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(±)-Tazifylline

カタログ番号GC31026

(±)-タジフィリンは、強力で選択的な長時間作用型のヒスタミン H1 受容体拮抗薬です。

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(±)-Tazifylline 化学構造

Cas No.: 79712-55-3

サイズ 価格 在庫数 個数
1mg
$276.00
在庫あり
5mg
$552.00
在庫あり
10mg
$937.00
在庫あり
20mg
$1,655.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

(±)-Tazifylline is a potent, selective and long-acting histamine H1 receptor antagonist.

Tazifylline potently inhibits contractions evoked by stimulation of histamine H1-receptors in isolated guinea pig ilea and exhibits high affinity for these receptors in radioligand binding studies in vitro Tazifylline has much lower affinity for histamine H2-receptors, alpha- and beta-adrenoceptors, 5-hydroxytryptamine and muscarinic receptor subtypes. Tazifylline poorly inhibits the release of histamine from rat peritoneal mast cells[1].

In rats, guinea pigs and dogs the antihistaminic effect of Tazifylline is rapid in onset and long-lived. In anesthetized guinea pigs, Tazifylline markedly inhibits histamine-induced bronchoconstriction and protects conscious animals from the lethal effect of large doses of the amine. In conscious rats, Tazifylline is more potent in reducing the inflammatory effects of intradermal histamine than that evoked by anaphylactic reaction. In conscious dogs, orally administered Tazifylline inhibits histamine-induced skin inflammation for long periods of time and in anesthetized animals attenuated that portion of the histamine-evoked hypotension attributable to stimulation of H1-receptors. Large oral doses of Tazifylline does not reduce spontaneous locomotor activity in mice, nor do they produce overt symptoms of behavioral depression in conscious rats[1].

[1]. Poizot A, et al. Animal pharmacology of the selective histamine H1-receptor antagonist tazifylline. Arzneimittelforschung. 1986 Apr;36(4):695-702.

Chemical Properties

Cas No. 79712-55-3 SDF
Canonical SMILES O=C(N1C)N(C)C2=C(N(CC(O)CN3CCN(CCCSC4=CC=CC=C4)CC3)C=N2)C1=O
Formula C23H32N6O3S M.Wt 472.6
溶解度 Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.116 mL 10.5798 mL 21.1595 mL
5 mM 0.4232 mL 2.116 mL 4.2319 mL
10 mM 0.2116 mL 1.058 mL 2.116 mL
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