Piclamilast RP 73401; RPR 73401|cas:144035-83-6|西域试剂

Piclamilast RP 73401; RPR 73401

产品编号：Bellancom-12887| CAS NO：144035-83-6| 分子式：C₁₈H₁₈Cl₂N₂O₃| 分子量：381.25

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货号	价格	库存与货期
Bellancom-12887	￥1500.00	杭州北京（现货）
Bellancom-12887	￥2400.00	杭州北京（现货）
Bellancom-12887	￥5200.00	杭州北京（现货）
Bellancom-12887	￥8300.00	杭州北京（现货）

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Piclamilast RP 73401; RPR 73401

产品介绍

Piclamilast (RP 73401) 是有效的磷酸二酯酶 4 (PDE4) 的抑制剂，其在猪主动脉和可溶性嗜酸性粒细胞中的 IC₅₀ 值分别为 16 nM 和 2 nM。

生物活性

Piclamilast (RP 73401) is a phosphodiesterase 4 (PDE4) inhibitor, with IC₅₀ values of 16 nM and 2 nM in pig aorta and eosinophil soluble, respectively^[4].

体外研究

Piclamilast (RP 73401, 1 μM, 30 min) significantly inhibits the changes in 23 genes via mechanisms involving AP-1 activation and c-Jun phosphorylation at Ser63.
Piclamilast (RP 73401) exhibits IC₅₀ values >100 μM, 40 μM, >100 μM, 14 μM for PDE1, PDE2, PDE3 and PDE5. Respectively^[4].

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

RT-PCR

Cell Line:	Human A549 type II lung epithelial cells.
Concentration:	1 μM (H₂O₂ 200 μM).
Incubation Time:	30 min.
Result:	Prevented H₂O₂ -induced changes in gene expression levels in A549 cells.

Cell Viability Assay

Cell Line:	NB4 cells.
Concentration:	30 μM.
Incubation Time:	3 days.
Result:	Exerted a significant enhancing effect on the induction of STAT1 observed in ATRA-treated NB4 cells. Caused a significant increase in the number of cells expressing NBT-R activity.

体内研究
(In Vivo)

Piclamilast (RP 73401, 10 mg/kg, 30 min) alone does not affect the MST of leukemia-bearing animals. Piclamilast combined with ATRA (HY-14649) significantly more effective than ATRA alone in increasing the MST (40 days; interval 34–45 days) of leukemia-bearing animals.

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

Animal Model:	SCID mice.
Dosage:	10 mg/kg (combined with ATRA (HY-14649)).
Administration:	Injection daily.
Result:	Significantly more effective than ATRA alone in increasing the MST (40 days; interval 34–45 days) of leukemia-bearing animals.

体内研究

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

Animal Model:	SCID mice.
Dosage:	10 mg/kg (combined with ATRA (HY-14649)).
Administration:	Injection daily.
Result:	Significantly more effective than ATRA alone in increasing the MST (40 days; interval 34–45 days) of leukemia-bearing animals.

体内研究

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

Animal Model:	SCID mice.
Dosage:	10 mg/kg (combined with ATRA (HY-14649)).
Administration:	Injection daily.
Result:	Significantly more effective than ATRA alone in increasing the MST (40 days; interval 34–45 days) of leukemia-bearing animals.

性状

Solid

溶解性数据

In Vitro:

DMSO : 33.33 mg/mL (87.42 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6230 mL	13.1148 mL	26.2295 mL
5 mM	0.5246 mL	2.6230 mL	5.2459 mL
10 mM	0.2623 mL	1.3115 mL	2.6230 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。-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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式