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- 上海莼试
- CS-01Y64732
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- 2026年02月02日
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- 详细信息
- 文献和实验
- 技术资料
- 库存：
20
- 英文名：
K-604 dihydrochloride
- CAS号：
217094-32-1
- 供应商：
上海莼试
- 保存条件：
Store at -20°C
- 规格：
10mM*1mLinDMSO 5mg 10mg 25mg
使用方法：
1.本蛋白酶抑制剂混合物为100×的储存液，使用时按照1:100的比例加入到裂解液中(例如，1ml裂解液中加入10μl蛋白酶抑制剂混合物)，混匀后即可使用。根据需要，0.5M的EDTA也按照1:100的比例加入到裂解液中（如用于检测金属蛋白酶活性，则不宜添加EDTA）。含有蛋白酶抑制剂混合物的裂解液宜现用现配，不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后，就可以开始进行哺乳动物组织的裂解和蛋白提取。
商品属性：
产品描述：
分子式:C23H32Cl2N6OS3
分子量:575.64
溶解度:DMSO: 62.5 mg/mL (108.57 mM)
储存条件:Store at -20°C
General tips:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
K-604 dihydrochloride is a potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT-1) inhibitor with an IC50 of 0.45±0.06 μM.The potency and selectivity of K-604 for human ACAT-1 and ACAT-2 is examined. The IC50 value of K-604 for human ACAT-1 is 0.45 μM and that for human ACAT-2 is 102.85 μM, indicating that K-604 is 229-fold more selective for ACAT-1 than ACAT-2. Kinetic analysis indicates that the inhibition is competitive with respect to oleoyl-coenzyme A with a Ki value of 0.378 μM. K-604 efficiently inhibits cholesterol esterification in human macrophages with IC50 value of 68 nM[1]. In cell free biochemical assays, K604 at 0.5 μM inhibits ACAT1 enzymatic activity by 70% without significantly inhibiting the ACAT2 enzyme activity. To investigate whether blocking ACAT1 increases autophagy in neuronal cells, N2a cells are treated with K604. The result shows that at 0.1 to 1 μM, K604 inhibits ACAT activity by 60-80%. Next K604 is added to N2a cells at concentrations from 0.1 to 1 μM for 24 h, and LC3 levels are examined by western blot. The result shows that K604 increases the LC3-II/LC3-I ratio, a reliable marker for autophagosome formation, in a dose-dependent manner. The number of the fluorescent LC3 puncta is significantly increased in N2a cells after K604 treatment. By western blot, K604 significantly decreases the levels of p62 in N2a cells[2].Using F1B hamsters, an animal model susceptible to diet-induced hyperlipidemia and atherosclerosis, the effects of K-604 on aortic lesion areas and plasma cholesterol levels are assessed. Administration of K-604 does not affect body weight or food consumption. The plasma cholesterol levels in fat-fed hamsters are ~12-fold higher than those in chow-fed hamsters, which are significantly decreased by K-604 only at the highest dose tested (30 mg/kg) but not at lower doses (1-10 mg/kg).The fatty streak lesions stain with oil red O are markedly induced by the high-fat diet, which is significantly reduced by administration of K-604. Further, the histological analyses of the atherosclerotic lesions are performed. The fatty streak lesions in the control group are characterized by accumulation of foamy macrophages in the subendothelial space. In contrast, the areas occupied by foamy macrophages are markedly reduced by administration of K-604[1].[1]. Ikenoya M, et al. A selective ACAT-1 inhibitor, K-604, suppresses fatty streak lesions in fat-fed hamsters without affecting plasma cholesterol levels. Atherosclerosis. 2007 Apr;191(2):290-7. [2]. Shibuya Y, et al. Acyl-coenzyme A:cholesterol acyltransferase 1 blockage enhances autophagy in the neurons of triple transgenic Alzheimer's disease mouse and reduces human P301L-tau content at the presymptomatic stage. Neurobiol Aging. 2015 Jul;36(7):2248-2259.
