基本描述

别名	(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	DGAT-1 Inhibitor 4a \| (1R,2R)-2-(4'-(3-Phenylureido)-[1,1'-biphenyl]-4-carbonyl)cyclopentanecarboxylic acid \| SCHEMBL2742723 \| SMR004702890 \| A922500 \| A-922500 \| EX-A3976 \| (1R,2R)-2-({4'-[(anilinocarbonyl)amino]-1,1'-biphenyl-4-yl}carbonyl)cyclopentanec
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
作用类型	抑制剂
产品介绍	DGAT-1 inhibitor A 922500 (A-922500) reduces serum triglyceride levels from baseline at all doses tested; however, this is only statistically significant at the 3 mg/kg dose, which lowers serum triglycerides by 53%. Similarly, the 3 mg/kg dose of A 922500 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 A 922500 dpes not significantly affect LDL-cholesterol or HDL-cholesterol individually, the serum LDL/HDL-cholesterol ratio is significantly improved by A 922500 at 0.3 and 3 mg/kg. Similar to the dyslipidemic hamster, treatment with 3 mg/kg A 922500 significantly reduces serum triglyceride concentrations (39%). FFA levels significantly increase over the 14-day period in vehicle-treated animals. This increase is inhibited in a dose-dependent manner by A 922500 such that FFA concentrations are 32% lower after 14 days of treatment with the DGAT-1 inhibitor at 3 mg/kg, compared with the vehicle group (p < 0.05). HDL-cholesterol is significantly increased from baseline levels by A 922500 at 0.3 and 3 mg/kg; however, this is only significantly increased compared with vehicle at the 3 mg/kg dose. Body weight significantly increases over the 2-week period in vehicle-treated rats, and this is not affected by A 922500. 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 Description DGAT-1 inhibitor A 922500 (A-922500) reduces serum triglyceride levels from baseline at all doses tested; however, this is only statistically significant at the 3 mg/kg dose, which lowers serum triglycerides by 53%. Similarly, the 3 mg/kg dose of A 922500 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 A 922500 dpes not significantly affect LDL-cholesterol or HDL-cholesterol individually, the serum LDL/HDL-cholesterol ratio is significantly improved by A 922500 at 0.3 and 3 mg/kg. Similar to the dyslipidemic hamster, treatment with 3 mg/kg A 922500 significantly reduces serum triglyceride concentrations (39%). FFA levels significantly increase over the 14-day period in vehicle-treated animals. This increase is inhibited in a dose-dependent manner by A 922500 such that FFA concentrations are 32% lower after 14 days of treatment with the DGAT-1 inhibitor at 3 mg/kg, compared with the vehicle group (p < 0.05). HDL-cholesterol is significantly increased from baseline levels by A 922500 at 0.3 and 3 mg/kg; however, this is only significantly increased compared with vehicle at the 3 mg/kg dose. Body weight significantly increases over the 2-week period in vehicle-treated rats, and this is not affected by A 922500. 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 Application 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.
纯度	≥98%

关联靶点（人）

DGAT1 Tclin 二酰甘油O-酰基转移酶1(Diacylglycerol O-acyltransferase 1) (4 活性数据)

点击查看靶蛋白信息： DGAT1

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

SOAT2 Tchem Acyl coenzyme A:cholesterol acyltransferase 2 (288 活性数据)

点击查看靶蛋白信息： SOAT2

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

Caco-2 (12174 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

HepG2 (196354 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

DGAT2 Tchem Diacylglycerol O-acyltransferase 2 (347 活性数据)

点击查看靶蛋白信息： DGAT2

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

DGAT1 Tclin Diacylglycerol O-acyltransferase 1 (1719 活性数据)

点击查看靶蛋白信息： DGAT1

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

关联靶点（其它种属）

Soat1 Acyl coenzyme A:cholesterol acyltransferase 1 (295 活性数据)

点击查看靶蛋白信息： Soat1

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

Hdac6 Histone deacetylase 6 (222 活性数据)

点击查看靶蛋白信息： Hdac6

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

Canis familiaris (36305 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

Mus musculus (284745 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

Rattus norvegicus (775804 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

Rotavirus (147 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

rep Replicase polyprotein 1ab (378 活性数据)

点击查看靶蛋白信息： rep

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

SARS-CoV-2 (38078 活性数据)

点击查看此靶标相关信息

活性类型	Relation	Activity value	Units	Action Type	期刊	PubMed Id	doi	Assay Aladdin ID

作用机制

作用机制	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	参考文献

名称和识别符

PubChem SID	504769811
分子类型	小分子
IIUPAC Name	(1R,2R)-2-[4-[4-(phenylcarbamoylamino)phenyl]benzoyl]cyclopentane-1-carboxylic acid
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
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
分子量	428.48
Reaxy-Rn	29788907
Reaxys-RN link address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=29788907&ln=

化学和物理性质

溶解性	溶于DMSO, 最高浓度 (mg/mL): 21.42, 最高浓度(mM): 50
分子量	428.500 g/mol
XLogP3	4.300
氢键供体数Hydrogen Bond Donor Count	3
氢键受体数Hydrogen Bond Acceptor Count	4
可旋转键计数Rotatable Bond Count	6
精确质量Exact Mass	428.174 Da
单同位素质量Monoisotopic Mass	428.174 Da
拓扑极表面积Topological Polar Surface Area	95.500 Å²
重原子数Heavy Atom Count	32
形式电荷Formal Charge	0
复杂度Complexity	659.000
同位素原子数Isotope Atom Count	0
定义的原子立体中心计数Defined Atom Stereocenter Count	2
未定义的原子立体中心计数Undefined Atom Stereocenter Count	0
定义的键立体中心计数Defined Bond Stereocenter Count	0
未定义的键立体中心计数Undefined Bond Stereocenter Count	0
所有立体化学键的总数The total count of all stereochemical bonds	0
共价键合单元计数Covalently-Bonded Unit Count	1

安全和危险性（GHS）

象形图	GHS06, GHS07, GHS09
信号词	危险
危险声明	H301: 吞咽会中毒 H319: 引起严重眼睛刺激 H400: 对水生生物有剧毒 H410: 对水生生物有剧毒并具有长期持续影响
预防措施声明	P264: 处理后要彻底洗手。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P273: 避免释放到环境中。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P321: 特殊处理（请参阅此标签上的...）。 P330: 漱口 P391: 收集溢出物 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。 P301+P316: 如果吞咽：立即寻求紧急医疗救助。 P337+P317: 如果眼睛刺激持续：寻求医疗帮助。

质检证书（CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):

输入批号以搜索分析图谱:

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找到6个结果

批号(Lot Number)	证书类型	货号
L2403109	分析证书	A129800
I2123073	分析证书	A129800
I2123075	分析证书	A129800
I2123070	分析证书	A129800
I2123071	分析证书	A129800
I2123072	分析证书	A129800

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货号 (SKU)	包装规格	是否现货
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A922500,DGAT-1抑制剂

库存信息

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库存信息

基本描述

关联靶点（人）

关联靶点（其它种属）

作用机制

名称和识别符

化学和物理性质

安全和危险性（GHS）

质检证书（CoA,COO,BSE/TSE 和分析图谱)

溶液计算器

摩尔浓度计算器

稀释计算器

复溶计算器