Vamorolone (Synonyms: VBP15)
目录号: PL07297 纯度: ≥99%
CAS No. :13209-41-1
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中文名称
Vamorolone
中文别名
17,21-二羟基-16alpha-甲基孕甾-1,4,9(11)-三烯-3,20-二酮;地塞米松EP杂质E
英文名称
Vamorolone
英文别名
Pregna-1,4,9(11)-triene-3,20-dione,17,21-dihydroxy-16-methyl-, (16a)-;16α-Methyl-9,11-dehydro Prednisolone;17,21-dihydroxy-16alpha-methylpregna-1,4,9(11)-triene-3,20-dione;16α-Methyl-9,11-dehy;(8S,10S,13S,14S,16R,17R)-17-hydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-7,8,12,14,15,16-hexahydro-6H-cyclopenta[a]phenanthren-3-one;Dexamethasone impurity E;(16α)-17,21-Dihydroxy-16-Methylpregna-1,4,9(11)-triene-3,20-dione;17.alpha.,21-Dihydroxy-16.alpha.-methylpregna-1,4,9(11)-triene-3,20-dione;Vamorolone
Cas No.
13209-41-1
分子式
C22H28O4
分子量
356.46
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Vamorolone (VBP15) 是首创的,具有口服活性的解离性类固醇 (dissociative steroidal) 抗炎药和膜稳定剂。Vamorolone 改善肌营养不良,无副作用。Vamorolone 抑制 (NF-κB) 抑制作用,并降低了激素的影响。
生物活性
Vamorolone (VBP15) is a first-in-class, orally active dissociative steroidal anti-inflammatory drug and membrane-stabilizer. Vamorolone improves muscular dystrophy without side effects. Vamorolone shows potent NF-κB inhibition and substantially reduces hormonal effects.
性状
Solid
体外研究(In Vitro)
Vamorolone (VBP15) inhibits TNFα-induced pro-inflammatory NF-κB signaling in C2C12 muscle cells at 1 nM or more. Vamorolone binds the glucocorticoid receptor (GR) and mineralocorticoid receptor (MR) with similar affinity.
Vamorolone (0.1, 1μM; 30 minutes) reduces production of IL1βand CCL5 inflammatory mediators in primary human macrophages.
Vamorolone is a first-in-class mineralocorticoid receptor (MR) antagonist/dissociative glucocorticoid receptor (GR) ligand. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Vamorolone (5-30 mg/kg; cherry syrup) shows a superior side effect profile compared to pharmacological glucocorticoids in mdx mice.
Vamorolone (30 mg/kg; orally; daily for 20 days) reduces CNS Inflammation in murine experimental autoimmune encephalomyelitis. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Heier CR, et al. VBP15, a novel anti-inflammatory and membrane-stabilizer, improves muscular dystrophy without side effects. EMBO Mol Med. 2013 Oct;5(10):1569-85.
[2]. Dillingham BC, et al. VBP15, a novel anti-inflammatory, is effective at reducing the severity of murine experimental autoimmune encephalomyelitis. Cell Mol Neurobiol. 2015 Apr;35(3):377-387.
溶解度数据
In Vitro: DMSO : 62.5 mg/mL (175.34 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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