Tirofiban

製品コードS3085 バッチS308501

化学情報

	Synonyms	MK-383	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₂H₃₆N₂O₅S
	分子量	440.6	CAS No.	144494-65-5
Solubility (25°C)*	体外	5%TFA	3.02 mg/mL (6.85 mM)
		DMSO	0.005 mg/mL (0.01 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	Tirofiban (MK-383) is a selective platelet GPIIb/IIIa antagonist which inhibits platelet aggregation with IC50 of 9 nM.
in vitro	Tirofiban (MK-383, Aggrastat) is a nonpeptide derivative of tyrosine that selectively inhibits the GP-IIb/IIIa receptor, with minimal effects on the ɑvβ3 vitronectin receptor. ^[1]^[2] It inhibits platelet aggregation of gel-filtered platelets induced by 10 μM ADP with IC50 of 9 nM, but the IC50 for inhibition of human umbilical vein adhesion to vitronectin, which depends on ɑvβ3 vitronectin receptors, is 62 μmol/L. ^[2]
in vivo	Tirofiban (10 to 500 mg/kg or 360-min continuous i.v. infusions of 1 to 10 micrograms/kg/min) inhibits platelet aggregation responses to ADP and collagen in canine models. ^[3] When administered to humans at 0.15μg/kg/min for 4 h, Tirofiban produced a 2.5-fold increase in bleeding time and 97% inhibition of ADP-induced platelet aggregation. ^[4]^[5]

プロトコル(参考用のみ)

キナーゼアッセイ	Binding assay
キナーゼアッセイ	¹²⁵ I-labeling of human fibrinogen is done usinglodogen reagent as described.22 Platelets are isolated from freshhuman blood drawn into acid/citrate/dextrose by differential centrifugation followed by gel filtration in a modified Tyrode buffer (pH 7.2) containing 2% bovine serum albumin, as previously described.23 Binding of ¹²⁵I-fibrinogen (25 000 cpm/.g) to washed platelets is performed with 108 cells/mL in the presence of 0.5 mM calcium, 25 μM ADP, and MK-383 at the indicated concentration. After an incubation period of 30 minutes, the bound ligand is separated from the free ligand by centrifugation of 80-tuL aliquots of the reaction mixture through a 15% sucrose solution andis quantitated by measuring the radioactivity associated with platelets.

参考

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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：

Coenzyme Q10 attenuates platelet integrin αIIbβ3 signaling and platelet hyper-reactivity in ApoE-deficient mice. [ Food Funct, 2020, 11(1):139-152]	PubMed: 31755492

Coenzyme Q10 attenuates platelet integrin αIIbβ3 signaling and platelet hyper-reactivity in ApoE-deficient mice. [ Food Funct, 2020, 11(1):139-152]

PubMed: 31755492

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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