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| Size | Price | Stock |
|---|---|---|
| 250mg | $1020 | Check With Us |
| 500mg | $1480 | Check With Us |
| 1g | $2220 | Check With Us |
: Cat #: V0856 CAS #: 1030612-90-8; Purity ≥ 98%
Description: MK-8245 (MK8245; MK 8245) is a novel and potent liver-targeted inhibitor of stearoyl-CoA desaturase (SCD) with anti-diabetic and anti-dyslipidemic activities. It inhibits stearoyl-CoA desaturase with an IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1. It exhibits high anti-diabetic and anti-dyslipidemic efficacy in vivo and a significantly improved therapeutic window.
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| Molecular Weight (MW) | 467.25 |
|---|---|
| Molecular Formula | C17H16BrFN6O4 |
| CAS No. | 1030612-90-8; |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 93 mg/mL (199.0 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| Solubility In Vivo | 1% CMC+0.5% Tween-80: 30mg/mL |
| SMILES Code | FC1=CC=C(Br)C(OC2CCN(C3=NOC(C4=NNN=N4)=C3)CC2)=C1 |
| Synonyms | MK-8245; MK 8245; MK8245; |
| Protocol | In Vitro | MK-8245 exhibits a significant SCD inhibition in the rat hepatocyte assay which contains functional, actives organic anion transporting polypeptides (OATPs) with IC50 of 68 nM, while being only weakly active OATPs in the HepG2 cell assay which is devoid of active with IC50 of ~1 μM. 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 SCD. MK-8245 is a potent and liver-specific SCD inhibit. |
|---|---|---|
| In Vivo | MK-8245 improves glucose clearance in a dose-dependent manner in eDIO mice administrated before the glucose challenge. MK-8245 (10mg/kg; p.o.) exhibits a tissue distribution profile concentrated in the liver, with low exposure in tissues associated with potential adverse events in rats, dogs, and rhesus monkeys. |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.1402 mL | 10.7009 mL | 21.4018 mL | 42.8036 mL |
| 5mM | 0.4280 mL | 2.1402 mL | 4.2804 mL | 8.5607 mL |
| 10mM | 0.2140 mL | 1.0701 mL | 2.1402 mL | 4.2804 mL |
| 20mM | 0.1070 mL | 0.5350 mL | 1.0701 mL | 2.1402 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (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.