2. Membrane Transporter/Ion Channel
  3. Sodium Phosphate Cotransporter
  4. 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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LY3358966

LY3358966 Chemical Structure

CAS No. : 2187395-66-8

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Description

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[1].

In Vitro

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 Related Antibodies
Parmacokinetics
Species Dose Route AUC T1/2 Cmax Tmax F
Mice[1] 1 mg/kg i.v. 323 nM·h 5 h / / /
Mice[1] 1 mg/kg p.o. 39 nM·h / 25 nM 0.4 h 12 %
Mice[1] 3 mg/kg p.o. 96 nM·h / 50 nM 0.4 h 10 %
Mice[1] 10 mg/kg p.o. 284 nM·h / 83 nM 0.4 h 9 %
In Vivo

LY3358966 (0.0001-100 mg/kg; p.o.; single dose) dose-dependently inhibits acute intestinal phosphate uptake into plasma in healthy mice and rats[1].
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.

Animal Model: C57BL/6 (male, 9 weeks old, 23-28 g)[1]
Dosage: 9 mg/kg
Administration: p.o.; three doses at 4-hour intervals
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.
Molecular Weight

801.94

Formula

C43H49F2N5O6S
CAS No.
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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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LY3358966 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:

LY33589662187395-66-8LY 3358966LY-3358966Sodium Phosphate CotransporterNPT2bPiT1mouseCHO cellsNPT2aNPT2crenal diseaserathumansodium-dependent phosphate cotransporter 2bInhibitorinhibitorinhibit

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