Disease Area, Infectious Disease I
Product Name: ABT-378 (Lopinavir) l HIV-1 protease inhibitor (#C2378-10)
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Lopinavir (ABT-378), designed in response to Val82 mutant strains of HIV [1], is a potent inhibitor of HIV
protease with Ki of 1.3-3.6 pM. Lopinavir inhibits replication of HIV-1 with an EC50 of 6-17 nM. [2]
Ritonavir was found to inhibit the metabolism of lopinavir with no other antagonistic effects; therefore
lopinavir's drug exposure can be enhanced by co-formulation with ritonavir. In the presence of 50% human
serum, the mean EC50 of lopinavir for five laboratory HIV-1 isolates ranged from 65 to 289 nM. [3]
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Details
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Chemical Formula:
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C37H48N4O5
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CAS No.:
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192725-17-0
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Molecular weight:
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628.8
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Purity:
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> 98%
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Appearance:
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White
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Chemical name:
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(S)-N-((2S,4S,5S)-5-(2-(2,6-dimethylphenoxy)acetamido)-4-hydroxy-1,6-
diphenylhexan-2-yl)-3-methyl-2-(2-oxo-tetrahydropyrimidin-1(2H)-yl)butanamide
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Solubility:
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Up to 100 mM in DMSO
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Synonyms:
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ABT-378, ABT378, Lopinavir
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Storage:
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For longer shelf life, store solid powder at 4oC desiccated, or DMSO solution
at -20oC
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1. Stoll et al., X-ray Crystallographic Structure of ABT-378 (Lopinavir) Boudn to HIV-1 Protease. Bioorg. Med.
Chem. 2002, 10, 2803-2806. Pubmed ID: 12057670
2. Sham et al., ABT-378, a Highly Potent Inhibitor of the Human Immunodeficiency Virus Protease.
Antimicrob. Agents Chemother. 1998, 42(12), 3218-3224. Pubmed ID: 9835517
3. Qazi et al., Lopinavir/ritonavir (ABT-378/r). Expert Opin. Pharmacother. 2002, 3(2), 315-327.
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Product Name: AMD3100 (Plerixafor) l HIV-1 entry blocker (#C2310-5)
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Plerixafor (AMD3100) is a bis-tetraazadecane-based, selective inhibitor of human immunodeficiency virus. It
is inhibitory to the replication of various HIV-1 and HIV-2 strains in various cell lines at an EC50 of
1-10 ng/mL, about 100,000-fold lower than cytotoxic concentrations (>500 uM/mL). [1] Plerixafor shows
inhibition to HIV-1(IIIB) and several clinical HIV-1 isolates at an EC50 of less than 1 ng/mL.
Plerixafor has been shown to be active in HIV strains resistant to reverse transcriptase inhibitors AZT, DDI,
3TC, aAPA, and TIBO. [2]
Plerixafor blocks HIV-1 entry and membrane fusion via the CXCR4 co-receptor, but not via CCR5. It also
prevents monoclonal antibody 12G5 from binding to CXCR4. Entry into CXCR-expressing cells was strongly
inhibited by Plerixafor at IC50 values of 0.01-0.1 nM. [3] Plerixafor demonstrates a specific antagonism of the
interaction between chemokine SDF-1 and CXCR4, reducing severity of inflammation in CIA models. [4]
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Details
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Chemical Formula:
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C28H54N8
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CAS No.:
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110078-46-1, 155148-31-5
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Molecular weight:
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502.78
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Purity:
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> 98%
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Appearance:
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White
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Chemical name:
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1,1'-[1,4-Phenylenebis(methylene)]bis [1,4,8,11-tetraazacyclotetradecane]
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Solubility:
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Up to 100 mM in water in DMSO
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Synonyms:
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AMD3100, AMD 3100, Plerixafor, Mozobil, bicyclam JM-2987
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Storage:
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For longer shelf life, store solid powder at 4oC desiccated, or DMSO solution
at -20oC
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References
1. De Clercq et al., Highly potent and selective inhibition of human immunodeficiency virus by the bicyclam
derivative JM3100. Antimicrob. Agents Chemother. 1994, 38(4), 668-674. Pubmed ID: 7913308
2. Este et al., Antiviral activity of the bicyclam derivative JM3100 against drug-resistant strains of human
immunodeficiency virus type 1. Antiviral Res. 1996, 29, 297-307. Pubmed ID: 8739608
3. Donzella et al., AMD3100, a small molecule inhibitor of HIV-1 entry via the CXCR4 co-receptor. Nature
Med. 1998, 4(1), 72-77. Pubmed ID: 9427609
4. Matthys et al., AMD3100, a potent and specific antagonist of the stromal cell-derived factor-1 chemokine
receptor CXCR4, inhibits autoimmune joint inflammation in IFN-gamma receptor-deficient mice. J.
