Ritonavir (ABT-538) - Moligand™, 10mM in DMSO , Cytochrome P450 3A inhibitor, CAS No.155213-67-5, Cytochrome P450 3A inhibitor

CAS: 155213-67-5 Cat. No.: R408427 Peso molecular: 720.94 Número EC: 605-001-5

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

A 84538, RTV, Norvir, Norvir Softgel | (3S,​4S,​6S,​9S)​-4-​hydroxy-​12-​methyl-​9-​(1-​methylethyl)​-​13-​[2-​(1-​methylethyl)​-​4-​thiazolyl]​-​8,​11-​dioxo-​3,​6-​bis(phenylmethyl)​-​2,​7,​10,​12-​Tetraazatridecanoic acid 5-​thiazolylmethyl ester

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Ritonavir (ABT-538, A 84538, RTV, Norvir, Norvir Softgel) is aCytochrome P450 3AandProteaseInhibitor; Also inhibitsCytochrome P450 2D6,P-Glycoproteinand inducesCytochrome P450 2C19,Cytochrome P450 1A2,Cytochrome P450 2C9,Cytochrome P450 2B6andUDP Glucuron
In vitro

Ritonavir is a very potent inhibitor of CYP3A4 mediated testosterone 6β-hydroxylation with mean Ki of 19 nM and also inhibits tolbutamide hydroxylation with IC50 of 4.2 μM. Ritonavir is found to be a potent inhibitor of CYP3A-mediated biotransformations (nifedipine oxidation with IC50 of 0.07 mM, 17alpha-ethynylestradiol 2-hydroxylation with IC50 of 2 mM; terfenadine hydroxylation with IC50 of 0.14 mM). Ritonavir is also found to be an inhibitor of the reactions mediated by CYP2D6 (IC50 = 2.5 mM) and CYP2C9/10 (IC50 = 8.0 mM). Ritonavir results in an increase in cell viability in uninfected human PBMC cultures. Ritonavir markedly decreases the susceptibility of PBMCs to apoptosis correlated with lower levels of caspase-1 expression, decreases in annexin V staining, and reduces caspase-3 activity in uninfected human PBMC cultures. Ritonavir inhibits induction of tumor necrosis factor (TNF) production by PBMCs and monocytes in a time- and dose-dependent manner at nontoxic concentrations. Ritonavir inhibits p-glycoprotein-mediated extrusion of saquinavir with an IC50 of 0.2 μM, indicating a high affinity of ritonavir for p-glycoprotein. Ritonavir inhibits human liver microsomal metabolism of ABT-378 potently with Ki of 13 nM. Ritonavir combined with ABT-378 (at 3:1 and 29:1 ratios) inhibits CYP3A (IC50 = 1.1 and 4.6 μM), albeit less potently than Ritonavir (IC50 = 0.14 μM).

In vivo

Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥98%

Specifications

Sinónimos

A 84538, RTV, Norvir, Norvir Softgel | (3S, ​4S, ​6S, ​9S)​-4-​hydroxy-​12-​methyl-​9-​(1-​methylethyl)​-​13-​[2-​(1-​methylethyl)​-​4-​thiazolyl]​-​8, ​11-​dioxo-​3, ​6-​bis(phenylmethyl)​-​2, ​7, ​10, ​12-​Tetraazatridecanoic acid 5-​thiazolylmethyl ester

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Ritonavir (ABT-538, A 84538, RTV, Norvir, Norvir Softgel) is a Cytochrome P450 3A and Protease Inhibitor; Also inhibits Cytochrome P450 2D6, P-Glycoprotein and induces Cytochrome P450 2C19, Cytochrome P450 1A2, Cytochrome P450 2C9, Cytochrome P450 2B6 and

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Cytochrome P450 3A inhibitor

Propiedades del producto

• ALogP: 6

Nombres e identificadores

• Isómeros SMILES: CC(C)C1=NC(=CS1)CN(C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC2=CC=CC=C2)C[C@@H]([C@H](CC3=CC=CC=C3)NC(=O)OCC4=CN=CS4)O
• WGK Alemania: 3
• RTECS: XA5310000
• Peso molecular: 720.94

Objetivos asociados (humanos)

CYP3A4 Tclin Cytochrome P450 3A4 (11 Activities)

Discover Target: CYP3A4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP2C9 Tchem Cytochrome P450 2C9 (1 Activities)

Discover Target: CYP2C9

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP3A5 Tclin Cytochrome P450 3A5 (2 Activities)

Discover Target: CYP3A5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLCO1B1 Tchem Solute carrier organic anion transporter family member 1B1 (2 Activities)

Discover Target: SLCO1B1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC47A1 Tchem Multidrug and toxin extrusion protein 1 (1 Activities)

Discover Target: SLC47A1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

UGT1A1 Tchem UDP-glucuronosyltransferase 1-1 (1 Activities)

Discover Target: UGT1A1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TBXAS1 Tchem Thromboxane-A synthase (1 Activities)

Discover Target: TBXAS1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 26 mg/mL (199.84 mM); Water: 26 mg/mL (199.84 mM); Ethanol: 26 mg/mL
• Punto de fusión (°C): 125 °C

Referencias

1. Han Xie, Li Song, Sagie Katz, Jinyu Zhu, Yawen Liu, Jinping Tang, Linjun Cai, Peter Hildebrandt, Xiao Xia Han.  (2022)  Electron transfer between cytochrome c and microsomal monooxygenase generates reactive oxygen species that accelerates apoptosis.  Redox Biology,      [PMID:35609401] [10.1016/j.redox.2022.102340]

2. Qing Shen, Huijuan Yang, Yunyan Li, Shiyan Li, Kang Chen, Honghai Wang, Haixing Wang, Jianfeng Ma.  (2022)  Rapid determination of antiviral drugs in yellow catfish (Pelteobagrus fulvidraco) using graphene/silica nanospheres (G/KCC-1) based pipette tip solid-phase extraction with ultra-performance liquid chromatography-tandem mass spectrometry.  JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES,      [PMID:35007897] [10.1016/j.jchromb.2022.123097]

3. Dai Tianming, Wang Min, Wang Pengzhen, Dai Libing, Dai Renke, Meng Qingqi.  (2021)  Inhibition effects of eight anti-coronavirus drugs on glycosides metabolism and glycosidases in human gut microflora.  PHARMAZIE,  76  (5): (195-201).  [PMID:33964992] [10.1691/ph.2021.01005]

4. Ma Zhiyuan, Bai Mengru, Shen Shuying, Zhou Junshan, Dong Rong, Zhang Jiangjun, Weng Yayun, Li Li, Li Yongchen, Liu Dan, Yan Wei, Lin Nengming, Xia Jianmei.  (2025)  Real-world Plasma Exposure of Nirmatrelvir/Ritonavir in Chinese Hospitalized Patients With COVID-19: A Multicenter Retrospective Study.  THERAPEUTIC DRUG MONITORING,      [PMID:39882748] [10.1097/FTD.0000000000001305]

5. Lingzhu Zhao, Siduo Xu, Shouhan Yao, Zhiqiang Wei, Guohua Lou, Jinjin Qi, Haofeng Xu, Xueyu Wang, Zhenggang Yang, Min Zheng.  (2026)  GLS4 Induces the Interferon Signaling Pathway During Hepatitis B Virus (HBV) Infection.  JOURNAL OF MEDICAL VIROLOGY,  98  (1): (e70777).  [PMID:41480806] [10.1002/jmv.70777]