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5.34337

Sigma-Aldrich

HIV Inhibitor, CADA

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Synonym(s):
HIV Inhibitor, CADA, 1-Benzyl-7-methylene-5,9-ditosyl-5,9-diaza-azoniacyclododecan-1-ium chloride, CD4 Inhibitor, CADA
Empirical Formula (Hill Notation):
C31H39N3O4S2 · xHCl
Molecular Weight:
581.79 (free base basis)

assay

≥98% (HPLC)

Quality Level

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 10 mg/mL
water: insoluble

storage temp.

−20°C

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HIV Inhibitor, CADA

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HMTase Inhibitor IV, UNC0638

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RPN13 Inhibitor, RA190

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HIF Inhibitor V

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥97% (HPLC)

assay

≥99% (HPLC)

form

solid

form

powder

form

solid

form

powder

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

−20°C

storage temp.

−20°C

storage temp.

−20°C

storage temp.

2-8°C

solubility

DMSO: 10 mg/mL, water: insoluble

solubility

DMSO: 10 mg/mL

solubility

water: 5 mg/mL, DMSO: 50 mg/mL

solubility

DMSO: 50 mg/mL

General description

A cell-permeable macrocyle cyclotriazadisulfonamide derivative compound that inhibits HIV replication (IC50 = 300 nM to 3.3 µM) and entry into cells by blocking co-translational translocation of nascent CD4 across endoplasmic reticulum membranes. Its action appears to be highly selective in reducing the expression of human CD4 and it does not affect the level of any other cell surface marker studied. Does not affect CD4 mRNA levels in cells. Shown to be effective against HIV-1 subtypes A to H, AE, and O and human herpesvirus 7 (HHV-7; IC50, 300 nM to 1.5 µM) in T-cell lines and PBMCs. Also reported to block X4 HIV-1 NL4.3 and R5 SIVmac251 laboratory strains infection in human T cells. Can act synergistically with cellulose acetate phthalate (CAP) and other anti-HIV drugs to inhibit HIV-1 and SIV infections.

Biochem/physiol Actions

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

Vermeire, K., et al. 2008. Curr. HIV Res.6, 246.
Bell, T. W., et al. 2006. J. Med. Chem.49, 1291.
Vermeire, K., et al. 2004. AIDS.18, 2115.
Vermeire, K., et al. 2002. Virology.302, 342.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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