Bisegliptin
Bisegliptin (KRP-104) is a small molecule compound with antidiabetic activity. Bisegliptin is metabolized mainly by converting the cyano group to the carboxylic acid form, and DPP-4 plays a partial role in its metabolism. The carboxylic acid metabolite of bisegliptin can be detected both in vivo and in vitro. In rat experiments, the plasma concentration of the carboxylic acid metabolite of bisegliptin was affected by other DPP inhibitors, showing the complexity of its metabolic process. The amide intermediate of bisegliptin was detected both in vivo and in vitro, and its conversion rate was significantly faster than that of the parent compound when incubated with DPP-4.
For research use only. We do not sell to patients.
- CAS No.: 862501-61-9
- Formula: C18H26FN3O3
- Molecular Weight:351.42
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Storage:
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
- Protocols
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Biological Activity
Description
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 862501-61-9
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Molecular Weight 351.42
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Formula C18H26FN3O3
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SMILES
CCOC(C12CCC(CC2)(NCC(N3C[C@@H](F)C[C@H]3C#N)=O)CC1)=O
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Synonyms
KRP-104
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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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Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Bisegliptin Related Classifications
HY-121029 Related Classifications
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