2096455-90-0
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- CAS号:
- 2096455-90-0
- 英文名:
- PF-3893787 hydrochloride
- 英文别名:
- Adriforant hydrochloride;PF-3893787 hydrochloride
- 中文名:
- 2096455-90-0
- 中文别名:
- 化合物 T12435
- CBNumber:
- CB14694839
- 分子式:
- C13H25ClN6O
- 分子量:
- 316.83
- MOL File:
- 2096455-90-0.mol
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2096455-90-0化学性质
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储存条件:
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Store at -20°C
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溶解度:
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DMSO : ≥ 83.33 mg/mL (224.16 mM)
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2096455-90-0性质、用途与生产工艺
Adriforant hydrochloride (PF-3893787 hydrochloride) 是一种新型组胺 H4 受体亲和型拮抗剂 (Ki=2.4 nM),也是一种H4 受体功能性拮抗剂 (Ki=1.56 nM)。
Ki: 2.4 nM (H4R bind), 1.56 nM (H4R func)
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.
2096455-90-0
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更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-19705B | 2096455-90-0 Adriforant hydrochloride | 2096455-90-0 | 5mg | 800元 |
2024/04/30 | HY-19705B | 2096455-90-0 Adriforant hydrochloride | 2096455-90-0 | 10mM * 1mLin DMSO | 880元 |
2096455-90-0, 2096455-90-0 相关搜索:
- 化合物 T12435
- 2096455-90-0
- Adriforant hydrochloride
- PF-3893787 hydrochloride