Home Immunology & Inflammation Immunology & Inflammation related inhibitor Sulfasalazine

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Sulfasalazine Immunology & Inflammation related inhibitor

제품 번호S1576

Sulfasalazine is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. This compound is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. It induces ferroptosis, apoptosis and autophagy.
Sulfasalazine Immunology & Inflammation related inhibitor Chemical Structure

화학 구조

분자량: 398.39

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품질 관리 (Quality Control)

배치: 순도: 99.65%
99.65

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

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
HEK293 Flp-In Function assay Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting, Ki=0.53μM 22541068
HEK293 Flp-In Function assay Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting, IC50=0.56μM 22541068
HepG2 Function assay 1 hr Inhibition of NF-kappaB activation expressed in TNFalpha-stimulated human HepG2 cells co-transfected with PPRE-Luc plasmid pretreated for 1 hr before TNFalpha challenge measured after 24 hrs by luciferase reporter gene assay, IC50=0.9μM 21889336
HepG2 Function assay 1 hr Inhibition of TNF-alpha-induced NFkappaB activation in human HepG2 cells after 1 hr by luciferase reporter assay, IC50=0.9μM 21870831
HepG2 Function assay 1 hr Inhibition of TNFalpha-induced NFkappaB transcriptional activity in human HepG2 cells pretreated for 1 hr before TNFalpha challenge by luciferase reporter gene analysis, IC50=0.9μM 22381047
HepG2 Function assay 1 hr Inhibition of NF-kappaB expressed in human HepG2 cells assessed as inhibition of TNFalpha-induced luciferase activity preincubated for 1 hr followed by TNFalpha challenge measured after 1 hr by reporter gene assay, IC50=0.9μM 23031596
HepG2 Function assay 1 hr Inhibition of TNF-alpha-induced NF-kappaB transcriptional activation in human HepG2 cells preincubated for 1 hr followed by TNF-alpha challenge measured after 1 hr by luciferase reporter gene assay, IC50=0.9μM 24314396
HEK293 Flp-In Function assay 5 mins Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting, Ki=3μM 22541068
HEK293 Flp-In Function assay 5 mins Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting, IC50=3μM 22541068
U2OS Function assay 10 mins Inhibition of HA-tagged human NTCP expressed in human U2OS cells assessed as reduction in [14C]taurocholate uptake preincubated for 10 mins followed by [14C] taurocholate addition and further incubation for 10 mins by scintillation counting method, IC50=9.6μM 31439379
HEK293 Flp-In Function assay 5 mins Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting, Ki=11μM 22541068
HEK293 Flp-In Function assay 5 mins Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting, IC50=12μM 22541068
U87 Function assay 15 mins Inhibition of xc-cystine-glutamate antiporter-mediated cystine uptake in human U87 cells using L-[14C]cystine as substrate after 15 mins by liquid scintillation counting, IC50=30μM 21889337
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 398.39 화학식

C18H14N4O5S

 보관 (수령일로부터)
CAS 번호 599-79-1 SDF 다운로드 SDF 다운로드 원액 보관

동의어 NSC 667219, Sulphasalazine Smiles C1=CC=NC(=C1)NS(=O)(=O)C2=CC=C(C=C2)N=NC3=CC(=C(C=C3)O)C(=O)O

용해도 (Solubility)

In vitro
배치:

DMSO : 80 mg/mL (200.8 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
NF-κB
COX-2
TGF-β
시험관 내(In vitro)

Sulfasalazine, like methotrexate, enhances adenosine release at an inflamed site and that adenosine diminishes inflammation via occupancy of A2 receptors on inflammatory cells. This compound treatment for 4 hours inhibits kappaB-dependent transcription with an IC50 value of approximately 0.625 mM. This chemical (2.5 mM) results in cell death of T-lymphocytes in a dose- and time-dependent manner. This compound but not 5ASA or sulfapyridine, strongly inhibits NF-kappaB activation and potently induces apoptosis in T-lymphocytes. It is cleaved into sulfapyridine and 5-aminosalicylic acid (5-ASA; mesalamine) by colonic bacteria, and the latter, too, is reported to suppress NF-kappaB activity. This compound but not its cleaved form 5-ASA causes a dose-dependent inhibition of glioma growth, this effect is entirely attributable to the inhibition of cystine uptake via the system x(c)(-) cystine-glutamate transporter. It inhibits cystine uptake causing a chronic depletion of intracellular GSH and consequently compromised cellular redox defense which stymied tumor growth.

생체 내(In vivo)

Sulfasalazine markedly decreases the number of leukocytes that accumulated in the inflamed (carrageenan, 2 mg/ml) air pouch in the murine air pouch model of inflammation. This compound treatment promotes a marked increase in splenocyte 5-aminoimidazole-4-carboxamidoribonucleotide (AICAR) concentration, which is consistent with the in vitro observation that it inhibits AICAR transformylase.

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/22381741/

임상시험 정보 (Clinical Trial Information)

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

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
NCT06134388 Recruiting
Metastatic Colorectal Cancer
Tanta University
 September 1 2023 Phase 3
NCT03487926 Active not recruiting
Major Depressive Episode|Inflammatory Bowel Diseases
Centre for Addiction and Mental Health|McMaster University
 September 14 2022 --
NCT04720183 Completed
Healthy
Galapagos NV
 January 11 2021 Phase 1
NCT01577966 Completed
Brain Tumor
University of Alabama at Birmingham
 January 2012 Not Applicable