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- 详细信息
- 技术资料
- 库存:
49
- 英文名:
A 943931 dihydrochloride
- CAS号:
1227675-50-4
- 供应商:
上海莼试
- 保存条件:
Store at -20°C
- 规格:
10mg 50mg
商品属性:
产品描述:
分子式:C17H21N5.2HCl
分子量:368.31
溶解度:<36.83mg/ml in H2O; <36.83mg/ml in DMSO
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
A 943931, is an H4R (one of histamine receptor subtypes) antagonist [1] with high affinities to H4Rs of human (Ki = 5 nM), rat (Ki = 4 nM) and mouse (Kb = 6 nM) [2].H4R is one of 4 known G-protein-coupled receptors (H1, H2, H3 and H4 receptors) of histamine for histamine to mediate its physiological functions [3].HMC-1 cells incubated with A 943931 at a concentration of 300 nM for 20 min inhibited the increase in ALDH2 activity induced by H4R [4]. In microglia, A 943931 at a concentration of 10 μM partially abolish the release of TNF-α and IL-6 induced by histamine at a concentration of 0.1 μg/ml [5]. In bone marrow-derived mast cells, A 943931 inhibited the shape change induced by histamine (IC50 = 0.38 μM) [6].Intraperitoneal administration of A 943931 at a dose of 33 μmol/kg potently inhibited itch induced by H4R agonist in mice [6]. In several preclinical models, H4R had been shown to be linked to inflammation [7]. A 943931 had excellent antagonistic activity both in vivo and in vitro across multiple species, displayed good oral bioavailability (90%) and excellent metabolic stability. This compound displays good efficacy in rat pain models and is a good anti-inflammatory agent in mice [8]. A 943931 has an in vivo oral bioavailability of 34% and a half-life of 2.6 h in rats [2]. A 943931 efficaciously reduced acute inflammatory pains induced by formalin in the flinch model and by carrageenan in mechanical and thermal hyperalgesia models in rats [9].
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。
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。
公司正在出售的产品:
| 货号 | CS-01Y75689 | 规格 | 10mg 50mg |
| CAS号 | 1227675-50-4 | 分子量 | 368.31 |
| 含量 | >98.00% | 别名 | |
| 分子式 | C17H21N5.2HCl | 化学名 | (R)-1-(2-imino-2,5,6,7-tetrahydro-1H-benzo[6,7]cyclohepta[1,2-d]pyrimidin-4-yl)pyrrolidin-3-amine dihydrochloride |
| 产地 | 国产 | 用途 | 仅供科研研究实验 |
分子式:C17H21N5.2HCl
分子量:368.31
溶解度:<36.83mg/ml in H2O; <36.83mg/ml in DMSO
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
A 943931, is an H4R (one of histamine receptor subtypes) antagonist [1] with high affinities to H4Rs of human (Ki = 5 nM), rat (Ki = 4 nM) and mouse (Kb = 6 nM) [2].H4R is one of 4 known G-protein-coupled receptors (H1, H2, H3 and H4 receptors) of histamine for histamine to mediate its physiological functions [3].HMC-1 cells incubated with A 943931 at a concentration of 300 nM for 20 min inhibited the increase in ALDH2 activity induced by H4R [4]. In microglia, A 943931 at a concentration of 10 μM partially abolish the release of TNF-α and IL-6 induced by histamine at a concentration of 0.1 μg/ml [5]. In bone marrow-derived mast cells, A 943931 inhibited the shape change induced by histamine (IC50 = 0.38 μM) [6].Intraperitoneal administration of A 943931 at a dose of 33 μmol/kg potently inhibited itch induced by H4R agonist in mice [6]. In several preclinical models, H4R had been shown to be linked to inflammation [7]. A 943931 had excellent antagonistic activity both in vivo and in vitro across multiple species, displayed good oral bioavailability (90%) and excellent metabolic stability. This compound displays good efficacy in rat pain models and is a good anti-inflammatory agent in mice [8]. A 943931 has an in vivo oral bioavailability of 34% and a half-life of 2.6 h in rats [2]. A 943931 efficaciously reduced acute inflammatory pains induced by formalin in the flinch model and by carrageenan in mechanical and thermal hyperalgesia models in rats [9].
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。
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。
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A 943931 dihydrochloride
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