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TAK-779

Cat. No. M9135
TAK-779 Structure
Synonym:

Takeda 779; TAK779 Chloride

Size Price Availability Quantity
5mg USD 100  USD100 In stock
10mg USD 160  USD160 In stock
25mg USD 290  USD290 In stock
50mg USD 490  USD490 In stock
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Quality Control & Documentation
Biological Activity

TAK-779 is a potent and selective nonpeptide antagonist of CCR5, with a Ki of 1.1 nM for CCR5. TAK-779 strongly inhibited migration of CXCR3/CCR5 bearing CD4+, CD8+ and CD11b+ leukocytes to the CNS. TAK-779 effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.

In vivo, TAK-779 (10 mg/kg per day, s.c.) significantly prolongs the allograft survival of the rat intestinal transplantation model. 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. Treatment with TAK-779 reduced incidence and severity of experimental autoimmune encephalomyelitis.

Chemical Information
Molecular Weight 531.13
Formula C33H39ClN2O2
CAS Number 229005-80-5
Solubility (25°C) DMSO: ≥ 20 mg/mL
Water: ≥ 10 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Takama Y, et al. Transpl Immunol. Effects of a calcineurin inhibitor, FK506, and a CCR5/CXCR3 antagonist, TAK-779, in a rat small intestinal transplantation model.

[2] Ni J, et al. Br J Pharmacol. The chemokine receptor antagonist, TAK-779, decreased experimental autoimmune encephalomyelitis by reducing inflammatory cell migration into the central nervous system, without affecting T cell function.

[3] Baba M, et al. Proc Natl Acad Sci U S A. A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity.

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Keywords: TAK-779, Takeda 779; TAK779 Chloride supplier, CCR, inhibitors, activators


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