Clotrimazole

製品コードS1606 バッチS160602

化学情報

	Synonyms	BAY b 5097, FB 5097	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₂H₁₇ClN₂
	分子量	344.84	CAS No.	23593-75-1
Solubility (25°C)*	体外	Ethanol	69 mg/mL (200.09 mM)
		DMSO	11 mg/mL (31.89 mM)
		Water	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.

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生物活性

製品説明	Clotrimazole (BAY b 5097, FB 5097) alters the permeability of the fungal cell wall by inhibiting the biosynthesis of ergosterol, used in the treatment of fungal infections.
in vitro	Clotrimazole causes a sustained depletion of intracellular Ca2+ stores, which results in activation of PKR, phosphorylation of eIF2alpha, and thereby in inhibition of protein synthesis at the level of translation initiation. Clotrimazole preferentially decreases the expression of the growth promoting proteins cyclin A, E and D1, resulting in inhibition of cyclin-dependent kinase activity and blockage of cell cycle in G1.^[1] Clotrimazole inhibits ADP-ribose-activated currents in HEK-293 cells expressing recombinant human TRPM2(hTRPM2). Clotrimazole (3 mM to 30 mM) produces an essentially complete inhibition of theTRPM2-mediated current. Clotrimazole antagonizes ADP-ribose-activated whole-cell and single-channel currents in the rat insulinoma cell-line CRI-G1. ^[2] Clotrimazole (2 mM) causes a sharp decline in parasitemia, complete inhibition of parasite replication, and destruction of parasites and host cells within a single intraerythrocytic asexual cycle (approximately 48 hours). Clotrimazole effectively and rapidly inhibits parasite growth in five different strains of P. falciparum, in vitro, irrespective of their Chloroquine sensitivity. ^[3]
in vivo	Clotrimazole stimulates a subset of capsaicin-sensitive and mustard oil-sensitive trigeminal neurons, and evoked nocifensive behavior and thermal hypersensitivity with intraplantar injection in mice. Clotrimazole-induced pain behavior is suppressed by the TRPV1-antagonist BCTC [(N-(-4-tertiarybutylphenyl)-4-(3-cholorpyridin-2-yl)tetrahydropyrazine-1(2H)-carboxamide)] and absent in TRPV1-deficient mice. Clotrimazole inhibits the cold and menthol receptor TRPM8, and blocks menthol-induced responses in capsaicin- and mustard oil-insensitive trigeminal neurons. ^[4]

プロトコル(参考用のみ)

参考

[4] Meseguer V, et al. J Neurosci,?008, 28(3), 576-586.

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Lipopolysaccharide induces placental mitochondrial dysfunction in murine and human systems by reducing MNRR1 levels via a TLR4-independent pathway [ iScience, 2022, 25(11):105342]	PubMed: 36339251
Ultra-fast proteomics with Scanning SWATH [ Nat Biotechnol, 2021, 10.1038/s41587-021-00860-4]	PubMed: 33767396
The protective effect of EGF-activated ROS in human corneal epithelial cells by inducing mitochondrial autophagy via activation TRPM2. [ J Cell Physiol, 2020, 10.1002]	PubMed: 32083315
Interaction of the phosphorylated DNA-binding domain in nuclear receptor CAR with its ligand-binding domain regulates CAR activation [Shizu R, et al. J Biol Chem, 2018, 293(1):333-344]	PubMed: 29133527

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。

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