导致 高乙酰化组蛋白 和转录因子的积累。- Masahiro Yamada, .et al. , Int J Hematol, 2024, Sep;120(3):325-336 PMID: 38954186
- Amy E Neely, .et al. , Commun Biol, 2023, Jun 23;6(1):664 PMID: 37353594
- Ting-Yu Chang, .et al. , Biomed Pharmacother, 2021, Jun;138:111485 PMID: 33740521
- David Diaz-Carballo, .et al. , Commun Biol, 2021, Mar 3;4(1):276 PMID: 33658617
- Arshdeep Singh, .et al. , Eur J Med Chem, 2021, Apr 5;215:113169 PMID: 33588178
- Shariful Islam, .et al. , Blood Adv, 2020, 4(20): 5297-5310 PMID: 33108458
- Giovanni Bocci, .et al. , ACS Pharmacol Transl Sci, 2020, Oct 14
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PI3K/mTOR Inhibitor
PF-04691502 是一种 PI3K/mTOR 激酶抑制剂,同时也是针对 磷脂酰肌醇3激酶(PI3K) 和 哺乳动物雷帕霉素靶蛋白(mTOR) 的药物,作用于 PI3K/mTOR 信号通路。- Yusuke Murase, .et al. , Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
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JAK1/2 Inhibitor
INCB018424 是一种强效且选择性的 Janus-associated kinase (JAK) 1 和 2 抑制剂,其半抑制浓度(IC50)分别为 JAK1 2.7 nM、JAK2 4.5 nM 和 JAK3 332 nM。- Meenu Kesarwani, .et al. , Blood Adv, 2024, Jun 11;8(11):2765-2776 PMID: 38531054
- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Daniel Doheny, .et al. , Oncogene, 2020, Oct;39(42):6589-6605 PMID: 32929154
- Rasmus Siersbek, .et al. , Cancer cell, 2020, Jul 6;S1535-6108(20)30311-1 PMID: 32679107
- Brittany M. Duggan, .et al. , Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Kagoya Y, .et al. , Blood., 2014, Nov 6;124(19):2996-3006 PMID: 25217696
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PDGFR/FLT3 Inhibitor
Crenolanib (CP-868596) 是一种口服生物利用度高的选择性小分子抑制剂,针对 PDGFR 酪氨酸激酶 进行抑制,能在皮克摩尔浓度下同时抑制 PDGFRA 和 PDGFRB。- N Naganna, .et al. , EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
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Autophagy/PI3K Inhibitor
3-甲基腺嘌呤是III类磷脂酰肌醇3激酶(PI 3-激酶)的抑制剂。- Yu-Chih Hsu, .et al. , Int J Med Sci, 2023, 20(4): 444-454 PMID: 37057216
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Protein translocation Inhibitor
Brefeldin A 阻断 ADP-核糖基化因子 与 高尔基体 的结合,并抑制 GDP-GTP 交换。 -
CXCR4 antagonist
AMD 070 是一种 CXCR4趋化因子受体拮抗剂。- Uchida D, .et al. , Oncol Rep, 2018, Jul;40(1):303-308 PMID: 29749473
- Mamoru Morimoto, .et al. , BMC Cancer, 2016, 16: 305 PMID: 27175473
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K+/Na+/Ca+ Channel Blocker
Dronedarone Hydrochloride 是一种非碘化的 阿米奥达隆衍生物,能够抑制 Na+、K+ 和 Ca2+ 电流。 -
JAK1/2 inhibitor
Ruxolitinib sulfate(INCB018424 sulfate)是首个进入临床的强效、选择性 JAK1/2 抑制剂,其 IC50 值分别为 3.3 nM/2.8 nM,并且对 JAK1/2 比 JAK3 的选择性高出 130 倍以上。 -
JAK inhibitor
磷酸鲁索替尼是鲁索替尼的磷酸盐形式,这是一种口服生物可用的Janus相关激酶(JAK)抑制剂,具有潜在的抗肿瘤和免疫调节活性。 -
CXCR1/CXCR2 antagonist
SCH527123 是一种强效且选择性的人类 CXCR1 和 CXCR2 受体拮抗剂,其 IC50 分别为 42 nM 和 3 nM。- Ruijie Zhang, .et al. , Int J Oncol, 2022, May;60(5):50 PMID: 35315502
- Fu S, .et al. , Int J Oncol, 2018, Jul;53(1):349-357 PMID: 29749433
- Fu S, .et al. , Anticancer Res, 2018, Nov;38(11):6271-6279 PMID: 30396947
- Amiodarone hydrochloride 是一种抗心律失常药物,用于抑制 ATP敏感性钾通道,其半抑制浓度(IC50)为19.1微摩尔。
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neuromuscular blocking agent
Cisatracurium besylate (51W89) 是一种非去极化神经肌肉阻断剂,通过抑制神经肌肉传导来对抗乙酰胆碱的作用。 -
CXCR4 antagonist
AMD 3465 是一种强效、选择性的 CXCR4 拮抗剂。- Kentaro Suzuki, .et al. , Sci Rep, 2019, 9: 15284