产品名称

英文名称：A922500

同义词

959122-11-3、A 922500、A-922500、A922500、DGAT-1 Inhibitor 4a、Cyclopentanecarboxylic acid, 2-((4'-(((phenylamino)carbonyl)amino)(1,1'-biphenyl)-4-yl)carbonyl)-, (1R,2R)-、44698M475X、(1R,2R)-2-(4'-(3-phenylureido)-[1,1'-biphenyl]-4-carbonyl)cyclopentane-1-carbo、DGAT-1 Inhibitor 4a、(1R,2R)-2-[[4-[[(苯基氨基)羰基]氨基][1,1-联苯]-4-基]甲酰基]环戊烷羧酸

产品性质

CAS编号：959122-11-3

分子式：C26H24N2O4

分子量：428.48

PubChem编号：24768261

别名：DGAT-1 Inhibitor 4a|(1R,2R)-2-[[4-[[(苯基氨基)羰基]氨基][1,1-联苯]-4-基]甲酰基]环戊烷羧酸

英文别名：959122-11-3|A 922500|A-922500|A922500|DGAT-1 Inhibitor 4a|Cyclopentanecarboxylic acid, 2-((4'-(((phenylamino)carbonyl)amino)(1,1'-biphenyl)-4-yl)carbonyl)-, (1R,2R)-|44698M475X|(1R,2R)-2-(4'-(3-phenylureido)-[1,1'-biphenyl]-4-carbonyl)cyclopentane-1-carbo

规格或纯度：98%

英文名称：A922500

生化机理：二酰基甘油酰基转移酶1（DGAT-1）抑制剂（在人和小鼠DGAT-1处的IC50值分别为7和24 nM），对DGAT-2，ACAT1或ACAT2没有活性。在不改变食物摄入量的情况下引起明显的体重减轻，并降低体内肝脏和血浆甘油三酸酯的水平。口服有效。

储存温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：产品介绍DGAT-1 inhibitor A922500 (A-922500) reduces serum triglyceride levels from baseline at all doses tested; however, this is only statistically significant at the 3mg/kg dose, which lowers serum triglycerides by 53%. Similarly, the 3mg/kg dose of A922500 significantly reduces serum FFA concentrations by 55% and total cholesterol by 25%. DGAT-1 inhibition has no significant effect on body weight at any dose tested. Although A922500 dpes not significantly affect LDL-cholesterol or HDL-cholesterol individually, the serum LDL/HDL-cholesterol ratio is significantly improved by A922500 at 0.3 and 3mg/kg. Similar to the dyslipidemic hamster, treatment with 3mg/kg A922500 significantly reduces serum triglyceride concentrations (39%). FFA levels significantly increase over the 14-day period in vehicle-treated animals. This increase is inhibited in adose-dependent manner by A922500 such that FFA concentrations are 32% lower after 14 days of treatment with the DGAT-1 inhibitor at 3mg/kg, compared with the vehicle group (p < 0.05). HDL-cholesterol is significantly increased from baseline levels by A922500 at 0.3 and 3mg/kg; however, this is only significantly increased compared with vehicle at the 3mg/kg dose. Body weight significantly increases over the 2-week period in vehicle-treated rats, and this is not affected by A922500. LDL-cholesterol is significantly reduced in the vehicle treated group. DGAT-1 inhibition does not further reduce LDL-cholesterol and has no effect on total cholesterol.产品用途A922500 has been used in the inhibition of diacylglycerol acyltransferase (DGAT) in epithelial human breast cancer cell line (MDA-MB-231), digitonin-permeabilized human cancer cells, human myotubes and macrophages.Product DescriptionDGAT-1 inhibitor A922500 (A-922500) reduces serum triglyceride levels from baseline at all doses tested; however, this is only statistically significant at the 3mg/kg dose, which lowers serum triglycerides by 53%. Similarly, the 3mg/kg dose of A922500 significantly reduces serum FFA concentrations by 55% and total cholesterol by 25%. DGAT-1 inhibition has no significant effect on body weight at any dose tested. Although A922500 dpes not significantly affect LDL-cholesterol or HDL-cholesterol individually, the serum LDL/HDL-cholesterol ratio is significantly improved by A922500 at 0.3 and 3mg/kg. Similar to the dyslipidemic hamster, treatment with 3mg/kg A922500 significantly reduces serum triglyceride concentrations (39%). FFA levels significantly increase over the 14-day period in vehicle-treated animals. This increase is inhibited in adose-dependent manner by A922500 such that FFA concentrations are 32% lower after 14 days of treatment with the DGAT-1 inhibitor at 3mg/kg, compared with the vehicle group (p < 0.05). HDL-cholesterol is significantly increased from baseline levels by A922500 at 0.3 and 3mg/kg; however, this is only significantly increased compared with vehicle at the 3mg/kg dose. Body weight significantly increases over the 2-week period in vehicle-treated rats, and this is not affected by A922500. LDL-cholesterol is significantly reduced in the vehicle treated group. DGAT-1 inhibition does not further reduce LDL-cholesterol and has no effect on total cholesterol.Product ApplicationA922500 has been used in the inhibition of diacylglycerol acyltransferase (DGAT) in epithelial human breast cancer cell line (MDA-MB-231), digitonin-permeabilized human cancer cells, human myotubes and macrophages.

IUPAC Name：(1R,2R)-2-[4-[4-(phenylcarbamoylamino)phenyl]benzoyl]cyclopentane-1-carboxylic acid

INCHI：InChI=1S/C26H24N2O4/c29-24(22-7-4-8-23(22)25(30)31)19-11-9-17(10-12-19)18-13-15-21(16-14-18)28-26(32)27-20-5-2-1-3-6-20/h1-3,5-6,9-16,22-23H,4,7-8H2,(H,30,31)(H2,27,28,32)/t22-,23-/m1/s1

InChi Key：BOZRFEQDOFSZBV-DHIUTWEWSA-N

Canonical SMILES：C1CC(C(C1)C(=O)O)C(=O)C2=CC=C(C=C2)C3=CC=C(C=C3)NC(=O)NC4=CC=CC=C4

Isomeric SMILES：C1C[C@H]([C@@H](C1)C(=O)O)C(=O)C2=CC=C(C=C2)C3=CC=C(C=C3)NC(=O)NC4=CC=CC=C4

PubChem CID：24768261

溶解性：溶于DMSO, 最高浓度 (mg/mL) 21.42, 最高浓度(mM) 50

象形图：

信号词：Danger

危险声明：H319 Causes serious eye irritationH301 Toxic if swallowedH400 Very toxic to aquatic lifeH410 Very toxic to aquatic life with long lasting effects

预防措施声明：P305+P351+P338,P273,P280,P321,P405,P501,P264,P270,P391,P330,P264+P265,P301+P316,P337+P317

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