Rifampicin
Rifampicin is an ansamycin antibiotic that exhibits antibacterial, neuroprotective, and anti-inflammatory activities. Rifampicin inhibits bacterial DNA-dependent RNA polymerase, preventing formation of the initiation complex in transcription and suppressing RNA synthesis; it is active against Mycobacterium and is clinically used to treat tuberculosis. In microglia, rifampicin decreases expression of the 26S protease regulatory subunit (MSS1), suppressing inflammatory cytokine release. Additionally, rifampicin upregulates expression of LRP1 and P-gp at the blood brain barrier, increasing clearance of amyloid-β (Aβ) and displaying potential efficacy in the treatment of Alzheimer’s disease.
References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18959039
Cas No. |
13292-46-1 |
---|---|
Purity |
≥98% |
Formula |
C43H58N4O12 |
Formula Wt. |
822.94 |
Chemical Name |
3-[[(4-Methyl-1-piperazinyl)imino]methyl]rifamycin |
Synonym |
Rifampin; Abrifam; Eremfat; Rifa; Rifaldin; Rifoldin |
Melting Point |
183-188°C (dec) |
Solubility |
Soluble in DMSO ethyl acetate, methanol and THF. Slightly soluble in water, acetone, and carbon terachloride, chloroform. Water pH 4.3 to 1.3 mg/mL; Water pH 7.3 to 2.5 mg/mL. |
Appearance |
Red Powder |
Sharma SK, Sharma A, Kadhiravan T, et al. Rifamycins (rifampicin, rifabutin and rifapentine) compared to isoniazid for preventing tuberculosis in HIV-negative people at risk of active TB. Cochrane Database Syst Rev. 2013 Jul 5;7:CD007545. PMID: 23828580.
Bi W, Jing X, Zhu L, et al. Inhibition of 26S protease regulatory subunit 7 (MSS1) suppresses neuroinflammation. PLoS One. 2012;7(5):e36142. PMID: 22629310.
Qosa H, Abuznait AH, Hill RA, et al. Enhanced brain amyloid-β clearance by rifampicin and caffeine as a possible protective mechanism against Alzheimers disease. J Alzheimers Dis. 2012;31(1):151-65. PMID: 22504320.
Campbell EA, Korzheva N, Mustaev A, et al. Structural mechanism for rifampicin inhibition of bacterial rna polymerase. Cell. 2001 Mar 23;104(6):901-12. PMID: 11290327.