CAS 105816-04-4|Nateglinide
Introduction：Basic information about CAS 105816-04-4|Nateglinide, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Nateglinide | ||
|---|---|---|---|
| CAS Number | 105816-04-4 | Molecular Weight | 317.423 |
| Density | 1.1±0.1 g/cm3 | Boiling Point | 527.6±39.0 °C at 760 mmHg |
| Molecular Formula | C19H27NO3 | Melting Point | 137-141ºC |
| MSDS | ChineseUSA | Flash Point | 272.9±27.1 °C |
Names
| Name | nateglinide |
|---|---|
| Synonym | More Synonyms |
Nateglinide BiologicalActivity
| Description | Nateglinide is an insulin secretagog agent used for the treatment of non-insulin-dependent diabetes mellitus (NIDDM).Target: OthersNateglinide 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 [1-3]. |
|---|---|
| Related Catalog | Signaling Pathways >>Others >>OthersResearch Areas >>Cardiovascular Disease |
| References | [1]. http://205.193.93.51/dpdonline/searchRequest.dodin=2245439 [2]. http://www.drugs.com/cdi/nateglinide.html [3]. http://www.drugbank.ca/drugs/DB00731 |
Chemical & Physical Properties
| Density | 1.1±0.1 g/cm3 |
|---|---|
| Boiling Point | 527.6±39.0 °C at 760 mmHg |
| Melting Point | 137-141ºC |
| Molecular Formula | C19H27NO3 |
| Molecular Weight | 317.423 |
| Flash Point | 272.9±27.1 °C |
| Exact Mass | 317.199097 |
| PSA | 66.40000 |
| LogP | 4.21 |
| Vapour Pressure | 0.0±1.5 mmHg at 25°C |
| Index of Refraction | 1.536 |
| Storage condition | Room temp |
Toxicological Information
CHEMICAL IDENTIFICATION |
ACUTE TOXICITY DATA - TYPE OF TEST :
- LD - Lethal dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- >2 gm/kg
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Gastrointestinal - hypermotility, diarrhea
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 25(Suppl 1),S5,1997
- TYPE OF TEST :
- LD - Lethal dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- >2 gm/kg
- TOXIC EFFECTS :
- Gastrointestinal - nausea or vomiting
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 25(Suppl 1),S9,1997 ** OTHER MULTIPLE DOSE TOXICITY DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 90 gm/kg/13W-I
- TOXIC EFFECTS :
- Endocrine - changes in adrenal weight Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 25(Suppl 1),S13,1997
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 182 gm/kg/52W-I
- TOXIC EFFECTS :
- Gastrointestinal - changes in structure or function of salivary glands Gastrointestinal - ulceration or bleeding from stomach Nutritional and Gross Metabolic - weight loss or decreased weight gain
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 25(Suppl 1),S63,1997
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 27300 mg/kg/13W-I
- TOXIC EFFECTS :
- Gastrointestinal - changes in structure or function of salivary glands Liver - change in gall bladder structure or function Related to Chronic Data - death
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 25(Suppl 1),S35,1997
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 36400 mg/kg/52W-I
- TOXIC EFFECTS :
- Gastrointestinal - changes in structure or function of salivary glands
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 25(Suppl 1),S79,1997 ** REPRODUCTIVE DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 27 gm/kg
- SEX/DURATION :
- female 17-22 day(s) after conception lactating female 1-21 day(s) post-birth
- TOXIC EFFECTS :
- Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
- REFERENCE :
- YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 25(Suppl 1),S139,1997
Safety Information
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
|---|---|
| Hazard Codes | Xn: Harmful; |
| Risk Phrases | R22 |
| Safety Phrases | 24/25-36 |
| RIDADR | NONH for all modes of transport |
| RTECS | SQ7318950 |
| HS Code | 2924299090 |
Customs
| HS Code | 2924299090 |
|---|---|
| Summary | 2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0% |
Articles50
More Articles| Formulation and in vitro evaluation of nateglinide microspheres using HPMC and carbopol-940 polymers by ionic gelation method. Pak. J. Pharm. Sci. 26(6) , 1229-35, (2013) This study involves the design and characterization of Nateglinide (NAT) microspheres to enhance patient compliance. Ionic gelation technique was used to prepare Nateglinide Microspheres by using rate... | |
| From evidence assessments to coverage decisions?: the case example of glinides in Germany. Health Policy 104(1) , 27-31, (2012) In Germany, coverage decisions in the statutory health insurance (SHI) system are based on the principles of evidence-based medicine. Recently, an evidence assessment by the Institute for Quality and ... | |
| Nateglinide--current and future role in the treatment of patients with type 2 diabetes mellitus. Int. J. Clin. Pract. 59(10) , 1218-28, (2005) Therapy for type 2 diabetes mellitus should aim to control not only fasting, but also postprandial glucose levels. Nateglinide, a d-phenylalanine derivative, restores postprandial early phase insulin ... |
Synonyms
| Glinate |
| Starsis |
| SDZ DJN 608 |
| Starlix |
| (2R)-2-{[(trans-4-Isopropylcyclohexyl)carbonyl]amino}-3-phenylpropanoic acid |
| N-{[trans-4-(1-methylethyl)cyclohexyl]carbonyl}-D-phenylalanine |
| (-)-N-(trans-4-Isopropylcyclohexanecarbonyl)-D-phenylalanine |
| (2R)-2-({[trans-4-(1-methylethyl)cyclohexyl]carbonyl}amino)-3-phenylpropanoic acid |
| DJN 608 |
| Natelide |
| N-[[trans-4-(1-Methylethyl)cyclohexyl]carbonyl]-D-phenylalanine |
| N-{[trans-4-(Propan-2-yl)cyclohexyl]carbonyl}-D-phenylalanin |
| MFCD00875706 |
| ay4166 |
| Starlix DS |
| Fastic-d5 |
| A-4166 |
| Fastic |
| D-Phenylalanine, N-[[trans-4-(1-methylethyl)cyclohexyl]carbonyl]- |
| N-[(trans-4-Isopropylcyclohexyl)carbonyl]-D-phenylalanine |
| (-)-N-(trans-4-Isopropylcyclohexyl-1-carbonyl)-D-phenylalanine |
| Nateglinide |
