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2096455-90-0

中文名稱 2096455-90-0
英文名稱 PF-3893787 hydrochloride
CAS 2096455-90-0
分子式 C13H25ClN6O
分子量 316.83
MOL 文件 2096455-90-0.mol
2096455-90-0 結(jié)構(gòu)式 2096455-90-0 結(jié)構(gòu)式

基本信息

中文別名
化合物 T12435
英文別名
Adriforant hydrochloride
PF-3893787 hydrochloride

物理化學(xué)性質(zhì)

儲存條件-20°C儲存
溶解度DMSO : ≥ 83.33 mg/mL (224.16 mM)
形態(tài)Solid
顏色White to off-white
2096455-90-0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
2024/11/08HY-19705B2096455-90-0
Adriforant hydrochloride
2096455-90-05mg800元
2024/11/08HY-19705B2096455-90-0
Adriforant hydrochloride
2096455-90-010mM * 1mLin DMSO880元
2024/11/08HY-19705B2096455-90-0
Adriforant hydrochloride
2096455-90-010mg1200元

常見問題列表

生物活性
Adriforant hydrochloride (PF-3893787 hydrochloride) 是一種新型組胺 H4 受體親和型拮抗劑 (Ki=2.4 nM),也是一種H4 受體功能性拮抗劑 (Ki=1.56 nM)。
靶點(diǎn)

Ki: 2.4 nM (H4R bind), 1.56 nM (H4R func)

體外研究

Adriforant is tested and observed binding K i =2.4 nM and functional K i =1.56 nM for H4R. Data from functional assays produce convergent projections of the free plasma efficacious concentration and Adriforant (Compound 13) is fast on/fast off on rhH4R. The in vitro IC 50 on human native isolated eosinophils assessing actin polymerisation is 1.16 nM and assuming need 10 times the IC 50 for >90% receptor occupancy (and therefore near complete inhibition of the response) suggested a concentration of 12 nM. The data in the whole blood GAFS assay demonstrates that the imetit induced shape change is completely blocked at a total blood concentration of 30 nM (which correcting for PPB and blood partitioning equates to approximately 10 nM free). For the purpose of dose projection and safety margin calculation, a Ceff/Cmin concentration of 10-15 nM is used.

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