YM-5883
中文名称 | YM-5883 |
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中文同义词 | 化合物YM58483;N-(4-(3,5-二(三氟甲基)-1H-吡唑-1-基)苯基)-4-甲基-1,2,3-噻二唑-5-甲酰胺 |
英文名称 | BTP2 |
英文同义词 | BTP2;N-[4-[3,5-BIS(TRIFLUOROMETHYL)-1H-PYRAZOL-1-YL]PHENYL]-4-METHYL-1,2,3-THIADIAZOLE-5-CARBOXAMIDE;4-methyl-4μ-[3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl]-1,2,3-thiadiazole-5-carboxanilide;YM-58483;CRAC Channel Inhibitor, BTP2;YM-58483(BTP2);BTP 2, N-[4-[3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-4-methyl-1,2,3-thiadiazole-5-carboxamide;YM-5883 |
CAS号 | 223499-30-7 |
分子式 | C15H9F6N5OS |
分子量 | 421.32 |
EINECS号 | |
相关类别 | 抑制剂 |
Mol文件 | 223499-30-7.mol |
结构式 |
YM-5883 性质
熔点 | 165-167 °C |
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密度 | 1.63±0.1 g/cm3(Predicted) |
储存条件 | 2-8°C |
溶解度 | DMSO:可溶10mg/mL,澄清 |
酸度系数(pKa) | 10.53±0.70(Predicted) |
形态 | 固体 |
颜色 | 白色至米色 |
YM-58483 can decrease the levels of P-ERK and P-CREB, without affecting the expression of CD11b and GFAP. YM-58483 also inhibits the release of spinal cord IL-1β, TNF-α, and PGE2. YM-58483 and cyclosporine A inhibits T cell proliferation in a one-way mixed lymphocyte reaction (mLR) with IC 50 values of 330 and 12.7 nM, respectively. YM-58483 inhibits DNP antigen-induced histamine release from and leukotrienes (LTs) production in IgE-primed RBL-2H3 cells, a rat basophilic leukemia cell line, with IC 50 values of 460 and 310 nM, respectively. YM-58483 also inhibits phytohemagglutinin-P (PHA)-stimulated IL-5 and IL-13 production in human peripheral blood cells with IC 50 values of 125 and 148 nM, respectively, which is approximately 5 times less potent than prednisolone. YM-58483 inhibits IL-4 and IL-5 production in a conalbumine-stimulated murine Th2 T cell clone (D10.G4.1), and IL-5 production in phytohemagglutinin-stimulated human whole blood cells with IC 50 values comparable to those reported for its CRAC channel inhibition (around 100 nM).
Intrathecal YM-58483 at the concentration of 300 μM (1.5 nmol) and 1000 μM (10 nmol) produces a significant central analgesic effect on the SNL rats. In the mouse graft-versus-host disease (GVHD) model, YM-58483 (1-30 mg/kg, p.o.) and cyclosporine A (1-30 mg/kg, p.o.) inhibit donor anti-host cytotoxic T lymphocyte (CTL) activity and IFN-γ production, and also reduce the number of donor T cells, especially donor CD8 + T cells, in the spleen. YM-58483 (1-10 mg/kg, p.o.) and cyclosporine A (2, 10 mg/kg, p.o.) inhibit the sheep red blood cell (SRBC)-induced delayed type hypersensitivity (DTH) response. M-58483 (30 mg/kg, p.o.) significantly suppresses ovalbumin (OVA)-induced bronchoconstriction in OVA-sensitized guinea pigs, whereas prednisolone does not. YM-58483 (3-30 mg/kg, p.o.) and prednisolone (100 mg/kg, p.o.) both significantly and completely suppress airway hyperresponsiveness (AHR) caused by OVA exposure. YM-58483 inhibits antigen-induced eosinophil infiltration into airways, and decreases IL-4 and cysteinyl-leukotrienes content in inflammatory airways induced in actively sensitized Brown Norway rats. Orally administered YM-58483 prevents antigen-induced late phase asthmatic broncoconstriction and eosinophil infiltration in actively sensitized guinea pigs.
安全信息
危险品标志 | Xn |
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危险类别码 | 22-36/37/38 |
安全说明 | 26-36/37 |
WGK Germany | 3 |
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/04/30 | HY-100831 | YM-5883 YM-58483 | 223499-30-7 | 2mg | 500元 |
2024/04/30 | HY-100831 | YM-5883 YM-58483 | 223499-30-7 | 10mM * 1mLin DMSO | 742元 |