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Nitazoxanide Influenza Virus inhibitor

제품 번호: S1627

Nitazoxanide is a synthetic nitrothiazolyl-salicylamide derivative and an antiprotozoal agent(IC50 for canine influenza virus ranges from 0.17 to 0.21 μM). This compound modulates autophagy and inhibits mTORC1 signaling.
Nitazoxanide Influenza Virus inhibitor Chemical Structure

화학 구조

분자량: 307.28

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품질 관리 (Quality Control)

배치: 순도: 99.99%
99.99

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
HepG2(2.2.15) Antiviral assay Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as decrease in extracellular viral DNA measured 24 hrs after last dose, EC50=0.12μM 21553812
HepG2(2.2.15) Antiviral assay Antiviral activity against HBV infected in human HepG2(2.2.15) cells assessed as inhibition of extracellular viral DNA level, IC50=0.12μM 28383274
Ava5 Antiviral assay 3 days Antiviral activity against HCV genotype 1b infected in Ava5 cells assessed as inhibition of viral replication after 3 days by blot hybridization analysis, EC50=0.21μM 22059983
Huh7.5 Antiviral assay 3 days Antiviral activity against HCV genotype 1a infected in Huh7.5 cells assessed as inhibition of viral replication after 3 days by blot hybridization analysis, EC50=0.33μM 22059983
HepG2(2.2.15) Antiviral assay Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as decrease in intracellular viral DNA measured 24 hrs after last dose, EC50=0.59μM 21553812
HepG2(2.2.15) Antiviral assay Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as decrease in extracellular viral DNA measured 24 hrs after last dose, EC90=0.83μM 21553812
Ava5 Antiviral assay 3 days Antiviral activity against HCV genotype 1b infected in Ava5 cells assessed as inhibition of viral replication after 3 days by blot hybridization analysis, EC90=0.93μM 22059983
Huh7.5 Antiviral assay 3 days Antiviral activity against HCV genotype 1a infected in Huh7.5 cells assessed as inhibition of viral replication after 3 days by blot hybridization analysis, EC90=1.1μM 22059983
BHK-21 Antiviral assay Antiviral activity against Chikungunya virus 0611aTw infected in BHK-21 cells by RT-qPCR analysis, EC50=1.96μM 28689975
HepG2(2.2.15) Antiviral assay Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as decrease in intracellular viral DNA measured 24 hrs after last dose, EC90=2.1μM 21553812
HCT8 Antiparasitic assay 48 hrs Antiparasitic activity against Cryptosporidium parvum SPL infected in human HCT8 cells incubated for 48 hrs by FITC/DAPI staining based fluorescence assay, EC50=2.3μM 29469575
Vero E6 Function assay 48 hrs IC50 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells), IC50=2.81838μM 32353859
HCT8 Antiparasitic assay 48 hrs Antiparasitic activity against Cryptosporidium parvum BGF infected in human HCT8 cells incubated for 48 hrs by FITC/DAPI staining based fluorescence assay, EC50=2.9μM 29469575
BHK-21 Antiviral assay Antiviral activity against Chikungunya virus infected in BHK-21 cells by RT-qPCR analysis, EC50=2.96μM 28689975
U2OS Antiviral assay Antiviral activity against Chikungunya virus infected in human U2OS cells by RT-qPCR analysis, EC50=3.01μM 28689975
HCT8 Antiparasitic assay Antiparasitic activity against Cryptosporidium parvum in HCT8 cells, IC50=3.25μM 16480281
HCT-8 Antimicrobial assay Antimicrobial activity against Cryptosporidium parvum infected in human HCT-8 cells, IC50=3.8μM 18591280
BHK-21 Antiviral assay Antiviral activity against Chikungunya virus 0810bTw infected in BHK-21 cells by RT-qPCR analysis, EC50=4.95μM 28689975
Vero Cytotoxicity assay 48 hrs Cytotoxicity against african green monkey Vero cells assessed as cell viability after 48 hrs by WST-1 assay, IC50=10.74μM 23787289
BHK21 Cytotoxicity assay 16 hrs Cytotoxicity against BHK21 cells assessed as reduction in cell viability after 16 hrs by CCK-8 assay, CC50=25μM 28689975
U2OS Cytotoxicity assay 16 hrs Cytotoxicity against human U2OS cells assessed as reduction in cell viability after 16 hrs by CCK-8 assay, CC50=25μM 28689975
Ava5 Cytotoxicity assay 3 days Cytotoxicity against human Ava5 cells after 3 days by neutral red dye assay, CC50=35μM 22059983
Huh7.5 Cytotoxicity assay 3 days Cytotoxicity against human Huh7.5 cells after 3 days by neutral red dye assay, CC50=49μM 22059983
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 307.28 화학식

C12H9N3O5S

 보관 (수령일로부터)
CAS 번호 55981-09-4 SDF 다운로드 원액 보관

동의어 NTZ, NSC 697855 Smiles CC(=O)OC1=CC=CC=C1C(=O)NC2=NC=C(S2)[N+](=O)[O-]

용해도 (Solubility)

In vitro
배치:

DMSO : 62 mg/mL (201.77 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 62 mg/mL

Water : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

Targets/IC50/Ki
PFOR
mTORC1
시험관 내(In vitro)

Nitazoxanide는 세포 배양에서 약물 관련 세포 독성의 증거가 거의 없이 기생충 성장을 90% 이상 억제합니다. 이 화합물은 광범위한 원생동물 및 연충류에 대해 우수한 체외(in vitro) 활성을 보이는 새로운 thiazolide계 항기생충제입니다. 이 화합물과 그 대사산물인 tizoxanide는 G. intestinalis, E. histolytica 및 T. vaginalis에 대해 metronidazole보다 체외(in vitro)에서 더 강력한 활성을 나타냅니다. 이 약제는 HBV와 HCV 복제를 모두 강력하게 억제합니다. HCV 레플리콘 함유 세포에서 이 화합물과 IFN을 병용 투여한 후의 효과를 증강시키지만, 이 화학물질과 2'CmeC를 병용했을 때는 그렇지 않습니다. 이 화학물질은 2.2.15 세포에 의해 생성되는 여러 HBV 단백질(HBsAg, HBeAg, HBcAg)의 감소를 유도하지만, HBV RNA 전사에는 영향을 미치지 않습니다. E. histolytica에 대해 각각 0.017 mg/mL 및 0.776 mg/mL의 IC50 및 IC90 값을, G. intestinalis에 대해 0.004 mg/mL 및 0.067 mg/mL를, T. vaginalis에 대해 0.034 mg/mL 및 2.046 mg/mL의 값을 나타냅니다. 이 화합물은 E. histolytica에 대해 metronidazole 및 albendazole보다 독성이 더 강합니다.

생체 내(In vivo)

Nitazoxanide는 무균 돼지 설사 모델에서 250 mg/kg/day 용량으로 11일간 경구 투여했을 때 기생충 부하를 줄이는 데 부분적으로 효과가 있었으나, 125 mg/kg/day 용량에서는 효과가 없었습니다. 이 화합물은 돼지에게 약물 관련 설사를 유발하며, 이는 치료 효능에 영향을 미쳤을 수 있습니다.

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/17888524/
  • [5] https://pubmed.ncbi.nlm.nih.gov/12120985/
  • [6] https://pubmed.ncbi.nlm.nih.gov/22589723/

임상시험 정보 (Clinical Trial Information)

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

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