ACLY-IN-1
ACLY-IN-1 is an orally active ACLY inhibitor. ACLY-IN-1 exhibits potent ACLY inhibitory activity (IC50 = 8.3 nM) and high binding affinity (KD = 72.0 nM) to ACLY. ACLY-IN-1 demonstrates good pharmacokinetic profiles and a potent in vivo hypolipidemic effect.
For research use only. We do not sell to patients.
- CAS No.: 2897695-26-8
- Formula: C20H12BrClF2N2O4S
- Molecular Weight:529.74
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
ACLY-IN-1 is very stable in human microsomes with long half-life (T1/2 > 120 min) and low intrinsic microsome clearance (Clint = 6.7 mL/min/kg)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
In Vivo
ACLY-IN-1 (1 g/kg, p.o.) has no death of C57BL/6JNifdc mice and no obvious toxic effects within 1 week after the treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male LDL-R-/- mice (7-8 weeks)[1]
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Dosage:30 mg/kg
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Administration:p.o., 30 mg/kg, once daily for 8 weeks.
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Result:Reduced serum triglyceride.
Reduced total cholesterol and LDL-c levels.
Reduced the liver weight and liver/body weight ratio.
Reversed the elevated hepatic triglyceride and total cholesterol in in LDL-R-/- mice.
Chemical Information
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CAS No. 2897695-26-8
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Molecular Weight 529.74
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Formula C20H12BrClF2N2O4S
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SMILES
ClC1=CC2=CC(S(=O)(NC3=CC(C4=C(C=CC(Br)=C4)CNC2=O)=C(C=C3F)F)=O)=C1O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)