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648449-76-7

中文名稱 5-[(2,2-二氟-1,3-苯并二惡茂-5-基)亞甲基]噻唑烷-2,4-二酮
英文名稱 AS 604850
CAS 648449-76-7
分子式 C11H5F2NO4S
分子量 285.22
MOL 文件 648449-76-7.mol
更新日期 2024/12/15 19:35:15
648449-76-7 結(jié)構(gòu)式 648449-76-7 結(jié)構(gòu)式

基本信息

中文別名
5-(2,2-二氟-苯唑[1,3]二氧-5-基亞甲基)-噻唑烷-2,4-二酮
5-[(2,2-二氟-1,3-苯并二惡茂-5-基)亞甲基]噻唑烷-2,4-二酮
英文別名
CS-538
AS 604850
AS-604850
AS 604850
AS 604850 USP/EP/BP
PI 3-Kγ Inhibitor II
AS604850
AS 604850
AS-604850
PI 3-Kinase Inhibitor (AS604850)
PI 3-Kinase Inhibitor (AS604850) B-0302
PI 3-Kγ Inhibitor II - CAS 648449-76-7 - Calbiochem
5-[(2,2-Difluoro-1,3-benzodioxol-5-yl)methylene]thiazolidine-2,4-dione

物理化學(xué)性質(zhì)

密度1.71
儲(chǔ)存條件2-8°C
溶解度二甲基亞砜:>10mg/mL
酸度系數(shù)(pKa)7.07±0.20(Predicted)
形態(tài)固體
顏色米白色

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H317
防范說(shuō)明P280
危險(xiǎn)品標(biāo)志Xi
危險(xiǎn)類(lèi)別碼43
安全說(shuō)明36/37
WGK Germany3
5-[(2,2-二氟-1,3-苯并二惡茂-5-基)亞甲基]噻唑烷-2,4-二酮價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-135315-[(2,2-二氟-1,3-苯并二惡茂-5-基)亞甲基]噻唑烷-2,4-二酮
AS-604850
648449-76-75mg579元
2024/11/08HY-135315-[(2,2-二氟-1,3-苯并二惡茂-5-基)亞甲基]噻唑烷-2,4-二酮
AS-604850
648449-76-710 mM * 1 mLin DMSO715元
2024/11/08HY-135315-[(2,2-二氟-1,3-苯并二惡茂-5-基)亞甲基]噻唑烷-2,4-二酮
AS-604850
648449-76-710mg910元

常見(jiàn)問(wèn)題列表

生物活性
AS-604850 是一種有效的,具有選擇性的和 ATP 競(jìng)爭(zhēng)性的 PI3Kγ 抑制劑,IC50 值為 0.25 μM,Ki 值為 0.18 μM。AS-604850 是 PI3Kγ 的同工型選擇性抑制劑,對(duì) PI3Kγ 的選擇性是 PI3Kδ/β 的 30 倍以上,是 PI3Kα 的 18 倍以上。
靶點(diǎn)

PI3Kγ

0.25 μM (IC 50 )

PI3Kγ

0.18 μM (Ki)

PI3Kα

4.5 μM (IC 50 )

體外研究

AS-604850 inhibits C5a-mediated PKB phosphorylation with an IC 50 of 10 μM in RAW264 mouse macrophages.
AS-604850 blocks PKB phosphorylation induced by MCP-1 and has little or no effect after stimulation with CSF-1 in in primary monocytes from Pik3cg +/+ or Pik3cg –/– mice.
AS-604850 (0-30 μM; 15 minutes; primary monocytes from Pik3cg +/+ mice) treatment inhibits MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3α andβ in a concentration-dependent manner. MCP-1-induced phosphorylation of p44/42 ERK (ERK1/2) MAPKs is also reduced, in a concentration dependent manner in primary monocytes from Pik3cg +/+ mice.

Western Blot Analysis

Cell Line: Primary monocytes from Pik3cg +/+ mice
Concentration: 0 μM, 1 μM, 3 μM, 10 μM, 30 μM
Incubation Time: 15 minutes
Result: Inhibited MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3α andβ in a concentration-dependent manner. MCP-1-induced phosphorylation of p44/42 ERK (ERK1/2) MAPKs was also reduced, in a concentrationdependent manner in primary monocytes from Pik3cg +/+ mice.
體內(nèi)研究

AS-604850 (10-100 mg/kg; oral administration; for 4.5 or 4.25 hours; Balb/C or C3H mice) treatment reduces RANTES-induced peritoneal neutrophil recruitment with an ED 50 value of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, oral administration of 10 mg/kg AS-604850 results in a 31% reduction of neutrophil recruitment.

Animal Model: Balb/C or C3H mice with human recombinant RANTES or thioglycollate
Dosage: 10 mg/kg, 30 mg/kg or 100 mg/kg
Administration: Oral administration; for 4.5 or 4.25 hours
Result: Reduced RANTES-induced peritoneal neutrophil recruitment with an ED 50 value of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, resulted in a 31% reduction of neutrophil recruitment.
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