Nylidrin

An agonist of β-ARs and antagonist of NR1A/2B subunit-containing NMDA receptors

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库存: 现货

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5mg

￥512.00

410.00

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10mg

￥937.00

750.00

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25mg

￥1950.00

1560.00

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50mg

￥3375.00

2700.00

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货号: ajcx24634
CAS: 447-41-6
别名: 脑清
分子式: C19H25NO2
分子量: 299.4
纯度: >98%
溶解度: DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:7): 0.12 mg/ml
储存: -20°C
库存: 现货

Background

Nylidrin is an agonist of β-adrenergic receptors and antagonist of NR1A/2B subunit-containing NMDA receptors.^1,2 It binds to β-adrenergic receptors (K_d = 0.37 µM) and activates adenylate cyclase with a K_a value of 1.3 µM.¹ Nylidrin is selective for NR1A/2B over NR1A/2A and NR1A/2C subunit-containing NMDA receptors (IC₅₀s = 0.18, 32, and 42 µM, respectively, for the recombinant receptors expressed in Xenopus oocytes).² It inhibits NMDA-induced currents in primary rat cortical neurons (IC₅₀ = 0.22 µM). It also decreases blood pressure and increases heart rate in spontaneously hypertensive rats (SHRs) with a minimum effective dose (MED) of 0.5 mg/kg.³ Nylidrin (20 and 100 µM) inhibits influenza hemagglutinin 2-mediated membrane fusion in Vero E6 cells.⁴ It inhibits infection of MDCK cells by H1N1 and H3N2 influenza isolates in vitro (EC₅₀s = 7.2 and 12.1 µM, respectively) and prevents infection in a mouse model of mouse-adapted H1N1 infection.

1.Bilezikian, J.P., Dornfeld, A.M., and Gammon, D.E.Structure-binding-activity analysis of beta-adrenergic amines—I. Binding to the beta receptor and activation of adenylate cyclaseBiochem. Pharmacol.27(10)1445-1454(1978) 2.Whittemore, E.R., Ilyin, V.I., Konkoy, C.S., et al.Subtype-selective antagonism of NMDA receptors by nylidrinEur. J. Pharmacol.337(2-3)197-208(1997) 3.Yen, T.T., and Pearson, D.V.Nylidrin: A potent antihypertensive agent in hypertensive ratsRes. Commun. Chem. Pathol. Pharmacol.23(1)11-28(1979) 4.Jang, Y., Shin, J.S., Lee, J.-Y., et al.In vitro and in vivo antiviral activity of nylidrin by targeting the hemagglutinin 2-mediated membrane fusion of influenza A virusViruses12(5)581(2020)