| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| Other Sizes |
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| 体外研究 (In Vitro) |
cetilistat 抑制大鼠胰腺脂肪酶活性，IC50 为 54.8 nM。此外，cetilistat 对人胰腺脂肪酶活性的抑制作用是大鼠胰腺脂肪酶的 9.2 倍，IC50 为 5.95 nM[1]。
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|---|---|
| 体内研究 (In Vivo) |
在雄性 SD 大鼠中，cetilistat（3、10、30 或 100 mg/kg）抑制胰腺脂肪酶活性，减少肠道脂肪吸收[1]。通过减少肠道脂肪吸收，西替司他（4.9、14.9或50.7 mg/kg；混入粉状高脂食品中；每天三次；持续三周）对DIO F344大鼠具有抗肥胖和降高脂作用[1]。
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| 动物实验 |
Animal/Disease Models: Fifty male SD rats (eight weeks of age)[1]
Doses: 3, 10 , 30, or 100 mg/kg Route of Administration: Orally administered; prepared in 0.5 % methylcellulose (MC) suspension Experimental Results: Dose-dependently decreased AUC 0-6 h of plasma triglyceride induced by oral loading of Intrafat 20%. The effect was statistically significant at 3 mg/kg, reaching 45% reduction, while an almost 90 % reduction was achieved at 100 mg/kg. Animal/Disease Models: Male diet-induced obesity (DIO) F344 rats (five weeks of age)[1] Doses: 4.9 , 14.9, or 50.7 mg/kg Route of Administration: Administered as food admixture in a high-fat diet; one time/day; for three weeks Experimental Results: Dramatically and dose-dependently decreased body weight gain compared with control. |
| 参考文献 | |
| 其他信息 |
Cetilistat is a benzoxazine.
Cetilistat is a novel inhibitor of pancreatic lipase being developed by Alizyme for the treatment of obesity and associated co-morbidities, including type 2 diabetes. Drug Indication Investigated for use/treatment in obesity. Mechanism of Action Cetilistat is a gastrointestinal lipase inhibitor that blocks fat digestion and absorption, leading to reduced energy intake, and thus weight loss. It is distinct from most other anti-obesity agents as it does not act on the brain to reduce appetite, but acts peripherally. The compound remains in the gastrointestinal tract with no significant absorption into the body. |
| 分子式 |
C25H39NO3
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|---|---|---|
| 分子量 |
401.58
|
|
| 精确质量 |
401.292
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| CAS号 |
282526-98-1
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| 相关CAS号 |
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| PubChem CID |
9952916
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| 外观&性状 |
White to off-white solid powder
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| 密度 |
1.0±0.1 g/cm3
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| 沸点 |
509.7±43.0 °C at 760 mmHg
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| 熔点 |
74°C
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| 闪点 |
158.9±22.6 °C
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| 蒸汽压 |
0.0±1.3 mmHg at 25°C
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| 折射率 |
1.521
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| LogP |
9.93
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|
| tPSA |
52.33
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| 氢键供体(HBD)数目 |
0
|
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| 氢键受体(HBA)数目 |
4
|
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| 可旋转键数目(RBC) |
16
|
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| 重原子数目 |
29
|
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| 分子复杂度/Complexity |
477
|
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| 定义原子立体中心数目 |
0
|
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| InChi Key |
MVCQKIKWYUURMU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H39NO3/c1-3-4-5-6-7-8-9-10-11-12-13-14-15-16-19-28-25-26-23-18-17-21(2)20-22(23)24(27)29-25/h17-18,20H,3-16,19H2,1-2H3
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| 化学名 |
2-hexadecoxy-6-methyl-3,1-benzoxazin-4-one
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| 别名 |
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| HS Tariff Code |
2934.99.9001
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 溶解度 (体外实验) |
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|---|
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4902 mL | 12.4508 mL | 24.9016 mL | |
| 5 mM | 0.4980 mL | 2.4902 mL | 4.9803 mL | |
| 10 mM | 0.2490 mL | 1.2451 mL | 2.4902 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液)：对于大多数产品，InvivoChem推荐用DMSO配置母液 (比如：5、10、20mM或者10、20、50 mg/mL浓度），个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息，或者很难将产品溶解在溶液中，请联系我们;
3、建议使用下列计算器进行相关计算（摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等）;
4、母液配好之后，将其分装到常规用量，并储存在-20°C或-80°C，尽量减少反复冻融循环。
计算结果:
工作液浓度： mg/mL；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度，请首先与我们联系。
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH2O，混匀澄清。
(1) 请确保溶液澄清之后，再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶；
(2) 一定要按顺序加入溶剂 (助溶剂) 。
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