Adriforant hydrochloride PF-3893787 hydrochloride|cas:2096455-90-0|西域试剂

Adriforant hydrochloride PF-3893787 hydrochloride,98.0%

产品编号：Bellancom-19705B| CAS NO：2096455-90-0| 分子式：C₁₃H₂₅Cl₃N₆| 分子量：371.74

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货号	价格	库存与货期
Bellancom-19705B	￥800.00	杭州北京（现货）
Bellancom-19705B	￥1200.00	杭州北京（现货）
Bellancom-19705B	￥3500.00	杭州北京（现货）
Bellancom-19705B	￥5500.00	杭州北京（现货）

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Adriforant hydrochloride PF-3893787 hydrochloride

产品介绍

Adriforant hydrochloride (PF-3893787 hydrochloride) 是一种新型组胺 H4 受体亲和型拮抗剂 (K_i=2.4 nM)，也是一种H4 受体功能性拮抗剂 (K_i=1.56 nM)。

生物活性

Adriforant hydrochloride (PF-3893787 hydrochloride) is a novel histamine H4 receptor antagonist binding affinity (K_i=2.4 nM) and is also a functional (K_i=1.56 nM) antagonist.

体外研究

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 IC₅₀ on human native isolated eosinophils assessing actin polymerisation is 1.16 nM and assuming need 10 times the IC₅₀ 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

性状

Solid

溶解性数据

In Vitro:

H₂O : 100 mg/mL (269.01 mM; Need ultrasonic)

DMSO : ≥ 83.33 mg/mL (224.16 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6901 mL	13.4503 mL	26.9005 mL
5 mM	0.5380 mL	2.6901 mL	5.3801 mL
10 mM	0.2690 mL	1.3450 mL	2.6901 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