Timolol Maleate

製品コードS4123 バッチS412302

化学情報

	Synonyms	MK-950,(S)-Timolol Maleate	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₃H₂₄N₄O₃S.C₄H₄O₄
	分子量	432.49	CAS No.	26921-17-5
Solubility (25°C)*	体外	DMSO	86 mg/mL (198.84 mM)
		Ethanol	4 mg/mL (9.24 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Timolol Maleate (MK-950,(S)-Timolol Maleate) is a non-selective, beta-adrenergic receptor antagonist for β1/β2 with K_i of 1.97 nM/2.0 nM.
in vitro	Timolol Maleate is a beta-adrenergic antagonist similar in action to propranolol. The levo-isomer is the more active. Timolol has been proposed as an antihypertensive, antiarrhythmic, antiangina, and antiglaucoma agent. Similar to propranolol and nadolol, timolol is a non-selective, beta-adrenergic receptor antagonist. ^[1] Timolol has a higher affinity for the beta 2-adrenoceptor than for the beta 1-adrenoceptor in human atrium. Timolol does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity, but does possess a relatively high degree of lipid solubility. ^[3] Timolol, when applied topically to the eye, has the action of reducing elevated, as well as normal, intraocular pressure, whether or not accompanied by glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual field loss and optic nerve damage. ^[4] Like propranolol and nadolol, timolol competes with adrenergic neurotransmitters such as catecholamines for binding at β1-adrenergic receptors in the heart and vascular smooth muscle and β2-receptors in the bronchial and vascular smooth muscle. β1-receptor blockade results in a decrease in resting and exercise heart rate and cardiac output, a decrease in both systolic and diastolic blood pressure, and, possibly, a reduction in reflex orthostatic hypotension. β2-blockade results in an increase in peripheral vascular resistance. The exact mechanism whereby timolol reduces ocular pressure is still not known. The most likely action is by decreasing the secretion of aqueous humor. ^[2]

製品説明

Timolol Maleate (MK-950,(S)-Timolol Maleate) is a non-selective, beta-adrenergic receptor antagonist for β1/β2 with K_i of 1.97 nM/2.0 nM.

in vitro

Timolol Maleate is a beta-adrenergic antagonist similar in action to propranolol. The levo-isomer is the more active. Timolol has been proposed as an antihypertensive, antiarrhythmic, antiangina, and antiglaucoma agent. Similar to propranolol and nadolol, timolol is a non-selective, beta-adrenergic receptor antagonist. ^[1] Timolol has a higher affinity for the beta 2-adrenoceptor than for the beta 1-adrenoceptor in human atrium. Timolol does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity, but does possess a relatively high degree of lipid solubility. ^[3] Timolol, when applied topically to the eye, has the action of reducing elevated, as well as normal, intraocular pressure, whether or not accompanied by glaucoma. Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual field loss and optic nerve damage. ^[4] Like propranolol and nadolol, timolol competes with adrenergic neurotransmitters such as catecholamines for binding at β1-adrenergic receptors in the heart and vascular smooth muscle and β2-receptors in the bronchial and vascular smooth muscle. β1-receptor blockade results in a decrease in resting and exercise heart rate and cardiac output, a decrease in both systolic and diastolic blood pressure, and, possibly, a reduction in reflex orthostatic hypotension. β2-blockade results in an increase in peripheral vascular resistance. The exact mechanism whereby timolol reduces ocular pressure is still not known. The most likely action is by decreasing the secretion of aqueous humor. ^[2]

プロトコル(参考用のみ)

参考

[4] Hirooka K, et al. Exp Eye Res, 2000, 70(5), 611-621.

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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：

Fractional 2940-nm Er:YAG laser-assisted drug delivery of timolol maleate for the treatment of deep infantile hemangioma. [ J Dermatolog Treat, 2020, 24:1-7]	PubMed: 32043380

Fractional 2940-nm Er:YAG laser-assisted drug delivery of timolol maleate for the treatment of deep infantile hemangioma. [ J Dermatolog Treat, 2020, 24:1-7]

PubMed: 32043380

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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