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TAK-779

编号: 25049
Cas号: 229005-80-5
纯度: 98% Min.

TAK-779 is a C-C chemokine receptor type 5 (CCR5) receptor antagonist potentially for the treatment of HIV infection. Treatment with TAK-779 reduced incidence and severity of experimental autoimmune encephalomyelitis. It strongly inhibited migration of CXCR3/CCR5 bearing CD4+, CD8+ and CD11b+ leukocytes to the CNS. TAK-779 did not reduce proliferation of anti-myelin oligodendrocyte glycoprotein T cells, the production of IFN-gamma by T cells or CXCR3 expression on T cells. In addition, TAK-779 did not affect production of IL-12 by antigen-presenting cells, CCR5 induction on T cells and the potential of myelin oligodendrocyte glycoprotein-specific T cells to transfer experimental autoimmune encephalomyelitis.

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化学信息

名称TAK-779
Iupac 化学名称N,N-dimethyl-N-(4-(2-(p-tolyl)-6,7-dihydro-5H-benzo[7]annulene-8-carboxamido)benzyl)tetrahydro-2H-pyran-4-aminium chloride
同义词TAK-779, TAK 779, TAK779 Chloride;
英文同义词TAK-779, TAK 779, TAK779 Chloride;
分子式C33H39ClN2O2
分子量531.13
SmileC[N+](C)(CC1=CC=C(NC(C2=CC3=CC(C4=CC=C(C)C=C4)=CC=C3CCC2)=O)C=C1)C5CCOCC5.[Cl-]
InChiKeyVDALIBWXVQVFGZ-UHFFFAOYSA-N
InChiInChI=1S/C33H38N2O2.ClH/c1-24-7-11-27(12-8-24)28-14-13-26-5-4-6-29(22-30(26)21-28)33(36)34-31-15-9-25(10-16-31)23-35(2,3)32-17-19-37-20-18-32;/h7-16,21-22,32H,4-6,17-20,23H2,1-3H3;1H
Cas号229005-80-5
相关CAS号

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包装价格库存纯度备货期
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Request Bulk Quote Download MSDS 电话 : +86-177 0271 9238   Email : sales@sun-shinechem.com
外观性状类白色固体
纯度98% Min.
存储 0-4℃,可保存几天到几周;-20℃,可保存 几个月。
可溶性溶于DMSO等有机溶剂
处理方式
运输条件可以在室温下进行运输。
海关编码
Coming soon.
Targets
Mechanism
Cell study
Animal study
Clinical study

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2: De Clercq E. The emerging role of fusion inhibitors in HIV infection. Drugs R D. 1999 Nov;2(5):321-31. doi: 10.2165/00126839-199902050-00010. PMID: 10728472.


3: Dragic T, Trkola A, Thompson DA, Cormier EG, Kajumo FA, Maxwell E, Lin SW, Ying W, Smith SO, Sakmar TP, Moore JP. A binding pocket for a small molecule inhibitor of HIV-1 entry within the transmembrane helices of CCR5. Proc Natl Acad Sci U S A. 2000 May 9;97(10):5639-44. doi: 10.1073/pnas.090576697. PMID: 10779565; PMCID: PMC25881.


4: Shiraishi M, Aramaki Y, Seto M, Imoto H, Nishikawa Y, Kanzaki N, Okamoto M, Sawada H, Nishimura O, Baba M, Fujino M. Discovery of novel, potent, and selective small-molecule CCR5 antagonists as anti-HIV-1 agents: synthesis and biological evaluation of anilide derivatives with a quaternary ammonium moiety. J Med Chem. 2000 May 18;43(10):2049-63. doi: 10.1021/jm9906264. PMID: 10821717.


5: Zhang Y, Lou B, Lal RB, Gettie A, Marx PA, Moore JP. Use of inhibitors to evaluate coreceptor usage by simian and simian/human immunodeficiency viruses and human immunodeficiency virus type 2 in primary cells. J Virol. 2000 Aug;74(15):6893-910. doi: 10.1128/jvi.74.15.6893-6910.2000. PMID: 10888629; PMCID: PMC112207.


6: Baba M, Miyake H, Okamoto M, Iizawa Y, Okonogi K. Establishment of a CCR5-expressing T-lymphoblastoid cell line highly susceptible to R5 HIV type 1. AIDS Res Hum Retroviruses. 2000 Jul 1;16(10):935-41. doi: 10.1089/08892220050058344. PMID: 10890354.


7: De Clercq E. Novel compounds in preclinical/early clinical development for the treatment of HIV infections. Rev Med Virol. 2000 Jul-Aug;10(4):255-77. doi: 10.1002/1099-1654(200007/08)10:4<255::aid-rmv282>3.0.co;2-6. Erratum in: Rev Med Virol 2000 Sep-Oct;10(5):349. PMID: 10891872.


