[CAS NO. 178870-32-1] UC-781
PRODUCTS SPECIFICATIONS [178870-32-1]
DESCRIPTION [178870-32-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 335.85 |
| Molecular Formula | C17H18ClNO2S |
| SMILES | S=C(C1=C(C)OC=C1)NC2=CC=C(Cl)C(OC/C=C(C)/C)=C2 |
Summary
UC-781 (NSC 675186) is a highly potent and selective nonnucleoside reverse transcriptase inhibitor (NNRTI) of human immunodeficiency virus (HIV)-1 with an IC 50 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] .
IC50 & Target
|
HIV-1 0.005 μM (IC 50 ) |
In Vitro
UC-781 (0.05, 0.2 and 0.5 % UC-781 replens gel; 10 days) is released from gel preparation and eliminates human immunodeficiency virus (HIV)-1 virus in CEM infected cells
[1]
.
UC-781 (3.75-30 μM) inhibits the growth of
Bacillus cereus
(about 50 %)
[1]
.
UC-781 inhibits HIV-1 (Ⅲ
B
) in CEM T cells (EC
50
=6 nM; IC
50
=23 nM). UC-781 inhibits HIV in Monocyte-Derived Dendritic Cell (MO-DC) and autologous CD4
+
T cells with EC
50
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-1
BaL
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
References
- [1] Balzarini J, et al. Preclinical studies on thiocarboxanilide UC-781 as a virucidal agent. AIDS. 1998 Jul 9;12(10):1129-38.
- [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.
- [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.
- [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.