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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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C75 trans [(±)-C75] is an isomer/enantiomer of C75 which is a synthetic fatty-acid synthase (FASN) inhibitor. It has weight loss and feeding inhibition in both high-fat diet wild type obese and leptin-deficient ob/ob mice.
ln Vitro |
trans-C75 ((±)-C75) inhibits PC3 cell growth with an IC50 of 35 μM at 24 hours. trans-C75 ((±)-C75) (10-50 μM) still decreases the development of LNCaP spheres at concentrated concentrations trans-C75 ((±)-C75) is active in inhibiting FAS and has cytotoxic effects on tumor cell types. Does not alter culture media. trans-C75 ((±)-C75) inhibits CPT1, and the differential activity of its C75 on enantiomers may lead to the development of possible novel cancer and luminescence medicines [2].
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ln Vivo |
Ten to twenty-four hours after intraperitoneal injection, C75 inhibited the expression of c-Fos caused by fasting in the paraventricular nucleus (PVN), hypothalamic ischemia region (LHA), and arcuate nucleus (Arc). After intraperitoneal injection of 30 mg/kg C75, within 2 hours, ≥ 95% of the suspended mice had eaten [3]. Mice treated with C75 showed a 50% reduction in body weight and a 32.9% increase in output as a result of mild oxidation. Even in the face of increased amounts of malonyl-CoA, C75 treatment of animal adipocytes, hepatocytes, and human mammary tissue methanol enhances plant oxidation and ATP levels via raising 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 |
Molecular Formula |
C₁₄H₂₂O₄
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Molecular Weight |
254.32
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CAS # |
191282-48-1
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Related CAS # |
C75;218137-86-1;(−)-C75;1234694-22-4
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SMILES |
O=C([C@@H](C1=C)[C@@H](CCCCCCCC)OC1=O)O
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InChi Key |
CWLZDVWHQVAJU-JHJMLUEUSA-N
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InChi Code |
InChI=1S/C14H22O4/c1-3-4-5-6-7-8-9-11-12(13(15)16)10(2)14(17)18-11/h11-12H,2-9H2,1H3,(H,15,16)/t11-,12?/m1/s1
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Chemical Name |
tetrahydro-4-methylene-2R-octyl-5-oxo-3S-furancarboxylic acid
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Synonyms |
(±)-C75 C75 C75 FASN inhibitor
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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 (~327.53 mM)
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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), suspension 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. |
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.