Home Microbiology Reverse Transcriptase inhibitor Nevirapine (NSC 641530)

연구용

Nevirapine (NSC 641530) Reverse Transcriptase inhibitor

제품 번호: S1742

Nevirapine (NSC 641530, NVP) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used to treat HIV-1 infection and AIDS.
Nevirapine (NSC 641530) Reverse Transcriptase inhibitor Chemical Structure

화학 구조

분자량: 266.3

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품질 관리 (Quality Control)

배치: 순도: 99.66%
99.66

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

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
CEM-SS cells Function assay Antiviral activity against HIV1 RF in CEM-SS cells assessed as inhibition of virus-induced cytopathic effect by XTT assay, EC50=1.5 nM
human MT4 cells Function assay Antiviral activity against Human immunodeficiency virus 1 subtype C infected in human MT4 cells assessed as reduction in virus induced cytopathicity, EC50=0.00488 μM
human Jurkat E6-1 cells Function assay 2 days Antiviral activity against HIV1 Env-pseudovirus infected in human Jurkat E6-1 cells after 2 days by luciferase assay, IC50=0.04 μM
human C1866 cells Cytotoxicity assay 72 h Cytotoxicity against human C1866 cells after 72 hrs by MTT assay, EC50=0.04943 μM
human MT2 cells Function assay 4 days Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as inhibition of p24 antigen production after 4 days by ELISA, EC50=0.053 μM
HeLa cells Function assay Antiviral activity against wild type HIV1 in HeLa cells by MAGI assay, IC50=0.053 μM
293T cells Function assay Inhibition of wild type HIV1 reverse transcriptase in 293T cells, IC50=0.06 μM
MDCK2 cells Function assay 10 μM Inhibition of human MRP2 expressed in MDCK2 cells assessed as increase in intracellular CMF fluorescence at 10 uM by CMFDA assay
클릭하여 더 많은 세포주 실험 데이터 보기

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

분자량 266.3 화학식

C15H14N4O

 보관 (수령일로부터)
CAS 번호 129618-40-2 SDF 다운로드 원액 보관

동의어 NSC 641530,NVP Smiles CC1=C2C(=NC=C1)N(C3=C(C=CC=N3)C(=O)N2)C4CC4

용해도 (Solubility)

In vitro
배치:

DMSO : 53 mg/mL (199.02 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

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)

Targets/IC50/Ki
Reverse transcriptase
시험관 내(In vitro)

Nevirapine (NSC 641530) is a non-nucleoside RT inhibitor with a well-characterized inhibitory activity on RT enzymes of retroviral origin. It is also an effective inhibitor of the endogenous RT in murine and human cell lines. This compound is a highly specific inhibitor of HIV-1 reverse transcriptase (RT) which exhibits an IC50 = 84 nM in enzyme assays and IC50 = 40nM against HIV-1 replication in cell culture. It alters the cleavage specificity of the RNase H, resulting in Nevirapine-induced stimulation of RNase H activity beyond the increase expected from the change in cleavage specificity. It is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki = 270 mM). Its exposure rescues the differentiation block present in acute myeloid leukemia (AML) cell lines and primary blasts from two AML patients, as indicated by morphological, functional and immunophenotypic assays.

생체 내(In vivo)

Nevirapine (NSC 641530) is metabolized to 4-CANVP as a major metabolite in all male animals and in female mice, dogs, and monkeys. 3-OHNVP is a major fecal metabolite in all animals except for the male rat. In the bile of rats, 4-CANVP is a major metabolite along with 12-OHNVP glucuronide.

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/7533167/
  • [5] https://pubmed.ncbi.nlm.nih.gov/10570025/

임상시험 정보 (Clinical Trial Information)

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

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
NCT05725252 Completed
Healthy Volunteers
NVP Healthcare
 May 28 2023 Phase 1
NCT05354713 Completed
Healthy Volunteers
NVP Healthcare
 November 5 2022 Phase 1
NCT04926727 Unknown status
Nausea Gravidarum|Vomiting of Pregnancy
Italfarmaco|Opera CRO a TIGERMED Group Company
 October 4 2021 --
NCT02738502 Completed
Maternal-fetal Infection Transmission
ANRS Emerging Infectious Diseases|Institut National de la Santé Et de la Recherche Médicale France
 July 6 2016 Phase 2
NCT02383849 Completed
Low-Birth-Weight Infant|Tuberculosis|HIV
International Maternal Pediatric Adolescent AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)
 August 4 2015 --