Cat. No.: HY-18630A

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Ro 48-8071

13 Cited Publications

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Based on 13 publication(s) in Google Scholar

Ro 48-8071 is an inhibitor of OSC (Oxidosqualene cyclase) with IC₅₀ of appr 6.5 nM.

For research use only. We do not sell to patients.

Purity: 99.89%
CAS No.: 189197-69-1
Formula: C₂₇H₃₁BrFNO₆
Molecular Weight:564.44

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Ro 48-8071 Chemical Structure

CAS No.: 189197-69-1

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Ro 48-8071 is an inhibitor of OSC (Oxidosqualene cyclase) with IC₅₀ of appr 6.5 nM.

IC₅₀ & Target

IC50: appr 6.5 nM (Oxidosqualene cyclase)^[1]

All Estrogen Receptor/ERR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	11.3 μM Compound: 2	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 22533316]
Caco-2	IC₅₀	2.99 μM Compound: 2	Cytotoxicity against human Caco2 cells after 72 hrs by MTT assay Cytotoxicity against human Caco2 cells after 72 hrs by MTT assay	[PMID: 22533316]
HCEC	IC₅₀	3.8 μM Compound: 2	Cytotoxicity against human HCEC cells assessed as reduction in cell survival after 72 hrs by MTT assay Cytotoxicity against human HCEC cells assessed as reduction in cell survival after 72 hrs by MTT assay	[PMID: 22533316]
HeLa	IC₅₀	2.89 μM Compound: 2	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	[PMID: 22533316]
KB	IC₅₀	2.88 μM Compound: 2	Cytotoxicity against human KB cells after 72 hrs by MTT assay Cytotoxicity against human KB cells after 72 hrs by MTT assay	[PMID: 22533316]
LN-18	IC₅₀	6.1 μM Compound: 2	Cytotoxicity against human LN18 cells assessed as reduction in cell survival after 72 hrs by MTT assay Cytotoxicity against human LN18 cells assessed as reduction in cell survival after 72 hrs by MTT assay	[PMID: 22533316]
LN-229	IC₅₀	8.8 μM Compound: 2	Cytotoxicity against human LN229 cells assessed as reduction in cell survival after 72 hrs by MTT assay Cytotoxicity against human LN229 cells assessed as reduction in cell survival after 72 hrs by MTT assay	[PMID: 22533316]
LNCaP	IC₅₀	>30 μM Compound: 2	Cytotoxicity against human LNCAP cells after 72 hrs by MTT assay Cytotoxicity against human LNCAP cells after 72 hrs by MTT assay	[PMID: 22533316]
MCF7	IC₅₀	6.77 μM Compound: 2	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 22533316]
OVCAR	IC₅₀	>30 μM Compound: 2	Cytotoxicity against human OVCAR cells after 72 hrs by MTT assay Cytotoxicity against human OVCAR cells after 72 hrs by MTT assay	[PMID: 22533316]

In Vitro

In HepG2 cells, Ro 48-8071 reduces cholesterol synthesis dose dependently with an IC₅₀ value of appr 1.5 nM^[1]. Ro 48-8071 (10 μM) significantly reduces the viability of PC-3 prostate cancer cells, but not normal prostate cells. Ro 48-8071 (10-30 μM) induces apoptosis of both LNCaP and C4-2 cell lines in a dose-dependent manner. And castration-resistant PC-3 and DU145 cells also demonstrate significant levels of apoptosis following 24-hour treatment with Ro 48-8071. Ro 48-8071 (10-25 μM) reduces AR protein expression in a dose-dependent manner. Ro 48-8071 (0.1-1 μM) increases ERβ protein expression dose-dependently in both hormone-dependent LNCaP and castration-resistant PC-3 cells^[2]. Using mammalian cells engineered to express human ERα or ERβ protein, together with an ER-responsive luciferase promoter, Ro 48-8071 dose-dependently inhibits 17β-estradiol (E2)-induced ERα responsive luciferase activity (IC₅₀, appr 10 μM), under conditions that are non-toxic to the cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ro 48-8071 lowers LDL-C maximally appr 60% at 150 μmol/kg per day, with no further reduction up to 300 μmol/kg per day, leaving HDL-C unchanged at all doses in hamsters. Ro 48-8071 (≥00 μmol/kg per day) increases the amount of MOS in liver of hamsters. Ro 48-8071 (300 μmol/kg per day) remarkedly and significantly reduces VLDL secretion of hamsters^[1]. Ro 48-8071 (5 or 20 mg/kg) significantly reduces in vivo tumor growth in mice, without weight loss of the mice. Furthermore, Ro 48-8071 at a concentration of 20 mg/kg, completely eradicates two of the 12 tumors being monitored in the mice in the timeframe tested^[2]. Ro 48-8071 (20 mg/day/kg body weight) leads to a rapid and sustained inhibition (>50%) of cholesterol synthesis in the whole small intestine of BALB/c mice. Sterol synthesis is also reduced in the large intestine and stomach^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 189197-69-1
Appearance Solid
Molecular Weight 564.44
Formula C₂₇H₃₁BrFNO₆
Color White to light yellow
SMILES

