UC-781
UC-781 (NSC 675186) is a highly potent and selective nonnucleoside reverse transcriptase inhibitor (NNRTI) of HIV-1 with an IC50 value of 5 nM. UC-781 is stable under low PH or various temperatures conditions. UC-781 has antiviral activity and resistance.
For research use only. We do not sell to patients.
- CAS No.: 178870-32-1
- Formula: C17H18ClNO2S
- Molecular Weight:335.85
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HIV-1 0.005 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MRC5 | IC50 |
>64 μM
Compound: UC781
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Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell growth after 72 hrs
Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell growth after 72 hrs
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[PMID: 25199582] |
| MRC5 | IC50 |
>64 μM
Compound: UC781
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Trypanocidal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC5 SV2 cells assessed as parasite growth inhibition after 168 hrs by beta-galactosidase assay
Trypanocidal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC5 SV2 cells assessed as parasite growth inhibition after 168 hrs by beta-galactosidase assay
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[PMID: 25199582] |
| MT2 | CC50 |
>100 μM
Compound: UC-781
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Cytotoxicity against human MT2 cells by MTT assay
Cytotoxicity against human MT2 cells by MTT assay
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[PMID: 16298131] |
| MT2 | CC50 |
>100 μM
Compound: UC-781
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Cytotoxicity against MT2 cells
Cytotoxicity against MT2 cells
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[PMID: 16263277] |
| MT2 | CC50 |
41 μM
Compound: 3
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Cytotoxicity against human MT2 cells by MTT assay
Cytotoxicity against human MT2 cells by MTT assay
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[PMID: 17918923] |
| MT2 | EC50 |
0.002 μM
Compound: UC-781
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Antiviral activity against HIV1 3B in MT2 cells by MTT assay
Antiviral activity against HIV1 3B in MT2 cells by MTT assay
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[PMID: 16298131] |
| TZM | CC50 |
>100 μM
Compound: UC781
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Cytotoxicity against human TZM-bl cells assessed as cell viability after 48 hrs by WST1 assay
Cytotoxicity against human TZM-bl cells assessed as cell viability after 48 hrs by WST1 assay
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[PMID: 25199582] |
UC-781 (0.05, 0.2 and 0.5 % UC-781 replens gel; 10 d) is released from gel preparation and eliminates HIV-1 virus in CEM cells[1].
UC-781 (3.75-30 μM) inhibits the growth of Bacillus cereus (about 50 %)[1].
UC-781 inhibits the activity of HIV-1 (ⅢB) in CEM T cells (EC50=6 nM; IC50=23 nM). UC-781 inhibits the activity of HIV in Monocyte-Derived Dendritic Cell (MO-DC) and autologous CD4+ T cells with EC50 values of 550 nM and 1588 nM, respectively[2].
UC-781 (1 µM or 10 µM; 24 h) effectively prevents or blocks MO-DC and autologous CD4+ T cells infected HIV[2].
UC-781 (0.001-1000 µM; 2 h) inhibits the transition of virus cervical explants infected with HIV-1BaL[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female rabbit (~1200 g; 10 weeks old)[1].
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Dosage:100 µl 5% UC-781 replens gel.
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Administration:Intravaginal; once daily for 10 days.
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Result:Released from gel preparation and had normal histology without significant increases inflammatory cells in rabbits.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 178870-32-1
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Molecular Weight 335.85
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Formula C17H18ClNO2S
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SMILES
S=C(C1=C(C)OC=C1)NC2=CC=C(Cl)C(OC/C=C(C)/C)=C2
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Synonyms
NSC 675186
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Balzarini J, et al. Preclinical studies on thiocarboxanilide UC-781 as a virucidal agent. AIDS. 1998 Jul 9;12(10):1129-38. [Content Brief]
[2]. Van Herrewege Y, et al. In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodeficiency virus microbicides. Antimicrob Agents Chemother. 2004 Jan;48(1):337-9. [Content Brief]
[3]. Balzarini J, et al. Highly favorable antiviral activity and resistance profile of the novel thiocarboxanilide pentenyloxy ether derivatives UC-781 and UC-82 as inhibitors of human immunodeficiency virus type 1 replication. Mol Pharmacol. 1996 Aug;50(2):394-401. [Content Brief]
[4]. Fletcher P, et al. The nonnucleoside reverse transcriptase inhibitor UC-781 inhibits human immunodeficiency virus type 1 infection of human cervical tissue and dissemination by migratory cells. J Virol. 2005 Sep;79(17):11179-86. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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