| Size | Price | |
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| 100mg | ||
| 250mg | ||
| 500mg | ||
| Other Sizes |
| 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) also inhibits the development of LNCaP spheroids in a concentration-dependent way [1]. Without changing food intake, (-)-C75 cytotoxically affects tumor cell lines and suppresses FAS function. Since (+)-C75 inhibits CPT1 and causes anorexia when administered, it appears that central CPT1 inhibition is necessary for C75's anorexigenic actions. The distinct actions of the C75 enantiomers could result in the creation of novel medications targeted specifically at fat and cancer [2].
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|---|---|
| ln Vivo |
10–24 hours following intraperitoneal administration, C75 inhibits the expression of c-Fos caused by fasting in the paraventricular nucleus (PVN), lateral hypothalamic region (LHA), and arcuate nucleus (Arc). Within two hours, mice's food intake can be inhibited by up to 95% when given an intraperitoneal injection of 30 mg/kg body weight of C75 [3]. Fatty acid oxidation caused DIO mice administered with C75 to lose 50% of their body weight and boost their energy production by 32.9 percent. Even in the face of high amounts of malonyl-CoA, C75 treatment of rodent adipocytes, hepatocytes, and human breast cancer cells boosts fatty acid oxidation and ATP levels through boosting CPT-1 activity [4].
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| References |
[1]. 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.
[2]. Rae C, et al. Inhibition of Fatty Acid Synthase Sensitizes Prostate Cancer Cells to Radiotherapy. [3]. 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. [4]. 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. [5]. 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
|
|---|---|
| Molecular Weight |
254.32
|
| CAS # |
1234694-22-4
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| Related CAS # |
C75;218137-86-1;trans-C75;191282-48-1
|
| SMILES |
CCCCCCCC[C@@H]1OC(=O)C(=C)[C@H]1C(=O)O
|
| 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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| 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.
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