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SUN 1334H
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SUN 1334H图片
CAS NO:607736-84-5
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
20mg电议

产品介绍
SUN1334H是一种有效的,可口服的,选择性的H1receptor拮抗剂,Ki值为9.7nM。
Cas No.607736-84-5
Canonical SMILESO=C(O)COC/C=C/CN1CCN(C(C2=CC=C(F)C=C2)C3=CC=C(F)C=C3)CC1.[H]Cl.[H]Cl
分子式C23H28Cl2F2N2O3
分子量489.38
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

SUN 1334H is a potent, orally active, highly selective H1 receptor antagonist, with Ki of 9.7 nM.

SUN-1334H causes potent inhibition of histamine induced contractions of isolated guinea-pig ileum with an IC50 (half the maximal inhibitory concentration) of 0.198 μM. In CHO-K1/hERG cells, SUN-1334H does not modulate hERG K+-currents at concentrations as high as 100 μM[1]. SUN-1334H, cetirizine and hydroxyzine cause comparable inhibition of NLF leukocytes, IL-4 and total protein concentrations[2].

SUN-1334H potently inhibits histamine-induced bronchospasm over 24 hours following oral administration and completely suppresses histamine-induced skin wheal in beagle dogs and ovalbumin-induced rhinitis in guinea pigs[1]. In skin allergy models, SUN-1334H shows potent reduction of passive and active cutaneous anaphylactic reactions. In central nervous system side effects models, SUN-1334H, desloratadine and fexofenadine are devoid of any significant effects[2].

[1]. Mandhane SN, et al. Preclinical efficacy and safety pharmacology of SUN-1334H, a potent orally active antihistamine agent. Drugs R D. 2008;9(2):93-112. [2]. Mandhane SN, et al. Characterization of anti-inflammatory properties and evidence for no sedation liability for the novel antihistamine SUN-1334H. Int Arch Allergy Immunol. 2010;151(1):56-69.