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    Nateglinide (Starlix; A4166)
    Nateglinide (Starlix; A4166)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0198
    CAS #: 105816-04-4Purity ≥98%

    Description: Nateglinide (formerly A-4166; trade names: Fastic, Starlix), a meglitinide analog, is a potent and orally bioavailable antihyperglycemic medication used for treating type 2 diabetes [non-insulin-dependent diabetes mellitus (NIDDM)]. It lowers blood glucose levels by acting as an insulin secretagog agent which stimulates insulin secretion from the pancreas. It is a short-acting insulin secretagogue that inhibits ATP-sensitive K+ channels in pancreatic β-cells, which depolarizes the β cells and opens voltage-gated calcium channels, leading to calcium influx and fusion of insulin-containing vesicles with the cell membrane, and insulin secretion occurs.

    References: Expert Opin Pharmacother. 2011 Sep;12(13):2097-106.

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    Molecular Weight (MW)317.42 
    CAS No.105816-04-4 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 63 mg/mL (198.5 mM) 
    Water: <1 mg/mL
    Ethanol: 63 mg/mL (198.5 mM) 
    Other info

    Chemical Name: (R)-2-((1r,4R)-4-isopropylcyclohexanecarboxamido)-3-phenylpropanoic acid


    InChi Code: InChI=1S/C19H27NO3/c1-13(2)15-8-10-16(11-9-15)18(21)20-17(19(22)23)12-14-6-4-3-5-7-14/h3-7,13,15-17H,8-12H2,1-2H3,(H,20,21)(H,22,23)/t15-,16-,17-/m1/s1

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

    SynonymsA-4166; A 4166; DJN-608l; DJN608; A4166; DJN 608; Nateglinide; Fastic; Starlix

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    In Vitro

    In vitro activity: Nateglinide is an insulin secretagog agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). Nateglinide is an oral antihyperglycemic agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM). It belongs to the meglitinide class of short-acting insulin secretagogues, which act by binding to β cells of the pancreas to stimulate insulin release. Nateglinide is an amino acid derivative that induces an early insulin response to meals decreasing postprandial blood glucose levels. It should only be taken with meals and meal-time doses should be skipped with any skipped meal. Approximately one month of therapy is required before a decrease in fasting blood glucose is seen. Meglitnides may have a neutral effect on weight or cause a slight increase in weight. The average weight gain caused by meglitinides appears to be lower than that caused by sulfonylureas and insulin and appears to occur only in those na?ve to oral antidiabetic agents. Due to their mechanism of action, meglitinides may cause hypoglycemia although the risk is thought to be lower than that of sulfonylureas since their action is dependent on the presence of glucose. In addition to reducing postprandial and fasting blood glucose, meglitnides have been shown to decrease glycosylated hemoglobin (HbA1c) levels, which are reflective of the last 8-10 weeks of glucose control. Meglitinides appear to be more effective at lowering postprandial blood glucose than metformin, sulfonylureas and thiazolidinediones. Nateglinide is extensively metabolized in the liver and excreted in urine (83%) and feces (10%). The major metabolites possess less activity than the parent compound. One minor metabolite, the isoprene, has the same potency as its parent compound .

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    ReferencesExpert Opin Pharmacother. 2011 Sep;12(13):2097-106.

    These protocols are for reference only. InvivoChem does not independently validate these methods.


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