2. Metabolic Enzyme/Protease
  3. ATP Citrate Lyase
  4. 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.

ACLY-IN-1

ACLY-IN-1 Chemical Structure

CAS No. : 2897695-26-8

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ACLY-IN-1 Related Antibodies

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Description

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[1].

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.

ACLY-IN-1 Related Antibodies
Parmacokinetics
Species Dose Route F T1/2 Tmax MRT Cmax AUC0-t CL
Rat[1] 10 mg/kg p.o. 58.1 % 6.6 h 2.0 h 4.4 h 12633 ng/mL 54101 ng·h/mL /
Rat[1] 2 mg/kg i.v. / 9 h / 3.9 h 35866 ng/mL 17877 ng·h/mL 1.7 mL/min/kg
In Vivo

ACLY-IN-1 (compound 55) (30 mg/kg, p.o., once daily for 8 weeks) has lipid-lowering effect in male LDL-R-/- mice[1].
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.

Animal Model: Male LDL-R-/- mice (7-8 weeks)[1]
Dosage: 30 mg/kg
Administration: p.o., 30 mg/kg, once daily for 8 weeks.
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.
Molecular Weight

529.74

Formula

C20H12BrClF2N2O4S
CAS No.
SMILES

ClC1=CC2=CC(S(=O)(NC3=CC(C4=C(C=CC(Br)=C4)CNC2=O)=C(C=C3F)F)=O)=C1O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ACLY-IN-1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ACLY-IN-12897695-26-8ATP Citrate LyaseACLYlipogenic enzymemetabolic and cardiovascular diseasesHyperlipidemiaInhibitorinhibitorinhibit

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