注意事项：
抗逆滴加序列
每次向板内滴加抗原时，移液器滴头要与平面45度悬空，不要触碰到孔内的液体，由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下，必须反应30min以上，若环境温度低于室温，可将微量反应板置于恒温培养箱中，使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定，往往在高压后pH值会有所改变，所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时，红细胞会产生自凝现象;当pH>7.8时，图形洗脱加快，易造成肉眼观察产生误差;p H=7.2时，红细胞沉降最充分，图形最清晰。
当滴注 1%红细胞悬液时，应经常摇晃红细胞悬液，使红细胞均匀地分布在磷酸缓冲液中，以防止红细胞下降。
反应时间及温度
加入鸡红血球之后，反应板在室温(20~25℃)静置30~40min，对照孔血球下沉于孔底，即可判定结果。若室温达不到实验要求，需相应调整反应时间。当环境温度低于4℃时，红细胞发生自凝;高于37℃时，会发生反应物分离和红细胞溶血。
公司正在出售的产品：
1.本蛋白酶抑制剂混合物为100×的储存液，使用时按照1:100的比例加入到裂解液中(例如，1ml裂解液中加入10μl蛋白酶抑制剂混合物)，混匀后即可使用。根据需要，0.5M的EDTA也按照1:100的比例加入到裂解液中（如用于检测金属蛋白酶活性，则不宜添加EDTA）。含有蛋白酶抑制剂混合物的裂解液宜现用现配，不宜配制后冻存待后续使用。
2. 待所需的抑制剂添加完毕混匀后，就可以开始进行哺乳动物组织的裂解和蛋白提取。
商品属性：
| 货号 | CS-01Y64732 | 规格 | 10mM*1mLinDMSO 5mg 10mg 25mg |
| CAS号 | 217094-32-1 | 分子量 | 575.64 |
| 含量 | >98.00% | 别名 | N/A |
| 分子式 | C23H32Cl2N6OS3 | 化学名 | N/A |
| 产地 | 国产 | 用途 | 仅供科研研究实验 |
分子式:C23H32Cl2N6OS3
分子量:575.64
溶解度:DMSO: 62.5 mg/mL (108.57 mM)
储存条件:Store at -20°C
General tips:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
K-604 dihydrochloride is a potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT-1) inhibitor with an IC50 of 0.45±0.06 μM.The potency and selectivity of K-604 for human ACAT-1 and ACAT-2 is examined. The IC50 value of K-604 for human ACAT-1 is 0.45 μM and that for human ACAT-2 is 102.85 μM, indicating that K-604 is 229-fold more selective for ACAT-1 than ACAT-2. Kinetic analysis indicates that the inhibition is competitive with respect to oleoyl-coenzyme A with a Ki value of 0.378 μM. K-604 efficiently inhibits cholesterol esterification in human macrophages with IC50 value of 68 nM[1]. In cell free biochemical assays, K604 at 0.5 μM inhibits ACAT1 enzymatic activity by 70% without significantly inhibiting the ACAT2 enzyme activity. To investigate whether blocking ACAT1 increases autophagy in neuronal cells, N2a cells are treated with K604. The result shows that at 0.1 to 1 μM, K604 inhibits ACAT activity by 60-80%. Next K604 is added to N2a cells at concentrations from 0.1 to 1 μM for 24 h, and LC3 levels are examined by western blot. The result shows that K604 increases the LC3-II/LC3-I ratio, a reliable marker for autophagosome formation, in a dose-dependent manner. The number of the fluorescent LC3 puncta is significantly increased in N2a cells after K604 treatment. By western blot, K604 significantly decreases the levels of p62 in N2a cells[2].Using F1B hamsters, an animal model susceptible to diet-induced hyperlipidemia and atherosclerosis, the effects of K-604 on aortic lesion areas and plasma cholesterol levels are assessed. Administration of K-604 does not affect body weight or food consumption. The plasma cholesterol levels in fat-fed hamsters are ~12-fold higher than those in chow-fed hamsters, which are significantly decreased by K-604 only at the highest dose tested (30 mg/kg) but not at lower doses (1-10 mg/kg).The fatty streak lesions stain with oil red O are markedly induced by the high-fat diet, which is significantly reduced by administration of K-604. Further, the histological analyses of the atherosclerotic lesions are performed. The fatty streak lesions in the control group are characterized by accumulation of foamy macrophages in the subendothelial space. In contrast, the areas occupied by foamy macrophages are markedly reduced by administration of K-604[1].[1]. Ikenoya M, et al. A selective ACAT-1 inhibitor, K-604, suppresses fatty streak lesions in fat-fed hamsters without affecting plasma cholesterol levels. Atherosclerosis. 2007 Apr;191(2):290-7. [2]. Shibuya Y, et al. Acyl-coenzyme A:cholesterol acyltransferase 1 blockage enhances autophagy in the neurons of triple transgenic Alzheimer's disease mouse and reduces human P301L-tau content at the presymptomatic stage. Neurobiol Aging. 2015 Jul;36(7):2248-2259.
