Home Microbiology Reverse Transcriptase 억제제 Tenofovir Disoproxil Fumarate

연구용

Tenofovir Disoproxil Fumarate Reverse Transcriptase 억제제

제품 번호: S1400

Tenofovir Disoproxil Fumarate는 항레트로바이러스 약물 계열에 속하며, 천연 기질인 deoxyadenosine 5’-triphosphate와 경쟁하고 DNA에 삽입된 후 DNA 사슬 종결을 유도함으로써 HIV Reverse Transcriptase의 활성을 억제하는 Microbiology적 기전을 가집니다.
Tenofovir Disoproxil Fumarate Reverse Transcriptase 억제제 Chemical Structure

화학 구조

분자량: 635.51

바로가기

품질 관리 (Quality Control)

배치: 순도: 99.94%
99.94

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

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
MT2 Function assay 5 days Inhibition of virus-induced cytopathic effect in wild type HIV 3a infected MT2 cells after 5 days, EC50=0.015μM 17562366
HepG2 Cytotoxicity assay 9 days Cytotoxicity against human HepG2 cells after 9 days by MTT assay, IC50=2.31μM 17888662
HepG2 Antiviral assay 9 days Antiviral activity against Hepatitis B virus infected human HepG2 cells after 9 days by MTT assay, IC50=5.1μM 17888662
MT-2 Antiviral assay Antiviral activity against HIV1 3B infected in human MT-2 cells by two fold dilution method in presence of 10% FBS, EC50=0.0068μM 19104010
MT2 Antiviral assay Antiviral activity against HIV1 infected in human MT2 cells assessed as inhibition of viral replication, IC50=0.54μM 19596885
HeLa P4/R5 Antiviral assay Antiviral activity against HIV1 infected in human HeLa P4/R5 cells assessed as inhibition of viral replication, IC50=4.7μM 19596885
HeLa P4/R5 Antiviral assay Antiviral activity against HIV1 harboring reverse transcriptase K65R mutant infected in human HeLa P4/R5 cells assessed as inhibition of viral replication, IC50=11.4μM 19596885
human bone marrow cells Cytotoxicity assay 24 hrs Cytotoxicity against human bone marrow cells after 24 hrs by BFU-E assay, CC50=0.9μM 20439609
human bone marrow cells Cytotoxicity assay 24 hrs Cytotoxicity against human bone marrow cells after 24 hrs by GM-CFU assay, CC50=1.9μM 20439609
HeLa-T4 Antiviral assay 48 hrs Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as luciferase activity after 48 hrs by exogenous RT assay, EC50=0.0029μM 21060108
HeLa-T4 Antiviral assay 48 hrs Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef infected in human HeLa-T4 cells assessed as luciferase activity after 48 hrs by exogenous RT assay, EC95=0.037μM 21060108
HeLaT4 Antiviral assay 24 hrs Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of infection using human HeLaT4 cells pretreated for 24 hrs followed by exposed to vi, EC50=0.12μM 21060108
HeLaT4 Antiviral assay Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of 2 mins magnetic nanopartials-medated infection in human HeLaT4 cells treated for 1, EC99.6=0.95μM 21060108
HeLaT4 Cytotoxicity assay Cytotoxicity against human HeLaT4 cells by WST-1 assay, CC50=34μM 21060108
HeLaT4 Function assay 24 hrs Drug uptake in human HeLaT4 cells assessed as compound persist measured after 3 times washout at 100 time EC95 for HIV1 for 24 hrs 21060108
HeLaT4 Antiviral assay 24 hrs Antiviral activity against single-round HIV1 NLX.Lux-R harboring inactivating mutations in env, vpr and carries firefly luciferase gene in place of nef assessed as level of infection using human HeLaT4 cells pretreated at 100 time EC95 for 24 hrs followed 21060108
PBMC Antiviral assay 7 days Antiviral activity against HIV1 infected in human PBMC assessed as inhibition of viral replication by measuring reverse transcriptase activity in cell supernatant preincubated with cells followed by viral infection measured after 7 days by radioactive inc, EC50=0.0046μM 27405794
HepG2.2.15 Antiviral assay 3 days Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as inhibition of viral DNA in cell supernatant incubated for 3 days in presence of 10% FBS followed by compound treatment in absence of 10% FBS for 3 days by qRT-PCR method, EC50=0.34μM 27405794
HepG2.2.15 Cytotoxicity assay 6 days Cytotoxicity against human HepG2.2.15 cells assessed as reduction in cell viability after 6 days by XTT assay, CC50=29.2μM 27405794
PBMC Antiviral assay 30 mins Antiviral activity against CXCR4-tropic HIV-1 NL4-3 infected in human PHA-stimulated PBMC assessed as inhibition of viral replication by measuring reduction in p24 antigen production preincubated with cells for 30 mins followed by viral infection measured, IC50=0.08μM 28682067
PBMC Antiviral assay 30 mins Antiviral activity against CCR5 tropic HIV1 BaL infected in human PHA-stimulated PBMC assessed as inhibition of viral replication by measuring reduction in p24 antigen production preincubated with cells for 30 mins followed by viral infection measured on , IC50=0.22μM 28682067
MT4 Antiviral assay 6 days Antiviral activity against CXCR4-tropic HIV-1 NL4-3 infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 6 days by XTT dye based assay, EC50=4.89μM 28682067
MT4 Antiviral assay 6 days Antiviral activity against tenofovir-resistant CXCR4-tropic HIV-1 NL4-3 harboring reverse transcriptase K65R mutant infected in human MT4 cells assessed as inhibition of viral replication inhibition of virus-induced cytopathic effect after 6 days by XTT d, EC50=11.3μM 28682067
HepG2.2.15 Antiviral assay Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in cytoplasmic DNA synthesis by reed and munch method, IC50=0.85μM 31223460
HepG2.2.15 Cytotoxicity assay Cytotoxicity against human HepG2.2.15 cells infected with HBV, CC50=20.71μM 31223460
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 635.51 화학식