O=C(C1=CC=C(Br)C=C1)C2=CC=C(OCCCCCCN(C)CC=C)C=C2F.O=C(O)/C=C/C(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (13)

All Cell Proliferation/Viability AssayFlow CytometryWBIn Vivo Efficacy StudyIF

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Journal Impact Factor

Cancer Cell

Exhaustion-associated cholesterol deficiency dampens the cytotoxic arm of antitumor immunity. [Abstract]

2023 Jul 10;41(7):1276-1293.e11. PMID: 37244259
Nat Commun

A polycistronic system for multiplexed and precalibrated expression of multigene pathways in fungi. [Abstract]

2023 Jul 17;14(1):4267. PMID: 37460548
Mol Cell

The ZMYND8-regulated mevalonate pathway endows YAP-high intestinal cancer with metabolic vulnerability. [Abstract]

2021 Jul 1;81(13):2736-2751.e8. PMID: 33932349
Cell Death Dis

Targeting epigenetic modulation of cholesterol synthesis as a therapeutic strategy for head and neck squamous cell carcinoma. [Abstract]

2021 May 13;12(5):482. PMID: 33986254
Cell Death Discov

Inhibition of lanosterol synthase linking with MAPK/JNK signaling pathway suppresses endometrial cancer. [Abstract]

2025 Feb 8;11(1):55. PMID: 39922821

Ro 48-8071 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Feb 8;11(1):55. [Abstract]

The results of CCK8 reflected the IC₅₀ of Ro 48-8071 (0-2 μM) in EC cells and that Ro 48-8071 significantly inhibited the proliferation of EC cells.

Ro 48-8071 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Feb 8;11(1):55. [Abstract]

Clone formation and Transwell experiments showed that the activity of EC cells was significantly inhibited by Ro 48-8071 (0-1 μM).

Ro 48-8071 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Feb 8;11(1):55. [Abstract]

Flow cytometry analysis found that Ro 48-8071 (0-1 μM) can promote the apoptosis of EC cells.

Ro 48-8071 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Feb 8;11(1):55. [Abstract]

Ro 48-8071 (0-1 μM) reduces the expression of phosphorylated JNK protein.

Ro 48-8071 purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2025 Feb 8;11(1):55. [Abstract]

Images of isolated tumors from the subcutaneous tumor nude mice model established using Ishikawa cells treated with Ro 48-8071 or SP600125(n = 6 mice per group).
Sci China Life Sci

NPC1-regulated dynamic of clathrin-coated pits is essential for viral entry. [Abstract]

2022 Feb;65(2):341-361. PMID: 34047913
Cell Rep

EGFR-phosphorylated GDH1 harmonizes with RSK2 to drive CREB activation and tumor metastasis in EGFR-activated lung cancer. [Abstract]

2022 Dec 13;41(11):111827. PMID: 36516759
Mol Med Rep

Cholesterol biosynthesis inhibitor RO 48‑8071 inhibits pancreatic ductal adenocarcinoma cell viability by deactivating the JNK and ERK/MAPK signaling pathway. [Abstract]

2021 Dec;24(6):828. PMID: 34590153
Neoplasia

Cholesterol biosynthesis as a drug-induced vulnerability in diffuse large B cell lymphoma insensitive to EZH2 inhibition. [Abstract]

2025 Oct 27:70:101243. PMID: 41151153
ACS Synth Biol

CMI: CRISPR/Cas9 Based Efficient Multiplexed Integration in Saccharomyces cerevisiae. [Abstract]

2023 May 19;12(5):1408-1414. PMID: 36853024
Cancer Res Commun

Synergistic effects of PARP inhibition and cholesterol biosynthesis pathway modulation. [Abstract]

2024 Sep 1;4(9):2427-2443. PMID: 39028932
Immunomedicine

Metabolic inhibitor screening identifies dihydrofolate reductase as an inducer of the tumor immune escape mediator CD24. [Abstract]

2022 Dec;2(2):e1041. PMID: 36816458
Oncotarget

Disabled cell density sensing leads to dysregulated cholesterol synthesis in glioblastoma. [Abstract]

2017 Feb 28;8(9):14860-14875. PMID: 28118603

Ro 48-8071 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Feb 28;8(9):14860-14875. [Abstract]

Cell death in TS600 glioma cells. Dead cells are visualized with SYTOX Orange 24 hours after treatment with DMSO (mock), 1 μM epirubicin, 10 μM clotrimazole, 5 μM ketoconazole, or 1 μM Ro 48-8071.

