| Bioactivity | 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[1][2]. | ||||||||||||
| Invitro | 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[1].Vamorolone (0.1, 1μM; 30 minutes) reduces production of IL1βand CCL5 inflammatory mediators in primary human macrophages[2].Vamorolone is a first-in-class mineralocorticoid receptor (MR) antagonist/dissociative glucocorticoid receptor (GR) ligand[3]. | ||||||||||||
| In Vivo | Vamorolone (5-30 mg/kg; cherry syrup) shows a superior side effect profile compared to pharmacological glucocorticoids in mdx mice[1].Vamorolone (30 mg/kg; orally; daily for 20 days) reduces CNS Inflammation in murine experimental autoimmune encephalomyelitis[2]. Animal Model: | ||||||||||||
| Name | Vamorolone | ||||||||||||
| CAS | 13209-41-1 | ||||||||||||
| Formula | C22H28O4 | ||||||||||||
| Molar Mass | 356.46 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. [3]. Heier CR, et al. Vamorolone targets dual nuclear receptors to treat inflammation and dystrophic cardiomyopathy. Life Sci Alliance. 2019 Feb 11;2(1). pii: e201800186. |