GSK837149A is a selective inhibitor of human Fatty Acid Synthase (FASN) targeting the KR domain. GSK837149A has reversible inhibition effect on FASN and selectivity for type I FASN (Ki=30 nM). GSK837149A is also a competitive inhibitor of NADPH and a non-competitive inhibitor of acetoacetyl-CoA. GSK837149A can be used for the research of obesity and breast cancer.
| Molecular Weight | 554.6 |
| Formula | C23H22N8O5S2 |
| CAS Number | 13616-29-0 |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related FAS Products |
|---|
| IPI-9119
IPI-9119 is an orally active, selective and irreversible Fatty Acid Synthase (FASN) inhibitor, with an IC50 of 0.3 nM. |
| Eicosapentaenoic acid ethyl ester
Eicosapentaenoic acid ethyl ester (AMR101, EPA ethyl ester, Ethyl eicosapentaenoate) is an omega-3 fatty acid agent that significantly reduces the triglyceride (TG) levels and improves other lipid parameters without significantly increasing the low-density lipoprotein (LDL) cholesterol levels. |
| FT113
FT113 is a potent inhibitor of fatty acid synthase(FASN) with ic50 of 213 nM. |
| PF429242 dihydrochloride
PF429242 dihydrochloride is a reversible and competitive SREBP site 1 protease (S1P) inhibitor with an IC50 of 175 nM. |
| Lycorine
Lycorine is a natural alkaloid extracted from the Amaryllidaceae plant. |
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