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My CartCAS：1177-87-3
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 1177-87-3 |
| Name | Dexamethasone Acetate |
| Molecular Formula | C24H31FO6 |
| Molecular Weight | 434.5 |
| Solubility | Soluble in DMSO ≥10mg/mL |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 214-646-8 |
| MDL | MFCD00027407 |
| SMILES | C[C@@]1([C@@]2(O)C(COC(C)=O)=O)[C@](C[C@H]2C)([H])[C@@](CCC3=CC4=O)([H])[C@@](F)([C@]3(C=C4)C)[C@@H](O)C1 |
| InChIKey | AKUJBENLRBOFTD-RPRRAYFGSA-N |
| InChI | InChI=1S/C24H31FO6/c1-13-9-18-17-6-5-15-10-16(27)7-8-21(15,3)23(17,25)19(28)11-22(18,4)24(13,30)20(29)12-31-14(2)26/h7-8,10,13,17-19,28,30H,5-6,9,11-12H2,1-4H3/t13-,17+,18+,19+,21+,22+,23+,24+/m1/s1 |
| PubChem CID | 236702 |
| Target Point | Glucocorticoid Receptor (GR, or GCR) |
| Passage | Immunology & Inflammation |
| Background | Dexamethasone Acetate is a glucocorticoid receptor agonist with anti-inflammatory and immunosuppressive activity. |
| Biological Activity | Dexamethasone是糖皮质素类甾体化合物，有抗炎和免疫抑制活性。[1-4] |
| In Vitro | 地塞米松调节几种转录因子，包括激活蛋白-1，核因子-AT和核因子-κB，导致激活和抑制参与炎症反应的关键基因[1]。地塞米松有效抑制A549细胞释放粒细胞 - 巨噬细胞集落刺激因子(GM-CSF)，EC50为2.2 nM。发现地塞米松(EC50 = 36nM)诱导β2受体的转录与糖皮质激素受体(GR)DNA结合相关，并且发生在比GM-CSF释放抑制高10-100倍的浓度。地塞米松(IC50 = 0.5 nM)抑制3×κB(NF-κB，IκBα和I-κBβ)，这与抑制GM-CSF释放有关[2]。 |
| In Vivo | 先前已报道用2×5mg/kg剂量的地塞米松有效抑制脂多糖(LPS)诱导的炎症。在我们的实验系统中，与暴露于LPS并仅注射溶剂(盐水)的动物相比，用单剂量地塞米松10mg/kg(ip)治疗显著降低了粒细胞的募集以及氧自由基的自发产生。当在吸入LPS之前1小时和之后1小时施用时，效果是统计学显著的。 BALF中的粒细胞数量下降到与健康动物相当的水平(给定水雾剂)[3]。用地塞米松处理的大鼠比对照大鼠消耗更少的食物并且重量更轻。虽然他们的食物摄入量相似，但处理过的大鼠也比配对喂养的动物重量轻。 5天的地塞米松注射导致肝脏质量(+ 42％)和肝脏与体重比率(+ 65％)显著增加。治疗5天后，腓肠肌的湿重减少20％，但相对于体重(g/100 g体重)，它仍未受影响，表明肌肉减重与体重减轻平行[4]。 |
| Animal Experiment | 小鼠[3]雌性C57Bl/6JBom小鼠(10-12周龄)用于所有实验。地塞米松以1或10mg/kg的单次注射给药。将地塞米松溶于盐水中，在LPS暴露前1小时或1小时腹膜内注射400μL。在一个实验中，从攻击前1小时开始每4 5小时连续注射N-乙酰半胱氨酸(NAC)(100和500mg/kg)(总共5次注射)。对照组的LPS暴露的动物腹膜内注射溶剂(盐水)。通过将100μLNAAC(50，100或500mg/kg)或地塞米松(10mg/kg)滴注到用15mg/kg Rapinovet(iv)麻醉的小鼠的肺中来进行气管内给药。使用大鼠[4]雄性Sprague-Dawley大鼠。每天一次用地塞米松(1.5mg/kg体重)腹膜内注射地塞米松处理的大鼠5天，并允许随意喂食。特别选择地塞米松剂量(1.5mg/kg /天)和治疗持续时间(5天)，因为该治疗诱导了可重复且显著的分解代谢状态。对照大鼠未接受任何治疗并随意喂食。为了考虑地塞米松处理诱导的食物摄入减少，使用第三组配对喂养的大鼠。给这些大鼠提供与注射地塞米松的大鼠相同量的食物，并用每日等容的腹膜内注射NaCl(0.9％)处理5天。在最后注射地塞米松或NaCl后，将动物禁食过夜，然后通过断头处死。 |
| Data Literature Source | [1]. LaLone CA，et al. Effects of a glucocorticoid receptor agonist，Dexamethasone，on fathead minnow reproduction，growth，and development. Environ Toxicol Chem. 2012 Mar;31(3):611-22. [2]. Adcock IM，et al. Ligand-induced differentiation of glucocorticoid receptor (GR) trans-repression and transactivation: preferential targetting of NF-kappaB and lack of I-kappaB involvement. Br J Pharmacol. 1999 Jun;127(4):1003-11 [3]. Rocksén D，et al. Differential anti-inflammatory and anti-oxidative effects of Dexamethasone and N-acetylcysteine in endotoxin-induced lung inflammation. Clin Exp Immunol. 2000 Nov;122(2):249-56 [4]. Roussel D，et al. Dexamethasone treatment specifically increases the basal proton conductance of rat liver mitochondria. FEBS Lett. 2003 Apr 24;541(1-3):75-9. |
| Unit | Bottle |
| Specification | 100mg 10mM*1mL in DMSO 500mg |
是糖皮质素类甾体化合物，有抗炎和免疫抑制活性。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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