1. Membrane Transporter/Ion Channel
    Metabolic Enzyme/Protease
  2. Potassium Channel
    Dipeptidyl Peptidase
  3. Nateglinide

Nateglinide (Synonyms: A4166; Senaglinide)

Cat. No.: HY-B0422 Purity: 98.11%
Handling Instructions

Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K+ channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus[1][2].

For research use only. We do not sell to patients.

Nateglinide Chemical Structure

Nateglinide Chemical Structure

CAS No. : 105816-04-4

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10 mM * 1 mL in DMSO USD 66 In-stock
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100 mg USD 370 In-stock
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Description

Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K+ channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus[1][2].

In Vitro

Nateglinide inhibits typical recordings of dinitrophenol-induced KATP currents in a concentration-dependent manner. Nateglinide exhibits IC50 values of 7.4 μM and 2.4 μM for 5 mM glucose (G5) and 16 mM (G16) glucose, respectively[2].

RT-PCR[2]

Cell Line: Rat pancreatic β-cells.
Concentration: 0-100 μM.
Incubation Time: ~20 min.
Result: Produced a complete inhibition of KATP current at concentration of 3 μM.
In Vivo

Nateglinide (50mg/kg, orally in mice) stimulates human C-peptide secretion in the humanized mice and improved postprandial glucose concentrations[3].

Animal Model: Mice[3].
Dosage: 50mg/kg.
Administration: Orally at 60min before oral administration of 4 g/kg glucose.
Result: Stimulates human C-peptide secretion.
Clinical Trial
Molecular Weight

317.42

Formula

C₁₉H₂₇NO₃

CAS No.

105816-04-4

SMILES

O=C(O)[[email protected]@H](CC1=CC=CC=C1)NC([[email protected]]2CC[[email protected]](C(C)C)CC2)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (315.04 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1504 mL 15.7520 mL 31.5040 mL
5 mM 0.6301 mL 3.1504 mL 6.3008 mL
10 mM 0.3150 mL 1.5752 mL 3.1504 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.88 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.88 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.88 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

NateglinideA4166SenaglinideA 4166A-4166Potassium ChannelDipeptidyl PeptidaseKcsADPPglucoseinsulindiabetesshort-actingβ-cellInhibitorinhibitorinhibit

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Nateglinide
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