注意事项：
抗逆滴加序列
每次向板内滴加抗原时，移液器滴头要与平面45度悬空，不要触碰到孔内的液体，由后向前依次滴加(即浓度由低往高滴加)。
抗感染反应期
抗原抗体在室温20~25℃下，必须反应30min以上，若环境温度低于室温，可将微量反应板置于恒温培养箱中，使二者充分反应。
旅游温度
磷酸盐缓冲液的pH值要在高压灭菌后进行滴定，往往在高压后pH值会有所改变，所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时，红细胞会产生自凝现象;当pH>7.8时，图形洗脱加快，易造成肉眼观察产生误差;p H=7.2时，红细胞沉降最充分，图形最清晰。
当滴注 1%红细胞悬液时，应经常摇晃红细胞悬液，使红细胞均匀地分布在磷酸缓冲液中，以防止红细胞下降。
反应时间及温度
加入鸡红血球之后，反应板在室温(20~25℃)静置30~40min，对照孔血球下沉于孔底，即可判定结果。若室温达不到实验要求，需相应调整反应时间。当环境温度低于4℃时，红细胞发生自凝;高于37℃时，会发生反应物分离和红细胞溶血。
公司正在出售的产品：
| N-Phthaloyl-Phe-OH | A2ti-1 |
| Dimethomorph | 视神经萎缩蛋白3检测试剂盒 OPA3 ELISA Kit |
| Anguizole | 视黄醇脱氢酶8检测试剂盒 RDH8 ELISA Kit |
| BMY-43748 | 视黄醇脱氢酶15检测试剂盒 RDH15 ELISA Kit |
| Thioridazine-d3 (hydrochloride) | 视黄醇脱氢酶5检测试剂盒 RDH5 ELISA Kit |
| Tenofovir hydrate | 视黄醇脱氢酶14检测试剂盒 RDH14 ELISA Kit |
| 2,3-Dimethoxybenzaldehyde (o-Veratraldehyde) | 视黄醇脱氢酶13检测试剂盒 RDH13 ELISA Kit |
| Bavachalcone (Broussochalcone B) | 视黄醇脱氢酶12检测试剂盒 RDH12 ELISA Kit |
| Tripterifordin | 视网膜钙黏附蛋白检测试剂盒 RCAD ELISA Kit |
| 13,21-Dihydroeurycomanone | 视网膜母细胞瘤蛋白1检测试剂盒 RB1 ELISA Kit |
| Plerixafor (AMD3100) | 视网膜劈裂蛋白检测试剂盒 RS ELISA Kit |
| Siamycin I | 视锥蛋白样蛋白1检测试剂盒 VSNL1 ELISA Kit |
| Garenoxacin (BMS284756) | K-604 dihydrochloride嗜乳脂蛋白亚家族1成员A1检测试剂盒 BTN1A1 ELISA Kit |
| Butylparaben (Butyl parahydroxybenzoate) | 嗜中性粒细胞胞浆因子4检测试剂盒 NCF4 ELISA Kit |
| 人冷诱导RNA结合蛋白ELISA试剂盒 | 受活性修饰蛋白2检测试剂盒 RAMP2 ELISA Kit |
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K-604 dihydrochloride
￥600 - 3200
