| Identification | Back Directory | [Name]
WAY-265920 (ILS 920) | [CAS]
892494-07-4 | [Synonyms]
ILS-920
WAY-265920 (ILS 920)
23,27-Epoxy-15,18-ethenopyrido[2,1-r][1,16,2,19]dioxadiazacyclohentriacontine-1,5,11,28,29(6H,12H,31H)-pentone, 3,4,9,10,13,14,15,16,18,21,22,23,24,25,26,27,32,33,34,34a-eicosahydro-9,27-dihydroxy-3-[(1R)-2-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethyl]-10,21-dimethoxy-6,8,12,14,20,26-hex... | [Molecular Formula]
C57H86N2O14 | [MDL Number]
MFCD30187579 | [MOL File]
892494-07-4.mol | [Molecular Weight]
1023.32 |
| Chemical Properties | Back Directory | [Boiling point ]
1028.3±75.0 °C(Predicted) | [density ]
1.22±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
DMSO: 20mg/mL, clear | [form ]
powder | [pka]
10.39±0.70(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
ILS-920 is a nonimmunosuppressive Rapamycin analog with reduced immunosuppressive activity and potent neuroprotective activity. ILS-920 binds selectively to the immunophilin FKBP52 and to the β1-subunit of L-type voltage-gated calcium channels (VGCC). ILS-920 shows 200-fold selectivity for FKBP52 versus FKBP12[1]. | [Biological Activity]
ILS-920 is a rapamycin derivative with reduced immunosuppressive activity and enhanced neuroprotective activities including efficacy in vivo stroke model. ILS-920 predominantly binds to FKBP52 with a 972-fold higher selectivity for FKBP52 vs. FKBP12 than th at of rapamycinand also binds to the β-subunit of L-type voltage dependent Ca2+ channels. This dual functionality may contribute to the compound′s efficacy in stroke models. | [in vivo]
In a transient middle cerebral artery occlusion (tMCAO) model of ischemic stroke, ILS-920, administered 4 h postocclusion at 10 and 30 mg/kg, significantly reduces infarct volume by 24% and 23% in 72 h, respectively, and robustly enhances functional recovery measured by improvement in neurological deficits[1]. | [IC 50]
L-type calcium channel | [References]
[1] Ruan B, et al. Binding of rapamycin analogs to calcium channels and FKBP52 contributes to their neuroprotective activities. Proc Natl Acad Sci U S A. 2008 Jan 8;105(1):33-8. DOI:10.1073/pnas.0710424105 |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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