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化學性質:
規格 | 5mg 10mg |
CAS | 1245319-54-3 |
別名 | PI4KIII beta inhibitor 3 |
化學名 | 4-(5-amino-2-pyridin-3-yl-[1,3]thiazolo[5,4-d]pyrimidin-7-yl)-N-(4-methylphenyl)piperazine-1-carboxamide |
分子式 | C22H22N8OS |
分子量 | 446.53 |
溶解度 | Soluble in DMSO |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述:
PI4KIII beta inhibitor 3 is a novel and high effective PI4KIIIβ inhibitor with IC50 of 5.7 nM.
PI4KIII beta inhibitor 3 is a PI4KIII inhibitor extracted from patent WO/2013034738 A1, the compound of formula 3, has an IC50 of 5.7 nM. PI4KIII beta inhibitor 3 exerts significant immunosuppressive activity, with IC50 value of 3 nM in the mixed lymphocyte reaction (MLR) assay. PI4KIII beta inhibitor 3 inhibits IL2 and IFNy secretion with IC50 values of less than InM in each case. Thus, PI4KIII beta inhibitor 3 is shown to be as effective at inhibiting IL2 and IFNy secretion as conventional immunosuppressants such as cyclosporine A. IC50 on IFNy and IL-2 release of Cyclosporine A are 2nM and less than 1 nM respectively[1].
PI4KIII beta inhibitor 3 (40 mg/kg per day, n=12) is able to delay the onset of arthritic symptoms and also to decrease symptom severity in a preventive model of arthritis compared to a vehicle control (MC 1%, n=12). PI4KIII beta inhibitor 3 reduces the anti-CII IgG titre and histological scores in the collagen-induced arthritis mouse model. Oral administration of PI4KIII beta inhibitor 3 results in prolonged graft survival in 3 out of 6 grafts in each group at day 30. Several grafts continued beating after withdrawal of the treatment (up to 60 days), indicating the induction of a certain type of graft tolerance. To evaluate the operational tolerance phenotype, animals with functional graft at day 60 are challenged with a second graft from the same donor strain or from a third party. No treatment is applied. The second grafts from the third party are rejected at day 8 (n=2) whereas second grafts from the same donor strain are functional for more than 90 days (n=2)[1].
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原創作者:上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業部
賬 號:2169 2341 6278