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5mg |
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10mg |
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Other Sizes |
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C75 is a novel and potent fatty-acid synthase (FASN) inhibitor used as a tool compound to study fatty acid synthesis in metabolic disorders and cancer.
ln Vitro |
PC3 cell growth is inhibited by C75, with an IC50 of 35 μM after 24 hours. With an IC50 of 50 μM, C75 (10-50 μM) still inhibits the development of LNCaP spheroids in a concentration-dependent way [1]. With harmful effects, (-)-C75 suppresses FAS activity in most tumor cell lines without influencing meal intake. The anorexic effects of C75 are dependent on central inhibition of CPT1, as (+)-C75 inhibits CPT1, which causes anorexia. Novel cancer and chemotherapy medications may be developed as a result of the distinct actions of C75 enantiomers [2].
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ln Vivo |
The paraventricular nucleus (PVN), hypothalamic lesion area (LHA), and arcuate nucleus (Arc) all showed increased expression of C-Fos 10–24 hours following intraperitoneal injection due to C75-like distention fasting? Over 95% of the mouse body weight can be absorbed in 2 hours by intraperitoneal injection of C75 at a dose of 30 mg/kg body weight [3]. Because of medium oxidation, DIO mice administered with C75 boosted their energy output by 32.9 percent and lost 50% of their body weight. Even in the presence of high malonyl-CoA concentrations, C75 treatment of odontozoan adipocytes, hepatocytes, and human breast cancer cells boosts medium oxidation and ATP levels through boosting CPT-1 activity [4].
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References |
[1]. Rae C, et al. Inhibition of Fatty Acid Synthase Sensitizes Prostate Cancer Cells to Radiotherapy.
[2]. Makowski K, et al. Differential pharmacologic properties of the two C75 enantiomers: (+)-C75 is a strong anorectic drug; (-)-C75 has antitumor activity. Chirality. 2013 May;25(5):281-7. [3]. Gao S, et al. Effect of the anorectic fatty acid synthase inhibitor C75 on neuronal activity in the hypothalamus and brainstem. Proc Natl Acad Sci U S A. 2003 May 13;100(10):5628-33. [4]. Thupari JN, et al. C75 increases peripheral energy utilization and fatty acid oxidation in diet-induced obesity. Proc Natl Acad Sci U S A. 2002 Jul 9;99(14):9498-502. [5]. Yan Xue, et al. Inhibition of Carnitine Palmitoyltransferase 1A Aggravates Fatty Liver Graft Injury via Promoting Mitochondrial Permeability Transition. Transplantation. 2021 Mar 1;105(3):550-560 |
Molecular Formula |
C14H22O4
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Molecular Weight |
254.32208
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CAS # |
218137-86-1
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Related CAS # |
trans-C75;191282-48-1;(−)-C75;1234694-22-4
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SMILES |
O=C(C(C1=C)C(CCCCCCCC)OC1=O)O
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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) |
DMSO : ≥ 83.3 mg/mL (~327.54 mM)
H2O : < 0.1 mg/mL |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.83 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 (9.83 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 (9.83 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: ≥ 1.25 mg/mL (4.92 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 1.25 mg/mL (4.92 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. 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. Solubility in Formulation 6: ≥ 1.25 mg/mL (4.92 mM) (saturation unknown) in 5% DMSO + 95% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.9321 mL | 19.6603 mL | 39.3205 mL | |
5 mM | 0.7864 mL | 3.9321 mL | 7.8641 mL | |
10 mM | 0.3932 mL | 1.9660 mL | 3.9321 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.