Home Microbiology Antineoplastic and Immunosuppressive Antibiotics 억제제 Tigecycline

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Tigecycline Antineoplastic and Immunosuppressive Antibiotics 억제제

제품 번호: S1403

Tigecycline은 정균 작용을 하며, Bacterial의 30S ribosomal 소단위에 결합하여 원핵생물의 번역 과정 중 ribosome의 A 부위로 Aminoacyl-tRNA가 진입하는 것을 차단함으로써 단백질 합성을 억제합니다. 이 화합물은 PI3K-AKT-mTOR 경로를 하향 조절함으로써 Autophagy를 유도합니다.
Tigecycline Antineoplastic and Immunosuppressive Antibiotics 억제제 Chemical Structure

화학 구조

분자량: 585.65

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품질 관리 (Quality Control)

배치: 순도: 99.86%
99.86

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

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
THP-1 Antibacterial assay 24 hrs Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient infected in human THP-1 cells assessed as log reduction of intracellular CFU level after 24 hrs in presence of thymidine 19188393
클릭하여 더 많은 세포주 실험 데이터 보기

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

분자량 585.65 화학식

C29H39N5O8

 보관 (수령일로부터)
CAS 번호 220620-09-7 SDF 다운로드 원액 보관

동의어 GAR-936, WAY-GAR-936, TBG-MINO Smiles CC(C)(C)NCC(=O)NC1=CC(=C2CC3CC4C(C(=O)C(=C(C4(C(=O)C3=C(C2=C1O)O)O)O)C(=O)N)N(C)C)N(C)C

용해도 (Solubility)

In vitro
배치:

DMSO : 100 mg/mL (170.75 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : 100 mg/mL

Ethanol : 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)

시험관 내(In vitro)

Tigecycline evades the Tet(A-E) efflux pumps, which account for most acquired resistance to tetracycline and minocycline in Enterobacteriaceae and Acinetobacter spp. This compound binds to bacterial ribosomes that have been modified by the Tet(M) protein, a mechanism that compromises all available tetracyclines, and which is frequent in Gram-positive cocci and Neisseria spp. It remains vulnerable to the chromosomally-encoded multidrug efflux pumps of Proteeae and Pseudomonas aeruginosa, and to Tet(X), a tetracycline-degrading mono-oxygenase found, albeit rarely, in Bacteroides spp. Its MICs for enterococci, staphylococci, and streptococci are mostly 0.06–0.25 mg/L, again with little or no skew to the distribution. This agent is prone to oxidation, and MIC values, particularly for the most susceptible isolates, may be raised if the drug is added to broth that has become oxygenated during storage, or if drug-containing media are stored before inoculation. It is a poor substrate for tetracycline-specific efflux pumps, and it still attaches to ribosomes that have been modified by the Tet(M) protein. This antibacterial has demonstrated activity against a wide variety of gram-positive and gram-negative pathogens, including multidrug-resistant strains. It is active against many gram-positive and -negative organisms, including methicillin-resistantStaphylococcus aureus, vancomycin-intermediate and -resistant enterococci, and extended-spectrum β-lactamase–producing Escherichia coli and Klebsiella pneumoniae. This compound exhibits antibacterial activity against a wide spectrum of aerobic and anaerobic bacteria. It is a broad-spectrum, protein-inhibiting, antibacterial agent possessing activity against strains resistant to other chemotherapeutic agents. This chemical demonstrates in vitro activities against the GISA and the methicillin-resistant and methicillin-susceptible staphylococcal strains tested (MICs at which 90% of isolates tested are inhibited [MIC90s], 0.5 to 1 μg/ml). It has MIC90s of 0.25 μg/ml for all of the S. pneumoniae strains and demonstrates similar activities against all of the S. pneumoniae strains tested.

생체 내(In vivo)

Tigecycline is bactericidal against methicillin-susceptible S. aureus (MSSA) in the rabbit osteomyelitis model and exhibits good, but not excellent, activity in Legionellapneumophila pneumonia in guinea pigs. This compound at 50 mg/kg twice daily was not toxic to mice. It is effective in inhibiting NSCLC growth in vivo through decreasing proliferation and increasing apoptosis of tumor cells.
참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/27009695/

적용 분야 (Applications)

방법 바이오마커 이미지 PMID
Western blot E-cadherin / Vimentin CDK2 / Cyclin E Cox-1 / Cox-2 / Cox-4 p-AMPKα / AMPKα / p-mTOR / mTOR / p-p70S6K / p70S6K / p-4E-BP-1 / 4E-BP1 p62 / LC3-I / LC3-II Cyclin D1 / CDK2 / p21
S1403-WB6
26621850
Growth inhibition assay Cell viability
S1403-viability1
30247801

임상시험 정보 (Clinical Trial Information)

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2026-03-20)

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
NCT07485010 NOT_YET_RECRUITING
Mycobacterium Abscessus Pulmonary Disease; Mycobacterium Abscessus Infection; Non-Tuberculous Mycobacterial (NTM) Infections; Non-Tuberculous Mycobacteria Pulmonary Disease
The University of Queensland
 2027-04 PHASE2
NCT04310930 RECRUITING
Pulmonary Disease Due to Mycobacteria (Diagnosis)
The University of Queensland
 2020-03-02 PHASE2; PHASE3
NCT07759453 NOT_YET_RECRUITING
Liver Transplant; Carbapenem-resistant Enterobacterales; CRE Colonization
IRCCS Azienda Ospedaliero-Universitaria di Bologna
 2026-10-01 PHASE3
NCT07004049 RECRUITING
Bloodstream Infection; Ventilator Associated Bacterial Pneumonia; Hospital Acquired Bacterial Pneumonia; Carbapenem Resistant Bacterial Infection; Multidrug Resistance
National University of Singapore
 2025-04-21 PHASE4
NCT07495150 NOT_YET_RECRUITING
Blood-Brain Barrier; Bacterial Meningitis
yilong Wang
 2026-04-01
NCT07524920 NOT_YET_RECRUITING
MDR Bacteria
Ain Shams University
 2026-04-01 PHASE2