연구용
제품 번호: S1835
화학 구조
| 세포주 | 분석 유형 | 농도 | 배양 시간 | 제형 | 활성 설명 | PMID |
|---|---|---|---|---|---|---|
| HeLa 299 | Antichlamydial assay | 44 to 48 hrs | Antichlamydial activity against Chlamydia trachomatis serovar L2 infected in human HeLa 299 cells assessed as reduction in number of inclusion bodies measured after 44 to 48 hrs by DAPI staining-based HCS assay, IC50=0.727μM. | 29232584 | ||
| THP1 | Function assay | 30 mins | Drug uptake in human THP1 cells at pH 6 to 7 after 30 mins | 19564365 | ||
| THP1 | Function assay | 24 hrs | Drug uptake in human THP1 cells after 24 hrs in presence of verapamil | 19564365 | ||
| THP1 | Function assay | 24 hrs | Drug uptake in human THP1 cells after 24 hrs in presence of gemfibrozil | 19564365 | ||
| Hep2 | Antichlamydial assay | 4 ug/ml | 8 hrs | Anti-Chlamydial activity against Chlamydia trachomatis Serovar LGV-L2 infected in Hep2 cells assessed as reduction in size and number of chlamydial inclusion at 4 ug/ml treated at 8 hrs post-infection and 24 hrs later re-infecting fresh Hep2 cells monolay | 32227948 | |
| Vero E6 | Antiviral assay | 2 days | Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days, EC50=2.12μM. | ChEMBL | ||
| Vero E6 | Antiviral assay | 2 days | Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days, EC90=8.65μM. | ChEMBL | ||
| 클릭하여 더 많은 세포주 실험 데이터 보기 | ||||||
| 분자량 | 748.98 | 화학식 | C38H72N2O12 |
보관 (수령일로부터) | |
|---|---|---|---|---|---|
| CAS 번호 | 83905-01-5 | SDF 다운로드 | 원액 보관 |
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| 동의어 | XZ-450,CP-62993 | Smiles | CCC1C(C(C(N(CC(CC(C(C(C(C(C(=O)O1)C)OC2CC(C(C(O2)C)O)(C)OC)C)OC3C(C(CC(O3)C)N(C)C)O)(C)O)C)C)C)O)(C)O | ||
|
In vitro |
DMSO
: 100 mg/mL
(133.51 mM)
Ethanol : 100 mg/mL Water : Insoluble |
|
In vivo |
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1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)
2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)
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.
| Targets/IC50/Ki |
protein synthesis
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|---|---|
| 시험관 내(In vitro) |
Azithromycin reduces about 40% of IL-8 mRNA and protein expression in cystic fibrosis (CF) cells reaching the levels of non-CF cells. This compound results in 50% and 70% reduction of NF-kappaB and AP-1 DNA binding, respectively, leading to levels of non-CF cells. It significantly enhances the intensity of a co-stimulatory molecule, CD80, on DCs but not CD86 and CD40 in dendritic cells (DCs). This macrolide significantly increases the production of IL-10 and Clarithromycin (CAM) significantly inhibits the production of IL-6 by DCs. It increases IL-10 and CAM decreases IL-2 productions significantly, when naive T cells derived from spleen are co-cultured with DCs treated in advance with LPS and these macrolides. This agent selectively inhibits fluid-phase endocytosis of horseradish peroxidase and lucifer yellow in J774 mouse macrophages. It delays sequestration of receptor-bound transferrin and peroxidase-anti-peroxidase immune complexes into cell-surface endocytic pits and vesicles. This chemical down-regulates cell surface transferrin receptors, but not Fc gamma receptors, by causing a major delay in the accessibility of internalized transferrin receptors to the recycling route, without slowing down subsequent efflux, resulting in redistribution of the surface pool to an intracellular pool. It inserts into the DOPC lipid bilayer, so as to decrease its cohesion and to facilitate the merging of DPPC into the DOPC fluid matrix.
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참조 |
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(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)
| NCT 번호 | 모집 | 조건 | 스폰서/협력자 | 시작일 | 단계 |
|---|---|---|---|---|---|
| NCT05972772 | Not yet recruiting | Infectious Disease|Therapeutics |
Lao-Oxford-Mahosot Hospital Wellcome Trust Research Unit|Mahidol Oxford Tropical Medicine Research Unit |
March 20 2024 | Phase 2|Phase 3 |
| NCT05796362 | Not yet recruiting | Infectious Disease|Drug Effect|Clinical Infection |
Brigham and Women''s Hospital|Bill and Melinda Gates Foundation |
April 2023 | Phase 1 |