CAS NO: | 50847-11-5 |
规格: | ≥98% |
包装 | 价格(元) |
2mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
1g | 电议 |
Molecular Weight (MW) | 230.31 |
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Formula | C14H18N2O |
CAS No. | 50847-11-5 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: 46 mg/mL (199.7 mM) |
Water: <1 mg/mL | |
Ethanol: 46 mg/mL (199.7 mM) | |
Solubility (In vivo) | ~2.7 mg/mL in 10% DMSO : 90% (20% SBE-β-CD in saline) ~2.7 mg/mL in 10% DMSO : 40% PEG300 : 5% Tween-80 : 45% saline ~2.7 mg/mL in 10% DMSO : 90% corn oil |
Synonyms | Ibudilast; AV-411, KC-404; KC 404; MN-166, AV 411, AV411, KC404; MN166, MN 166 Chemical Name: 2-methyl-1-(2-propan-2-ylpyrazolo[1,5-a]pyridin-3-yl)propan-1-one Exact Mass: 230.1419 |
SMILES Code | CC(C)C(C1=C2C=CC=CN2N=C1C(C)C)=O |
In Vitro | In vitro activity: Ibudilast inhibits pro-inflammatory cytokines (IL-6, IL-1β, TNF-α), toll-like receptor 4 blockade (TLR-4); suppresses a macrophage migration inhibitory factor (MIF), upregulates the anti-inflammatory cytokine (IL-10) and promotes neurotrophic factors (GDNF, NGF, NT-4). |
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In Vivo | Ibudilast is able to cross the blood-brain barrier and has a good tolerance. It inhibits platelet aggregation, improves cerebral blood flow and attenuates allergic reactions in clinical applications. In an animal model of encephalomyelitis, Ibudilast significantly attenuates inflammatory cell infiltration in the lumbar spinal cord. After oral administration, it is well absorbed and metabolized in the liver mainly to diOH-ibudilast, which has similar or even stronger pharmacological effects |
Animal model | Carotid artery thrombosis model |
Formulation & Dosage | Dissolved in saline; 0.3 and 1.0 mg/kg; i.v. |
References | Cardiovasc Drug Rev. 2001 Fall;19(3):215-25. |