C75 FASN inhibitor

C75 FASN inhibitor, also known as (±)-C75, is a stable inhibitor of FASN that leads to profound weight loss and feeding inhibition in both high-fat diet wild type obese and leptin-deficient ob/ob mice.

Product information

CAS Number: 191282-48-1

Molecular Weight: 254.32

Formula: C14H22O4

Synonym:

C75

(±)-C75

Chemical Name: tetrahydro-4-methylene-2R-octyl-5-oxo-3S-furancarboxylic acid

Smiles: CCCCCCCC[C@@]1(CC(=C)C(=O)O1)C(O)=O

InChiKey: CXEUTPLFFCPBCO-CQSZACIVSA-N

InChi: InChI=1S/C14H22O4/c1-3-4-5-6-7-8-9-14(13(16)17)10-11(2)12(15)18-14/h2-10H2,1H3,(H,16,17)/t14-/m1/s1

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

trans-C75 ((±)-C75) inhibits PC3 cell growht with an IC50 of 35 μM at 24 h. trans-C75 ((±)-C75)(10-50 μM) also reduces the growth of LNCaP spheroids in a concentration-dependent manner with an IC50 of 50 μM. trans-C75 ((±)-C75) inhibits FAS activity and has a cytotoxic effect on tumor cell lines, without affecting food consumption. trans-C75 ((±)-C75) inhibits CPT1 and its administration produces anorexia, suggesting that central inhibition of CPT1 is essential for the anorectic effect of C75. The differential activity of C75 enantiomers may lead to the development of potential new specific drugs for cancer and obesity.

In Vivo:

C75 blocks fasting-induced c-Fos expression in the arcuate nucleus (Arc), lateral hypothalamic area (LHA), and paraventricular nucleus (PVN) 10–24 h after i.p. injection. Intraperitoneal administration of C75 at 30 mg/kg body weight inhibits food intake of mice by ≥95% within 2 h after i.p. injection[3]. C75-treated DIO mice has a 50% greater weight loss, and a 32.9% increased production of energy because of fatty acid oxidation. C75 treatment of rodent adipocytes and hepatocytes and human breast cancer cells increases fatty acid oxidation and ATP levels by increasing CPT-1 activity, even in the presence of elevated concentrations of malonyl-CoA.

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.

Products are for research use only. Not for human use.