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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 178870-32-1
- 分子式: C17H18ClNO2S
- 分子量:335.85
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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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 |
化学情報
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CAS 番号 178870-32-1
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分子量 335.85
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分子式 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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別名
NSC 675186
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
UC-781 関連分類
HY-15351 関連分類
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