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Cat. No.: HY-15351

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UC-781

Name: UC-781
Brand: MedChemExpress
SKU: HY-15351
Availability: PreOrder

(Synonyms: NSC 675186)

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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CAS No.: 178870-32-1
Formule: C₁₇H₁₈ClNO₂S
Masse moléculaire:335.85

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

UC-781 Chemical Structure

CAS No.: 178870-32-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

HIV-1

0.005 μM (IC₅₀)

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Cellular Effect

Cell Line	Type	Value	Description	References
MRC5	IC₅₀	>64 μM Compound: UC781	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	[PMID: 25199582]
MRC5	IC₅₀	>64 μM Compound: UC781	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	[PMID: 25199582]
MT2	CC₅₀	>100 μM Compound: UC-781	Cytotoxicity against human MT2 cells by MTT assay Cytotoxicity against human MT2 cells by MTT assay	[PMID: 16298131]
MT2	CC₅₀	>100 μM Compound: UC-781	Cytotoxicity against MT2 cells Cytotoxicity against MT2 cells	[PMID: 16263277]
MT2	CC₅₀	41 μM Compound: 3	Cytotoxicity against human MT2 cells by MTT assay Cytotoxicity against human MT2 cells by MTT assay	[PMID: 17918923]
MT2	EC₅₀	0.002 μM Compound: UC-781	Antiviral activity against HIV1 3B in MT2 cells by MTT assay Antiviral activity against HIV1 3B in MT2 cells by MTT assay	[PMID: 16298131]
TZM	CC₅₀	>100 μM Compound: UC781	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	[PMID: 25199582]

In Vitro

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 (Ⅲ_B) 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-1_BaL^[4].

MedChemExpress (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 in female rabbit^[1].

MedChemExpress (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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 178870-32-1
Masse moléculaire 335.85
Formule C₁₇H₁₈ClNO₂S
SMILES

S=C(C1=C(C)OC=C1)NC2=CC=C(Cl)C(OC/C=C(C)/C)=C2
Synonyms

NSC 675186
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Pureté et documentation
Références

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UC-781

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