Tak 799
Tak 799 Basic information
- Product Name:
- Tak 799
- Synonyms:
-
- 2H-Oyran-4-aminium, N-((4-(((6,7-dihydro-2-(4-methylphenyl)-5H-benzocyclohepten-8-yl)carbonyl)amino)phenyl)methyl)tetrahydro-N,N-dimethyl-
- 2H-Pyran-4-aminium, N,N-dimethyl-N-(4-(((2-(4-methylphenyl)-6,7-dihydro-5H-benzocyclohepten-8-yl)carbonyl)amino)benzyl)tetrahydro-, chloride
- N,N-Dimethyl-N-(4-(((2-(4-methylphenyl)-6,7-dihydro-5H-benzocyclohepten-8-yl)carbonyl)amino)benzyl)tetrahydro-2H-pyran-4-aminium chloride
- Tak 799
- Takeda 779
- TAK 799 ;TAK 779
- TAK779;TAK 799;TAKEDA 779
- N,N-Dimethyl-N-[4-[[[2-(4-methylphenyl)-6,7-dihydro-5H-benzohepten-8-yl]carbonyl]amino]benzyl]tetrahydro-2H-pyran-4-aminium chloride
- CAS:
- 229005-80-5
- MF:
- C33H39N2O2.Cl
- MW:
- 531.136
- Mol File:
- 229005-80-5.mol
Tak 799 Chemical Properties
- storage temp.
- 2-8°C
- solubility
- H2O: soluble3mg/mL, clear (warmed)
- form
- powder
- color
- white to beige
- Water Solubility
- H2O: 3mg/mL, clear (warmed)
- InChIKey
- VDALIBWXVQVFGZ-UHFFFAOYSA-N
- SMILES
- C(=O)(NC1C=CC(=CC=1)C[N+](C)(C)C1CCOCC1)C1CCCC2C=CC(C3C=CC(C)=CC=3)=CC=2C=1.[Cl-]
Tak 799 Usage And Synthesis
Uses
TAK-779 has been used to inhibit CC chemokine ligand 5 (CCL5)– C-C chemokine receptor type 5 (CCR5) interaction in vitro in natural killer (NK) cytotoxicity assay. It has also been used as a blocker of CCR5 to study its effects and to evaluate the opening of the Panx-1 channels on peripheral blood mononuclear cells (PBMCs) isolated from human immunodeficiency virus (HIV)-infected individuals.
Biochem/physiol Actions
TAK-779 is a potent, dual antagonist at chemokine receptors C-C chemokine receptor type 2 (CCR2) and C-C chemokine receptor type 5 (CCR5) with IC50 = 1.4 nM at CCR5 and 2.3 nM at CCR2. Antagonists of both CCR2 and CCR5 such as TAK-779 have been investigated for treatment of viruses, rheumatoid arthritis, multiple sclerosis, and cancer. CCR5 is particularly targeted for anti-HIV therapy, since HIV entry into cells requires chemokine coreceptors CCR5 and C-X-C motif chemokine receptor 4 (CXCR4).
in vivo
TAK-779 (10 mg/kg per day, s.c.) significantly prolongs the allograft survival of the rat intestinal transplantation model. TAK-779 also decreases the number of CD4+ as well as CD8+ T cells in spleen, blood and recipient mesenteric lymph nodes (MLN)[2]. TAK-779 (150 μg per mouse, s.c.) supppresses the development of experimental autoimmune encephalomyelitis (EAE) in myelin oligodendrocyte glycoprotein (MOG)-immunized C57BL/6 mice. TAK-779 decreases the infiltration of CXCR3 and CCR5 bearing leukocytes into the spinal cord. TAK-779 does not alter myelin oligodendrocyte glycoprotein (MOG)-specific immune responses or affect the potential of MOG-specific T cells to transfer experimental autoimmune encephalomyelitis (EAE)[3].
IC 50
MIP-1α-CCR5: 1 nM (IC50, in CHO/CCR5 cells); MIP-1β-CCR5: 1 nM (IC50, in CHO/CCR5 cells); RANTES-CCR5: 1.4 nM (IC50, in CHO/CCR5 cells); MCP-1-CCR2b: 27 nM (IC50, in CHO/CCR5 cells); R5 HIV-1 (Ba-L): 1.2 nM (EC50, in MAGI-CCR5 cells); R5 HIV-1 (KK): 1.6 nM (EC50, in PBMCs); R5 HIV-1 (HHA): 3.2 nM (EC50, in PBMCs); R5 HIV-1 (CTV): 3.5 nM (EC50, in PBMCs); R5 HIV-1 (Ba-L): 3.7 nM (EC50, in PBMCs); R5 HIV-1 (Ba-L): 5.7 nM (EC90, in MAGI-CCR5 cells); R5 HIV-1 (HHA): 7.5 nM (EC90, in PBMCs); R5 HIV-1 (Ba-L): 12.8 nM (EC90, in PBMCs); R5 HIV-1 (KK): 20.8 nM (EC90, in PBMCs); R5 HIV-1 (CTV): 27 nM (EC90, in PBMCs); mCXCR3: 369 nM (IC50, in PBMCs)
storage
Store at -20°C
Tak 799Supplier
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- 0512-0512-13601744364 13601744364
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