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HSR6071 Sale

目录号 : GC32056

HSR6071是一种具有治疗哮喘潜力的抗过敏剂。

HSR6071 Chemical Structure

Cas No.:111374-21-1

规格 价格 库存 购买数量
1mg
¥1,080.00
现货
5mg
¥2,700.00
现货
10mg
¥4,320.00
现货

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Sample solution is provided at 25 µL, 10mM.

Description

HSR6071 is an antiallergic agent with potential for the treatment of asthma.

HSR-6071 suppresses antigen-induced histamine and SRS-A release from minced lung tissues of guinea-pigs sensitized passively with rabbit anti-EA serum and is a more potent inhibitor of the release of SRS-A than of histamine. On the other hand, histamine- or acetylcholine-induced bronchoconstriction in guinea-pigs is scarcely affected by HSR-6071 at doses sufficient to inhibit the experimental asthma, but LTD4-induced bronchoconstriction is dramatically inhibited. HSR-6071 inhibits cyclic AMP phosphodiesterase activity and produces relaxation of the guinea-pig isolated trachea[1]. HSR-6071 inhibits the IgE-mediated histamine release with an IC50 of 0.46 nM. HSR-6071 is effective not only by i.v. but also by p.o. administration on the IgE mediated PCA in rats. The most potent inhibition with HSR-6071 is observed when it is given p.o. 5 min before the antigen challenge, indicating the rapid absorption of HSR-6071 through the gastrointestinal tract[2].

[1]. Makino E, et al. Inhibitory effect of HSR-6071, a new anti-allergic agent, on experimental asthma in rats and guinea-pigs. J Pharm Pharmacol. 1990 Apr;42(4):236-41. [2]. Makino E, et al. Potent inhibitory activity of HSR-6071, a new antiallergic agent, on passive cutaneousanaphylaxis (PCA). Jpn J Pharmacol. 1990 Jan;52(1):87-94.

实验参考方法

Animal experiment:

Rats: In order to find out the proper pre treatment time with HSR-6071, 0.03 mg/kg, i.vi or 1 mg/kg, p.o. of HSR-6071 was given at varying times before the antigen challenge[2].

References:

[1]. Makino E, et al. Inhibitory effect of HSR-6071, a new anti-allergic agent, on experimental asthma in rats and guinea-pigs. J Pharm Pharmacol. 1990 Apr;42(4):236-41.
[2]. Makino E, et al. Potent inhibitory activity of HSR-6071, a new antiallergic agent, on passive cutaneousanaphylaxis (PCA). Jpn J Pharmacol. 1990 Jan;52(1):87-94.

化学性质

Cas No. 111374-21-1 SDF
Canonical SMILES O=C(C1=NC(N2CCCC2)=CN=C1)NC3=NN=NN3
分子式 C10H12N8O 分子量 260.26
溶解度 H2O : 50 mg/mL (192.12 mM; ultrasonic and adjust pH to 12 with NaOH) 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.8423 mL 19.2116 mL 38.4231 mL
5 mM 0.7685 mL 3.8423 mL 7.6846 mL
10 mM 0.3842 mL 1.9212 mL 3.8423 mL
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