saxagliptin
Modify Date: 2024-01-05 22:37:51
saxagliptin structure
|
Common Name | saxagliptin | ||
|---|---|---|---|---|
| CAS Number | 361442-04-8 | Molecular Weight | 315.410 | |
| Density | 1.35 | Boiling Point | 548.7±35.0 °C at 760 mmHg | |
| Molecular Formula | C18H25N3O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 285.6±25.9 °C | |
Use of saxagliptinSaxagliptin(BMS477118) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM and Ki of 1.3 nM.IC50 value: 26 nM [1]Target: DPP4in vitro: Saxagliptin has an inhibition constant Ki of 1.3 nM for DPP4 inhibition, which is 10-fold more potent than either vildagliptin or sitagliptin (another two DPP4 inhibitors) with Ki of 13 and 18 nM. In addition, Saxagliptin demonstrates greater specificity for DPP4 than for either the DPP8 or DPP9 enzymes (400- and 75- fold, respectively). The active metablite of saxagliptin is two-fold less potent than the parent. Both Saxagliptin and its metabolite are highly selective (>4000-fold) for the prevention of DPP4 compared with a range of other proteases (selectivity of sitagliptin and vildagliptin for DPP4 is >2600 and <250-fold, respectively, compared with DPP8 and DPP9) [2]. Saxagliptin reduces the degradation of the incretin hormone glucagon-like peptide-1, thereby enhancing its actions, and is associated with improved β-cell function and suppression of glucagon secretion.in vivo: Saxagliptin is highly effective at eliciting marked dose-dependent enhancements in glucose clearance in the dose range 0.13-1.3 mg/kg in ob/ob mice relative to controls. Saxagliptin dose-dependently elevate plasma insulin significantly at 15 min post-oGTT, with concomitant improvement in the glucose clearance curves at 60 min post-oGTT [4]. |
| Name | Saxagliptin |
|---|---|
| Synonym | More Synonyms |
| Description | Saxagliptin(BMS477118) is a selective and reversible DPP4 inhibitor with IC50 of 26 nM and Ki of 1.3 nM.IC50 value: 26 nM [1]Target: DPP4in vitro: Saxagliptin has an inhibition constant Ki of 1.3 nM for DPP4 inhibition, which is 10-fold more potent than either vildagliptin or sitagliptin (another two DPP4 inhibitors) with Ki of 13 and 18 nM. In addition, Saxagliptin demonstrates greater specificity for DPP4 than for either the DPP8 or DPP9 enzymes (400- and 75- fold, respectively). The active metablite of saxagliptin is two-fold less potent than the parent. Both Saxagliptin and its metabolite are highly selective (>4000-fold) for the prevention of DPP4 compared with a range of other proteases (selectivity of sitagliptin and vildagliptin for DPP4 is >2600 and <250-fold, respectively, compared with DPP8 and DPP9) [2]. Saxagliptin reduces the degradation of the incretin hormone glucagon-like peptide-1, thereby enhancing its actions, and is associated with improved β-cell function and suppression of glucagon secretion.in vivo: Saxagliptin is highly effective at eliciting marked dose-dependent enhancements in glucose clearance in the dose range 0.13-1.3 mg/kg in ob/ob mice relative to controls. Saxagliptin dose-dependently elevate plasma insulin significantly at 15 min post-oGTT, with concomitant improvement in the glucose clearance curves at 60 min post-oGTT [4]. |
|---|---|
| Related Catalog | |
| References |
| Density | 1.35 |
|---|---|
| Boiling Point | 548.7±35.0 °C at 760 mmHg |
| Molecular Formula | C18H25N3O2 |
| Molecular Weight | 315.410 |
| Flash Point | 285.6±25.9 °C |
| Exact Mass | 315.194672 |
| PSA | 90.35000 |
| LogP | -0.14 |
| Vapour Pressure | 0.0±3.3 mmHg at 25°C |
| Index of Refraction | 1.640 |
| Storage condition | -20℃ |
| Hazard Codes | Xn |
|---|---|
| Risk Phrases | 28-38-41-48 |
| Safety Phrases | 24/25-26-28-36/37/39 |
| RIDADR | 3077 |
| HS Code | 2933990090 |
| HS Code | 2933990090 |
|---|---|
| Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
| Onglyza |
| (1S,3S,5S)-2-{(2S)-2-Amino-2-[(1r,3R,5R,7S)-3-hydroxyadamantan-1-yl]acetyl}-2-azabicyclo[3.1.0]hexane-3-carbonitrile |
| 2-Azabicyclo[3.1.0]hexane-3-carbonitrile, 2-[(2S)-2-amino-2-[(5R,7S)-3-hydroxytricyclo[3.3.1.1]dec-1-yl]acetyl]-, (1S,3S,5S)- |
| saxagliptin |
| (1R,3S,5R)-2-((S)-2-amino-2-((1r,3R,5R,7S)-3-hydroxyadamantan-1-yl)acetyl)-2-azabicyclo[3.1.0]hexane-3-carbonitrile |