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223499-30-7

中文名稱 YM-5883
英文名稱 BTP2
CAS 223499-30-7
分子式 C15H9F6N5OS
分子量 421.32
MOL 文件 223499-30-7.mol
更新日期 2024/10/25 11:17:12
223499-30-7 結(jié)構(gòu)式 223499-30-7 結(jié)構(gòu)式

基本信息

中文別名
化合物YM58483
英文別名
BTP2
BPT2
CS-2404
YM-5883
YM-58483
YM-58483(BTP2)
YM58483
YM 58483
BPT2
CRAC Channel Inhibitor, BTP2
CRAC Channel Inhibitor, BTP2 - CAS 223499-30-7 - Calbiochem
N-[4-[3,5-bis(trifluoromethyl)pyrazol-1-yl]phenyl]-4-methylthiadiazole-5-carboxamide
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

熔點165-167 °C
密度1.63±0.1 g/cm3(Predicted)
儲存條件2-8°C
溶解度DMSO:可溶10mg/mL,澄清
酸度系數(shù)(pKa)10.53±0.70(Predicted)
形態(tài)固體
顏色白色至米色

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335
危險品標(biāo)志Xn
危險類別碼22-36/37/38
安全說明26-36/37
WGK Germany3

圖譜信息

YM-5883價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/08/19HY-100831YM-5883
YM-58483
223499-30-72mg500元
2024/08/19HY-100831YM-5883
YM-58483
223499-30-710mM * 1mLin DMSO742元
2024/08/19HY-100831YM-5883
YM-58483
223499-30-75mg800元

常見問題列表

生物活性
YM-58483 是一種有效的 CRAC channels 抑制劑,能夠抑制 Ca2+ 信號。
體外研究

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).

體內(nèi)研究

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.

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