| Losmapimodp38 MAPK inhibitor, orally active |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 98.19%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Related Biological Data
| Description | Losmapimod (GW856553X) is a selective, potent, and orally active inhibitor of p38 MAPK with a pKi values of 8.1 and 7.6 for p38α and p38β, respectively. | |||||
| Targets | p38α | p38β | ||||
| IC50 | (pKi=8.1) | (pKi=7.6) | ||||
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| Cas No. | 585543-15-3 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | N/A | ||
| Canonical SMILES | FC1=C(C)C(C(C=C2)=NC=C2C(NCC(C)(C)C)=O)=CC(C(NC3CC3)=O)=C1 | ||
| Formula | C22H26FN3O2 | M.Wt | 383.46 |
| Solubility | ≥19.15mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
Losmapimod (GW856553, GW856553X, GSK-AHAB) is a potent and selective inhibitor of p38 MAPK with pKi values of 8.1 and 7.6 for p38α and p38β, respectively [1].
p38 mitogen-activated protein kinase (p38 MAPK) is an intracellular signaling kinase and plays an important role in regulating transcription and translation of the inflammatory response in macrophages and endothelial cells [2].
Losmapimod is an orally active p38 MAPK inhibitor. In the spontaneously hypertensive stroke-prone rats (SHR-SPs) with a salt-fat diet, GSK-AHAB significantly improved survival and renal function in a dose-dependent way and induced vascular relaxation. Also, GSK-AHAB attenuated hypertension, cardiac remodeling, dyslipidemia, plasma renin activity (PRA), interleukin-1 (IL-1) and aldosterone [1]. In patients with hypercholesterolemia, losmapimod improved acetylcholine, sodium nitroprusside and NG-monomethyl-L-arginine (L-NMMA) responses by 25%, 20% and 10%, respectively. Also, losmapimod reduced C-reactive protein (a systemic inflammatory marker) by 57%. These results suggested that losmapimod improved NO-mediated vasodilatation and inhibited inflammation [2]. In patients with chronic obstructive pulmonary disease (COPD), losmapimod (7.5 mg twice daily) reduced plasma fibrinogen by 11% and was well tolerated [3].
References:[1]. Willette RN, Eybye ME, Olzinski AR, et al. Differential effects of p38 mitogen-activated protein kinase and cyclooxygenase 2 inhibitors in a model of cardiovascular disease. J Pharmacol Exp Ther, 2009, 330(3): 964-970. [2]. Cheriyan J, Webb AJ, Sarov-Blat L, et al. Inhibition of p38 mitogen-activated protein kinase improves nitric oxide-mediated vasodilatation and reduces inflammation in hypercholesterolemia. Circulation., 2011, 123(5): 515-523. [3]. Lomas DA, Lipson DA, Miller BE, et al. An oral inhibitor of p38 MAP kinase reduces plasma fibrinogen in patients with chronic obstructive pulmonary disease. J Clin Pharmacol, 2012, 52(3): 416-424.
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如图，方法是默克给的厂家标准，样品为叔丁醇
现在想把KOH滴定液换成NaOH滴定液，但是领导死活让找依据不然就要做验证
我想知道有没有哪位大神知道这个方法的具体出处。
最好权威一点