8: Trkola A, Ketas TJ, Nagashima KA, Zhao L, Cilliers T, Morris L, Moore JP, Maddon PJ, Olson WC. Potent, broad-spectrum inhibition of human immunodeficiency virus type 1 by the CCR5 monoclonal antibody PRO 140. J Virol. 2001 Jan;75(2):579-88. doi: 10.1128/JVI.75.2.579-588.2001. PMID: 11134270; PMCID: PMC113953.


9: Spenlehauer C, Gordon CA, Trkola A, Moore JP. A luciferase-reporter gene- expressing T-cell line facilitates neutralization and drug-sensitivity assays that use either R5 or X4 strains of human immunodeficiency virus type 1. Virology. 2001 Feb 15;280(2):292-300. doi: 10.1006/viro.2000.0780. PMID: 11162843.


10: Cormier EG, Tran DN, Yukhayeva L, Olson WC, Dragic T. Mapping the determinants of the CCR5 amino-terminal sulfopeptide interaction with soluble human immunodeficiency virus type 1 gp120-CD4 complexes. J Virol. 2001 Jun;75(12):5541-9. doi: 10.1128/JVI.75.12.5541-5549.2001. PMID: 11356961; PMCID: PMC114266.


11: Huang XQ, Jiang HL, Luo XM, Chen KX, Ji RY, Cao Y, Pei G. Building three- dimensional structures of HIV-1 coreceptor CCR5 and its interaction with antagonist TAK779 by comparative molecular modeling. Acta Pharmacol Sin. 2000 Jun;21(6):521-8. PMID: 11360686.


12: Kanbara K, Sato S, Tanuma J, Tamamura H, Gotoh K, Yoshimori M, Kanamoto T, Kitano M, Fujii N, Nakashima H. Biological and genetic characterization of a human immunodeficiency virus strain resistant to CXCR4 antagonist T134. AIDS Res Hum Retroviruses. 2001 May 1;17(7):615-22. doi: 10.1089/088922201300119716. PMID: 11375057.


13: De Clercq E. New developments in anti-HIV chemotherapy. Curr Med Chem. 2001 Nov;8(13):1543-72. doi: 10.2174/0929867013371842. PMID: 11562282.


14: Esté JA. TAK-779 (Takeda). Curr Opin Investig Drugs. 2001 Mar;2(3):354-6. PMID: 11575704.


15: Gorry PR, Bristol G, Zack JA, Ritola K, Swanstrom R, Birch CJ, Bell JE, Bannert N, Crawford K, Wang H, Schols D, De Clercq E, Kunstman K, Wolinsky SM, Gabuzda D. Macrophage tropism of human immunodeficiency virus type 1 isolates from brain and lymphoid tissues predicts neurotropism independent of coreceptor specificity. J Virol. 2001 Nov;75(21):10073-89. doi: 10.1128/JVI.75.21.10073-10089.2001. PMID: 11581376; PMCID: PMC114582.


16: De Clercq E, Schols D. Inhibition of HIV infection by CXCR4 and CCR5 chemokine receptor antagonists. Antivir Chem Chemother. 2001;12 Suppl 1:19-31. PMID: 11594685.


17: Bannert N, Farzan M, Friend DS, Ochi H, Price KS, Sodroski J, Boyce JA. Human Mast cell progenitors can be infected by macrophagetropic human immunodeficiency virus type 1 and retain virus with maturation in vitro. J Virol. 2001 Nov;75(22):10808-14. doi: 10.1128/JVI.75.22.10808-10814.2001. PMID: 11602722; PMCID: PMC114662.


18: Takashima K, Miyake H, Furuta RA, Fujisawa JI, Iizawa Y, Kanzaki N, Shiraishi M, Okonogi K, Baba M. Inhibitory effects of small-molecule CCR5 antagonists on human immunodeficiency virus type 1 envelope-mediated membrane fusion and viral replication. Antimicrob Agents Chemother. 2001 Dec;45(12):3538-43. doi: 10.1128/AAC.45.12.3538-3543.2001. PMID: 11709336; PMCID: PMC90865.


19: Brelot A, Alizon M. HIV-1 entry and how to block it. AIDS. 2001;15 Suppl 5:S3-11. doi: 10.1097/00002030-200100005-00002. PMID: 11816172.


20: Gorry PR, Taylor J, Holm GH, Mehle A, Morgan T, Cayabyab M, Farzan M, Wang H, Bell JE, Kunstman K, Moore JP, Wolinsky SM, Gabuzda D. Increased CCR5 affinity and reduced CCR5/CD4 dependence of a neurovirulent primary human immunodeficiency virus type 1 isolate. J Virol. 2002 Jun;76(12):6277-92. doi: 10.1128/jvi.76.12.6277-6292.2002. PMID: 12021361; PMCID: PMC136234.
17920529.

化学结构

25049 - TAK-779 | CAS 229005-80-5

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