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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Ro 48-8071 fumarate is an orally bioavailable inhibitor of OSC (Oxidosqualene cyclase) with IC50 of ~6.5 nM. OSC represents a new and unique target for cholesterol-lowering drugs. In addition, Ro 48-8071 has shown anticancer activity, at 10 μM, it 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.
| ln Vitro |
With an IC50 value of roughly 1.5 nM, Ro 48 -8071 decreases cholesterol synthesis in HepG2 cells in a dose-dependent manner [1]. The viability of PC-3 prostate cancer cells is significantly reduced by Ro 48 -8071 (10 μM), but not of normal prostate cells. In LNCaP and C4-2 cell lines, Ro 48 -8071 (10-30 μM) causes apoptosis in a dose-dependent manner. Significant levels of apoptosis were also seen in castration-resistant PC-3 and DU145 cells 24 hours after they were treated with Ro 48–8071. The reduction of AR protein expression is dose-dependent and occurs with Ro 48 -8071 (10-25 μM). In castration-resistant PC-3 cells and hormone-dependent LNCaP, Ro 48 -8071 (0.1-1 μM) dose-dependently upregulates the expression of the ERβ protein [2]. Mammalian cells engineered to express human ERα or ERβ proteins in combination with the ER-responsive luciferase promoter, enables Ro 48-8071 to dose-dependently inhibit 17β-estradiol (E2)-induced ERα-responsive luciferase. Activity (IC50, approximately 10 μM), in a cell-nontoxic environment [3].
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| ln Vivo |
In hamsters, Ro 48 -8071 decreases LDL-C by approximately 60% at 150 μmol/kg per day and stops at 300 μmol/kg per day; HDL-C does not change at any dose. The amount of MOS in hamster liver increases at Ro 48 -8071 (≥00 μMol/kg per day). In hamsters, Ro 48 -8071 (300 μmol/kg daily) dramatically lowers VLDL secretion [1]. Without causing weight loss, Ro 48 -8071 (5 or 20 mg/kg) dramatically slowed the growth of tumors in mice. Furthermore, two of the twelve tumors observed in mice during the test period were totally eradicated by Ro 48-8071 at a dosage of 20 mg/kg [2]. In the entire small intestine of BALB/c mice, Ro 48-8071 (20 mg/day/kg body weight) rapidly and persistently inhibits (>50%) the synthesis of cholesterol. Additionally, the stomach and large intestine produce less cholesterol [4].
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| Animal Protocol |
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| 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.
[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 [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. [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 |
| Molecular Formula |
C27H31BRFNO6
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| Molecular Weight |
564.44
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| CAS # |
189197-69-1
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| Related CAS # |
Ro 48-8071;161582-11-2
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| SMILES |
BrC1C([H])=C([H])C(=C([H])C=1[H])C(C1C([H])=C([H])C(=C([H])C=1F)OC([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C([H])=C([H])[H])=O.O([H])C(/C(/[H])=C(\[H])/C(=O)O[H])=O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 12.5 mg/mL (22.15 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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