C19H30N5O10P.C4H4O4

 보관 (수령일로부터)
CAS 번호 202138-50-9 SDF 다운로드 원액 보관

동의어 GS 1278, Tenofovir DF Smiles CC(C)OC(=O)OCOP(=O)(COC(C)CN1C=NC2=C(N=CN=C21)N)OCOC(=O)OC(C)C.C(=CC(=O)O)C(=O)O

용해도 (Solubility)

In vitro
배치:

DMSO : 100 mg/mL (157.35 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 100 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
HIV reverse transcriptase
(Cell-free assay)
시험관 내(In vitro)

Tenofovir is eliminated from systemic circulation renally through a combination of glomerular filtration and active tubular secretion. Tenofovir is not a substrate for human organic cation transporter type 1 (hOCT1) or hOCT2. Tenofovir accumulates to fivefold lower levels in MRP4-overexpressing cells, and its accumulation could be increased by an MRP inhibitor. Tenofovir produces no significant changes in mitochondrial DNA (mtDNA) levels in human hepatoblastoma (HepG2) cells, skeletal muscle cells (SkMCs), or renal proximal tubule epithelial cells. Tenofovir elevates lactate production by less than 20% in HepG2 cells or SkMCs. Tenofovir is efficiently phosphorylated to tenofovir diphosphate (TFV-DP) in both HepG2 cells and primary human hepatocytes. Tenofovir has a 50% effective concentration of 1.1 mM against HBV in cell-based assays, and potency is improved > 50-fold by the addition of bis-isoproxil progroups. Tenofovir has previously demonstrated full activity against lamivudine-resistant HBV in vitro and clinically. Tenofovir inhibits the proliferation of liver-derived HepG2 cells and normal skeletal muscle cells with CC(50) values of 398 μM and 870 μM, respectively. Tenofovir shows substantially weaker effects on proliferation and viability of renal proximal tubule epithelial cells than cidofovir, a related nucleotide analog with the potential to induce renal tubular dysfunction.

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/11888656/
  • [5] https://pubmed.ncbi.nlm.nih.gov/26711762/
  • [6] https://pubmed.ncbi.nlm.nih.gov/25568137/

임상시험 정보 (Clinical Trial Information)

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

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
NCT05874440 Recruiting
Chronic Hepatitis b Patients
Sohag University
 April 15 2023 --
NCT03576066 Completed
Chronic Hepatitis B
Assembly Biosciences
 June 11 2018 Phase 2
NCT03361956 Completed
Hepatitis B
Janssen Sciences Ireland UC
 February 13 2018 Phase 2
NCT02985996 Completed
HIV Infections
Emory University|Centers for Disease Control and Prevention
 February 6 2017 Phase 1