LY3358966
LY3358966 is an orally active sodium-dependent phosphate cotransporter 2b (NPT2b) inhibitor with a human IC50 of 32.4 nM, mouse IC50 of 43.9 nM, and rat of IC50 26.8 nM. LY3358966 inhibits NPT2b-mediated intestinal phosphate transport, decreases acute phosphate uptake into plasma, and increases fecal phosphate excretion. LY3358966 can be used for the research of renal disease.
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- CAS No.: 2187395-66-8
- 화학식: C43H49F2N5O6S
- 분자량:801.94
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
LY3358966 potently inhibits NPT2b (human IC50 = 32.4 nM, mouse IC50 = 43.9 nM, rat IC50 26.8 nM), also inhibits human NPT2a and NPT2c, and is highly selective against human PiT1 and PiT2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
LY3358966 (10-100 mg/kg; p.o.; single dose) does not affect gastric emptying in healthy Mus musculus at doses up to 100 mg/kg[1].
LY3358966 (9 mg/kg; p.o.; three doses at 4-hour intervals) increases fecal phosphate excretion in healthy mice, raising the percentage of radiolabeled phosphate recovered in feces from 9.86% to 18.44% over 48 hours[1].
LY3358966 (10 mg/kg; p.o.; single dose) modestly increases fecal phosphate excretion and gastrointestinal phosphate retention in healthy rats, producing a 5.34% increase in 48-hour fecal phosphate recovery and a 6.34% increase in 4-hour gastrointestinal phosphate retention at 10 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 9 weeks old, 23-28 g)[1]
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Dosage:9 mg/kg
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Administration:p.o.; three doses at 4-hour intervals
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Result:Significantly increased radiolabeled phosphate recovered in feces over 48 hours to 18.44% of the dose, compared to 9.86% in vehicle-treated controls.
Chemical Information
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CAS No. 2187395-66-8
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분자량 801.94
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화학식 C43H49F2N5O6S
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SMILES
O=C(C1=CC=C(CCC2=C(C=C(NC(C3=C(NC(C4=CC=CC(CN5CCN(CC5(C)C)C(NCCCCO)=O)=C4)=O)SC6=C3CCCC6)=O)C=C2F)F)C=C1)O
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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)
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