FABP4/5-IN-7
FABP4/5-IN-7 is a dual FABP4/FABP5 inhibitor, with an IC50 of 0.8 μM and a Kd of 0.01 μM for FABP4, and an IC50 of 1.4 μM for FABP5. FABP4/5-IN-7 inhibits lipolysis in adipocytes. FABP4/5-IN-7 inhibits MCP-1 release in macrophages. FABP4/5-IN-7 improves dyslipidemia in diet-induced obese mice. FABP4/5-IN-7 can be used in studies related to dyslipidemia.
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- CAS No.: 1227413-92-4
- 화학식: C19H15ClN4O2
- 분자량:366.80
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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FABP4 0.8 μM (IC50) |
FABP4 0.01 μM (Kd) |
FABP5 1.4 μM (IC50) |
FABP3 0.52 μM (Kd) |
FABP4/5-IN-7 (Compound 2) (15-100 μM) binds to recombinant FABP4 with high affinity (Kd = 0.01 μM) and to recombinant FABP3 with lower affinity (Kd = 0.52 μM) in TdF assays[1].
FABP4/5-IN-7 (10 μM) significantly inhibits basal lipolysis in fully differentiated 3T3-L1 adipocytes[1].
FABP4/5-IN-7 (3-30 μM; 1 h pre-incubation, followed by 4 h incubation with isoproterenol) inhibits isoprenaline (HY-B0468)-stimulated lipolysis in fully differentiated 3T3-L1 adipocytes[1].
FABP4/5-IN-7 (0.008-25 μM; 4 h) inhibits isoprenaline-stimulated lipolysis in primary human adipocytes, with an IC50 of 22 μM[1].
FABP4/5-IN-7 (24 h) inhibits basal MCP-1 release from THP-1 macrophage-like cells differentiated with PMA (HY-18739), with an IC50 of 7.5 μM[1].
FABP4/5-IN-7 (0.39-25 μM; 1 h pre-incubation, followed by 3 h incubation with LPS) significantly inhibits LPS (HY-D1056)-induced MCP-1 release from PMA-differentiated THP-1 macrophage-like cells at the concentration of 25 μM[1].
FABP4/5-IN-7 (1-25 μM; overnight) inhibits MCP-1 release from primary human macrophages at a concentration of 25 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
FABP4/5-IN-7 (30 mg/kg; p.o.; daily; for 3 consecutive days) shows a fat/plasma concentration ratio of 0.09 in diet-induced obese mice, with the proportion of free drug in plasma being <1%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (leptin-deficient Lep^ob/Lep^ob)[1]
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Dosage:30 mg/kg
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Administration:diet; daily; 8 weeks
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Result:Produced a minor improvement in intraperitoneal insulin tolerance tests.
Showed no decrease in body weight.
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Animal Model:C57BL/6J mice (diet-induced obesity, DIO)[1]
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Dosage:30 mg/kg
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Administration:diet; daily; 3 days
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Result:Achieved a fat/plasma concentration ratio of 0.09.
Resulted in <1% free drug fraction in plasma.
Chemical Information
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CAS No. 1227413-92-4
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분자량 366.80
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화학식 C19H15ClN4O2
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SMILES
O=C1C=C(COC2=C(C)C(Cl)=CC=C2)N=C3NC(C4=CC=CC=C4)=NN13
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FABP4/5-IN-7 Related Classifications
HY-183836 Related Classifications
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