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (177.17 mM; Need ultrasonic)

DMSO : ≥ 55 mg/mL (97.44 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7717 mL

8.8583 mL

17.7167 mL

5 mM

0.3543 mL

1.7717 mL

3.5433 mL

10 mM

0.1772 mL

0.8858 mL

1.7717 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.43 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS

Solubility: 12.5 mg/mL (22.15 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Protocol

Animal Administration^[2]

Six-week-old male athymic nude mice (nu/nu) weighing 20-22 g are used in the assay. Castration-resistant PC-3 cells (5×10⁶ in 0.15 mL solution) are mixed with matrigel and RPMI-1640 medium (1/1, v/v) and injected subcutaneously into both flanks of each mouse (n=6 animals/group) and tumors allowed to develop. The tumors are measured twice per week with a digital caliper. Tumor volumes are calculated by the formula (L × W × H) × π/6. Drug treatment is started when tumor volumes reach appr 100 mm³. Mice are given daily tail vein injections of 0.1 mL solution of either 5 or 20 mg/kg Ro 48-8071 for 5 days. This is followed by an injection every other day for six additional treatments and then a final injection 2 hours prior to sacrifice. Control mice receive the same volume of phosphate-buffered saline on the same schedule. The animals are weighed and tumor volumes are measured twice weekly throughout the drug treatment period.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Morand OH, et al. Ro 48-8.071, a new 2,3-oxidosqualene:lanosterol cyclase inhibitor lowering plasma cholesterol in hamsters, squirrel monkeys, and minipigs: comparison to simvastatin. J Lipid Res. 1997 Feb;38(2):373-90. [Content Brief]

[2]. Liang Y, et al. Cholesterol biosynthesis inhibitor RO 48-8071 suppresses growth of hormone-dependent and castration-resistant prostate cancer cells. Onco Targets Ther. 2016 May 30;9:3223-32 [Content Brief]

[3]. Liang Y, et al. Cholesterol biosynthesis inhibitors as potent novel anti-cancer agents: suppression of hormone-dependent breast cancer by the oxidosqualene cyclase inhibitor RO 48-8071. Breast Cancer Res Treat. 2014 Jul;146(1):51-62. [Content Brief]

[4]. Chuang JC, et al. Sustained and selective suppression of intestinal cholesterol synthesis by Ro 48-8071, an inhibitor of 2,3-oxidosqualene:lanosterol cyclase, in the BALB/c mouse. Biochem Pharmacol. 2014 Apr 1;88(3):351-63. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / H₂O	1 mM	1.7717 mL	8.8583 mL	17.7167 mL	44.2917 mL
	5 mM	0.3543 mL	1.7717 mL	3.5433 mL	8.8583 mL
	10 mM	0.1772 mL	0.8858 mL	1.7717 mL	4.4292 mL
	15 mM	0.1181 mL	0.5906 mL	1.1811 mL	2.9528 mL
	20 mM	0.0886 mL	0.4429 mL	0.8858 mL	2.2146 mL
	25 mM	0.0709 mL	0.3543 mL	0.7087 mL	1.7717 mL
	30 mM	0.0591 mL	0.2953 mL	0.5906 mL	1.4764 mL
	40 mM	0.0443 mL	0.2215 mL	0.4429 mL	1.1073 mL
	50 mM	0.0354 mL	0.1772 mL	0.3543 mL	0.8858 mL
	60 mM	0.0295 mL	0.1476 mL	0.2953 mL	0.7382 mL
	80 mM	0.0221 mL	0.1107 mL	0.2215 mL	0.5536 mL
H₂O	100 mM	0.0177 mL	0.0886 mL	0.1772 mL	0.4429 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Ro 48-8071

Bioactive Compound Library Max

Bioactive Compound Library

Apoptosis Compound Library

Anti-Cancer Compound Library

Targeted Diversity Library

Nuclear Receptor Compound Library

Membrane Receptor-targeted Compound Library

Cell Death Library

MCE Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Ro 48-8071

All Estrogen Receptor/ERR Isoforms

Biological Activity

Chemical Information

Publications (13)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Ro 48-8071

Bioactive Compound Library Max

Bioactive Compound Library

Apoptosis Compound Library

Anti-Cancer Compound Library

Targeted Diversity Library

Nuclear Receptor Compound Library

Membrane Receptor-targeted Compound Library

Cell Death Library

MCE Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Ro 48-8071

All Estrogen Receptor/ERR Isoforms

Biological Activity

Chemical Information

Publications (13)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Ro 48-8071 Related Classifications

HY-18630A Related Classifications