| Identification | Back Directory | [Name]
N-[4-chloro-3-(3-methylbut-2-enoxy)phenyl]-2-methyl-furan-3-carbothioamide | [CAS]
178870-32-1 | [Synonyms]
Nsc675186
Aids029940
Aids-029940
Thiocarboxanilide
N-[4-chloro-3-(3-methylbut-2-enoxy)phenyl]-2-methyl-furan-3-carbothioamide
N-[4-Chloro-3-(3-methyl-2-butenyloxy)phenyl]-2-methyl-3-furancarbothioamide
3-Furancarbothioamide, N-[4-chloro-3-[(3-methyl-2-buten-1-yl)oxy]phenyl]-2-methyl- | [Molecular Formula]
C17H18ClNO2S | [MDL Number]
MFCD00952139 | [MOL File]
178870-32-1.mol | [Molecular Weight]
335.85 |
| Hazard Information | Back Directory | [Uses]
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[1][2][3]. | [in vivo]
UC-781 (100 μl 5% UC-781 replens gel; intravaginal; once daily for 10 days) releases from gel preparation and shows low toxicity to normal tissues in female rabbit[1]. | Animal Model: | Female rabbit (~1200 g; 10 weeks old)[1]. | | Dosage: | 100 μl 5% UC-781 replens gel. | | Administration: | Intravaginal; once daily for 10 days. | | Result: | Released from gel preparation and had normal histology without significant increases inflammatory cells in rabbits. |
| [IC 50]
HIV-1: 0.005 μM (IC50) | [References]
[1] Balzarini J, et al. Preclinical studies on thiocarboxanilide UC-781 as a virucidal agent. AIDS. 1998 Jul 9;12(10):1129-38. DOI:10.1097/00002030-199810000-00004
[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. DOI:10.1128/AAC.48.1.337-339.2004
[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. PMID:8700148
[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. DOI:10.1128/JVI.79.17.11179-11186.2005 |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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