Immunol. 2001, 167(8), 4686-4692. Pubmed ID:8739608
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Product Name: BMS-207147 (Ravuconazole) | antifungal compound (#C2207-5)
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BMS207147 is a orally-available, triazole-based antifungal with MICs 2- to 4-fold more potent than
itraconazole and 40-fold more active than fluconazole against yeasts. In all but 9 of 116 Candida strains
tested, BMS207147 had MICs of < 0.5 ug/mL. [1] In oral mouse studies, BMS207147 was shown to have a
3-fold longer half-life than itraconazole. [2]
In 541 clinical isolates of Cryptococcus neoformans, BMS207147 again proved to be more potent than
itraconazole and fluconazole (0.25 ug/mL vs 0.5 ug/mL and 8 ug/mL). [3]
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Details
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Chemical Formula:
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C22H17F2N5OS
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CAS No.:
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182760-06-1
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Molecular weight:
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437.47
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Purity:
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> 98%
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Appearance:
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White
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Chemical name:
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4-[2-[(2R,3R)-3-(2,4-difluorophenyl)-3-hydroxy-4-(1,2,4-triazol-1-yl)butan-2-yl]
-1,3-thiazol-4-yl]benzonitrile
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Solubility:
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Up to 22 mM in DMSO
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Synonyms:
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BMS-207147, BMS 207147, BMS207147, Ravuconazole, ER-30346
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Storage:
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For longer shelf life, store solid powder at 4oC desiccated, or DMSO solution
at -20oC
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References
1. Fung-Tomc et al., In vitro activity of a new oral triazole, BMS-207147 (ER-30346). Antimicrob. Agents
Chemother. 1998, 42(2), 313-318. Pubmed ID: 9527778
2. Yamazumi et al., In vitro activities of BMS-207147 against over 600 contemporary clinical bloodstream
isolates of Candida species from the SENTRY Antimicrobial Surveillance Program in North America and
Latin America. Antimicrob. Agents Chemother. 1999, 43(9), 2236-2239. Pubmed ID: 10471571
3. Yamazumi et al., In vitro activities of ravuconazole (BMS-207147) against 541 clinical isolates of
Cryptococcus neoformans. Antimicrob. Agents Chemother. 2000, 44(10), 2883-2886. Pubmed ID: 10991880
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Product Name: BMS-232632 (Atazanavir) | HIV-1 protease inhibitor (#C2232-5)
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Atazanavir (BMS-232632) is an orally available, azapeptide human immunodeficiency virus type 1 (HIV-1)
protease inhibitor with EC50 of 2.6-5.3 nM, and EC90 of 9-15 nM. [1] Atazanavir has been shown to be
effective in HIV-1 strains resistant to other antivirals such as nelfinavir, saquinavir, and amprenavir.
Additionally, indinavir- and ritonavir-resistant strains are more six- to nine-fold more sensitive to atazanavir.
Atazanavir's is highly selective for HIV-1 protease and only exhibits cytotoxic effects in 6500- to 23000-fold
higher concentrations than is required for anti-HIV activity. Atazanavir has been shown to be additive or
synergistic with a number of different antiviral therapies without antagonistic anti-HIV activity or cytotoxicity.
[2, 3]
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Details
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Chemical Formula:
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C38H52N6O7
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CAS No.:
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198904-31-3, 229975-97-7
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Molecular weight:
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704.86
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Purity:
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> 99%
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Appearance:
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White
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Chemical name:
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2,5,6,10,13-Pentaazatetradecanedioic acid, 3,12-bis(1,1-dimethylethyl)
-8-hydroxy-4,11-dioxo-9-(phenylmethyl)-6-[[4-(2-pyridinyl)phenyl]methyl]-,
1,14-dimethyl ester, (3S,8S,9S,12S)-
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Solubility:
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Up to 100 mM in DMSO
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Synonyms:
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BMS-232632, BMS 232632, BMS232632, Atazanavir, Reyataz, CGP-73547
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Storage:
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For longer shelf life, store solid powder at 4oC desiccated, or DMSO solution
at -20oC
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References
1. Gong et al., In vitro resistance profile of the human immunodeficiency virus type 1 protease inhibitor
BMS-232632. Antimicrobial Agents Chemother. 2000, 44(9), 2319-2326. Pubmed ID: 10952574
2. Robinson et al., BMS-232632, a highly potent human immunodeficiency virus protease inhibitor that can
be used in combination with other available antiretroviral agents. Antimicrobial Agents Chemother. 2000,
44(8), 2093-2099. Pubmed ID: 10898681
3. Colonno et al., Activities of atazanavir (BMS-232632) against a large panel of human immunodeficiency
virus type 1 clinical isolates resistant to one or more approved protease inhibitors. Antimicrobial Agents
Chemother. 2003, 47(4), 1324-1333. Pubmed ID: 12654666
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