Phenothiazine

製品コードS4251 バッチS425101

化学情報

	Synonyms	ENT 38	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₂H₉NS
	分子量	199.27	CAS No.	92-84-2
Solubility (25°C)*	体外	DMSO	40 mg/mL (200.73 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Phenothiazine (ENT 38) is a dopamine-2 (D2) receptor antagonist therefore decreases the effect of dopamine in the brain.
in vitro	Phenothiazines mostly substitutes at position 10 with the dialkylaminoalkyl groups and additionally at position 2 with small groups exhibit valuable activities such as neuroleptic, antiemetic, antihistaminic, antipuritic, analgesic and antihelmintic. 2-trifluoromethyl-10-(4-aminobutyl)phenothiazine inhibits S. cerevisiae strains and T. mentagrophites with MIC of 0.4 μg/mL and 1.5 μg/mL, respectively. 10-carbamoylalkylphenothiazines shows significant activities against Gram-positive Bacillus subtilis with MIC’s in the range of 7.8 μg/mL–30 μg/mL. The tetracyclic phenothiazines (modified with the naphthoquinone ring) shows significant actibacterial activity against S. aureus with the MIC50 of 12.5 μg/mL. Phenothiazines with the butylene linker are more effective than with the propylene linker, the 2-chloro-10-chloroethylureidobutyl derivative giving GI50 of 1.4 μM and 1.6 μM against 4 leukemia cell lines and 7 colon cancer cell lines. 10-Amino(hydroxy)propylphenothiazines (5 μM) induces a marked G2/M phase of cell-cycle arrest followed by cell death in human transformed WI38VA cells after 2-day incubation. ^[1] Phenothiazine drugs undergo extensive metabolism in the body before being excreted, mainly ring hydroxylation, ring sulphoxidation, N-demethylation, N-oxidation, sulphate and glucuronide conjugation. Phenothiazines have considerably lower binding affinities to α2-adrenoceptors than to dopamine D2 receptors and al-adrenoceptors. ^[2] Phenothiazines have significant in vitro activity against susceptible, polydrug- and multidrug-resistant strains of M. tuberculosis, as well as enhancing the activity of some agents employed for first-line treatment. ^[3]

製品説明

Phenothiazine (ENT 38) is a dopamine-2 (D2) receptor antagonist therefore decreases the effect of dopamine in the brain.

in vitro

Phenothiazines mostly substitutes at position 10 with the dialkylaminoalkyl groups and additionally at position 2 with small groups exhibit valuable activities such as neuroleptic, antiemetic, antihistaminic, antipuritic, analgesic and antihelmintic. 2-trifluoromethyl-10-(4-aminobutyl)phenothiazine inhibits S. cerevisiae strains and T. mentagrophites with MIC of 0.4 μg/mL and 1.5 μg/mL, respectively. 10-carbamoylalkylphenothiazines shows significant activities against Gram-positive Bacillus subtilis with MIC’s in the range of 7.8 μg/mL–30 μg/mL. The tetracyclic phenothiazines (modified with the naphthoquinone ring) shows significant actibacterial activity against S. aureus with the MIC50 of 12.5 μg/mL. Phenothiazines with the butylene linker are more effective than with the propylene linker, the 2-chloro-10-chloroethylureidobutyl derivative giving GI50 of 1.4 μM and 1.6 μM against 4 leukemia cell lines and 7 colon cancer cell lines. 10-Amino(hydroxy)propylphenothiazines (5 μM) induces a marked G2/M phase of cell-cycle arrest followed by cell death in human transformed WI38VA cells after 2-day incubation. ^[1] Phenothiazine drugs undergo extensive metabolism in the body before being excreted, mainly ring hydroxylation, ring sulphoxidation, N-demethylation, N-oxidation, sulphate and glucuronide conjugation. Phenothiazines have considerably lower binding affinities to α2-adrenoceptors than to dopamine D2 receptors and al-adrenoceptors. ^[2] Phenothiazines have significant in vitro activity against susceptible, polydrug- and multidrug-resistant strains of M. tuberculosis, as well as enhancing the activity of some agents employed for first-line treatment. ^[3]

プロトコル(参考用のみ)

参考

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。