MK-8245 (Trifluoroacetate) [CAS 1415559-41-9]
MK-8245 (Trifluoroacetate) [CAS 1415559-41-9]
SKU:QM-0000451
Couldn't load pickup availability
Request quote or documents
![MK-8245 (Trifluoroacetate) [CAS 1415559-41-9]](http://quantimol.com/cdn/shop/files/quantimol-021.png?v=1773515276&width=1445)
Product Details
-
Description
MK-8245 trifluoroacetate is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy. IC50 value: 1 nM (hSCD1) [1] Target: SCD1 in vitro: MK-8245, a phenoxy piperidine isoxazole derivative, has been identified as a potent and liver-specific SCD inhibitor. It contains a tetrazole acetic acid moiety, which is the key molecule for OATPs recognition and liver-targeting. MK-8245 displays similar potencies against human, rat and mouse SCD1 with IC50 values of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1. MK-8245 exhibits a significant SCD inhibition in the rat hepatocyte assay which contains functional, active OATPs with IC50 of 68 nM, while being only weakly active in the HepG2 cell assay which is devoid of active OATPs with IC50 of ~1 μM. MK-8245 displays highly selective activity for the Δ-5 and Δ-6 desaturases (i.e., >100000 μM vs rat and human Δ5D and Δ6D as assessed in the HepG assay [1]. in vivo: Administration of MK-8245 at 10 mg/kg in mice exhibits a tissue distribution profile concentrated in the liver. It shows a liver-to-Harderian gland ratio of 21, suggesting a high degree of liver-targeting compared to a systemically distributed compound with liver-to-Harderian gland ratio of 1.5. Oral dosing of MK-8245 in mice, rats, dogs, and rhesus monkeys demonstrates that MK-8245 is distributed mainly to the liver, with low exposure in tissues associated with potential adverse events. The liver-to-skin ratios are >30:1 in all four species. Administration of MK-8245 to eDIO mice before the glucose challenge improves glucose clearance in a dose-dependent manner with ED50 of 7 mg/kg.
-
CAS Number
[1415559-41-9]
-
Molecular Formula
C19H17BrF4N6O6
-
Molecular Weight
581.27
-
Smiles
O=C(CN1N=C(N=N1)C2=CC(N3CCC(CC3)OC4=CC(F)=CC=C4Br)=NO2)O.FC(C(O)=O)(F)F
-
Target
Stearoyl-CoA Desaturase (SCD)
-
Purity
98.45
-
Solubility
10 mM in DMSO
-
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
-
Shipping Conditions
Room Temperature
Related Products
- QM-0054857-01 α-Ketoglutaric acid (disodium dihydrate) [CAS 1282616-74-3]
- QM-0054003 δ-Hexachlorocyclohexane-13C6
- QM-0053803 γ-Linolenic acid ethyl ester-d5
- QM-0052819-01 Zolpidem phenyl-4-carboxylic acid ethyl ester-d6 [CAS 1216455-48-9]
- QM-0052711 α-D-Glucopyranoside, 2-chloro-4-nitrophenyl, 2,3,4,6-tetraacetate [CAS 153823-58-6]
- QM-0052492-01 α-D-Galactopyranose,2- (acetylamino) -2-deoxy-,1,3,4,6-tetraacetate [CAS 10385-50-9]
- QM-0051894-01 β-D-Glucopyranoside,2-bromoethyl,2,3,4,6-tetraacetate [CAS 16977-78-9]
- QM-0051893 β-D-Glucopyranoside,2-chloro-4-nitrophenyl,2,3,4,6-tetraacetate [CAS 35023-71-3]
- QM-0051820-01 β-D-Glucopyranuronic acid, methyl ester,1,2,3,4-tetrakis (2-methylpropanoate) [CAS 150607-94-6]
- QM-0051622-01 α-Ketoglutaric acid (disodium hydrate)
Other industry favorites
- QM-0054857-01 α-Ketoglutaric acid (disodium dihydrate) [CAS 1282616-74-3]
- QM-0054003 δ-Hexachlorocyclohexane-13C6
- QM-0206023-01 α-Demethylnaproxen [CAS 23981-47-7]
- QM-0203548-01 α-Acetobromo-D-xylose, 95% [CAS 3068-31-3]
- QM-0071124 β-D-Ribofuranose, 3-deoxy-3-fluoro-, 1,2-diacetate 5- (4-methylbenzoate) [CAS 1884324-98-4]
- QM-0131262 [Thr28, Nle31]-Cholecystokinin (25-33), sulfated [CAS 77568-41-3]
- QM-0023392 α-Mycolic acid, keto cis [CAS 2260795-20-6]
- QM-0022881 [R- (Z) ]-4-Amino-3-chloro-2-pen-tenedioicacid [CAS 90288-29-2]
- QM-0167516 α-D-Glucopyranoside, methyl 4-deoxy-4-fluoro,2,3,6-tribenzoate [CAS 84065-98-5]
- QM-0166583-01 β-D-Galactosyl- (1→3) -N-acetyl-D-galactosamine [CAS 3554-90-3]
MK-8245 (Trifluoroacetate) [CAS 1415559-41-9]
MK-8245 (Trifluoroacetate) is a premium-grade research compound supplied by Quantimol for laboratory and scientific applications.