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Losmapimod
CAS No. 585543-15-3
Losmapimod ( GSK-AHAB | GW856553X | SB856553 | GW 856553X | SB 856553 )
产品货号. M15150 CAS No. 585543-15-3
Losmapimod (GSK-AHAB、GW856553X、SB856553) 是一种选择性、有效、口服活性的 p38 MAPK 抑制剂，p38α 和 p38β 的 pKi 分别为 8.1 和 7.6。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 2MG | ￥231 | 有现货 |
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| 5MG | ￥366 | 有现货 |
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| 10MG | ￥588 | 有现货 |
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| 25MG | ￥1181 | 有现货 |
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| 50MG | ￥1972 | 有现货 |
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| 100MG | ￥2673 | 有现货 |
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| 500MG | ￥6174 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
| 1 mL x 10 mM in DMSO | ￥428 | 有现货 |
|
生物学信息
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产品名称Losmapimod
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述Losmapimod (GSK-AHAB、GW856553X、SB856553) 是一种选择性、有效、口服活性的 p38 MAPK 抑制剂，p38α 和 p38β 的 pKi 分别为 8.1 和 7.6。
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产品描述Losmapimod (GSK-AHAB, GW856553X, SB856553)?is a selective, potent, orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively; displays no significant activity for p38γ, p38δ (<25% inhibition at 10 uM), and COX-2; significantly and dose-dependently improves survival, endothelial-dependent and -independent vascular relaxation in rat model of cardiovascular disease.Ischemia Phase 3 Clinical(In Vitro):In the spontaneously hypertensive stroke-prone rat (SHR-SP), chronic treatment with GSK-AHAB significantly and dose-dependently improves survival, endothelial-dependent and -independent vascular relaxation, and indices of renal function, and it attenuates dyslipidemia, hypertension, cardiac remodeling, plasma renin activity (PRA), aldosterone, and interleukin-1β (IL-1β).
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体外实验——
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体内实验In the spontaneously hypertensive stroke-prone rat (SHR-SP), chronic treatment with GSK-AHAB significantly and dose-dependently improves survival, endothelial-dependent and -independent vascular relaxation, and indices of renal function, and it attenuates dyslipidemia, hypertension, cardiac remodeling, plasma renin activity (PRA), aldosterone, and interleukin-1β (IL-1β).
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同义词GSK-AHAB | GW856553X | SB856553 | GW 856553X | SB 856553
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通路MAPK/ERK Signaling
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靶点p38 MAPK
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受体p38α|p38β
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研究领域Cardiovascular Disease
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适应症Ischemia
化学信息
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CAS Number585543-15-3
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分子量383.4591
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分子式C22H26FN3O2
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纯度>98% (HPLC)
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溶解度DMSO: ≥ 58 mg/mL
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SMILESO=C(C1=CC=C(C2=CC(C(NC3CC3)=O)=CC(F)=C2C)N=C1)NCC(C)(C)C
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化学全称3-Pyridinecarboxamide, 6-[5-[(cyclopropylamino)carbonyl]-3-fluoro-2-methylphenyl]-N-(2,2-dimethylpropyl)-
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Willette RN, et al. J Pharmacol Exp Ther. 2009 Sep;330(3):964-70.
2. Cheriyan J, et al. Circulation. 2011 Feb 8;123(5):515-23.
3. Lomas DA, et al. J Clin Pharmacol. 2012 Mar;52(3):416-24.
