Ro 48-8071

Cat. No.: HY-18630: FAQs
Data Sheet Handling Instructions

Molarity Calculator

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.

Ro 48-8071 Chemical Structure

CAS No. : 161582-11-2

Size		Stock
50 mg		Get quote
100 mg		Get quote
250 mg		Get quote
Other size		Get quote

Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of Ro 48-8071:

Ro 48-8071 fumarate

Other Forms of Ro 48-8071:

Ro 48-8071 fumarate In-stock

9 Publications Citing Use of MCE Ro 48-8071

: 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.

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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]
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. Ro 48-8071 Related Antibodies
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.
Molecular Weight	448.37
Formula	C₂₃H₂₇BrFNO₂
CAS No.	161582-11-2
SMILES	O=C(C1=CC=C(Br)C=C1)C2=CC=C(OCCCCCCN(C)CC=C)C=C2F
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (271 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]

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.

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

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]

Ro 48-8071 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ro 48-8071161582-11-2OthersInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks