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1,4-PBIT (dihydrobromide) Sale

目录号 : GC14627

A potent inhibitor of iNOS and nNOS

1,4-PBIT (dihydrobromide) Chemical Structure

Cas No.:157254-60-9

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10mg
¥222.00
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50mg
¥936.00
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100mg
¥1,650.00
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500mg
¥7,202.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

1,4-PBIT (dihydrobromide) is a potent inhibitor of iNOS and nNOS with Ki values of 7.4 and 16 nM, respectively [1].

Nitric oxide (NO) is an endogenously produced inorganic free radical gas which has been implicated in blood pressure homeostasis, platelet aggregation, neurotransmission, and immunological defense mechanisms. NO is synthesized by three isoforms of nitric oxide synthase (NOS): nNOS, eNOS and iNOS [1].

1,4-PBIT, also known as S,S’-(1,4-Phenylenebis(1,2-ethanediyl))bisisothiourea, is a potent and selective iNOS and nNOS inhibitor. 1,4-PBIT inhibited purified human iNOS, eNOS and nNOS with Ki values of 7.4 nM, 360 nM and 16 nM, respectively. In DLD-1 cells, 1,4-PBIT inhibited human iNOS with IC50 value of 30 μM, presumably to poor membrane permeability [1].

In anesthetized rats, 1,4-PBIT (10 mg/kg, given 1 h after LPS administration), 1,4-PBIT effectively reversed the systemic hypotension, reduced the exhaled NO concentration and prevented acute lung injury. 1,4-PBIT also significantly depressed LPS-induced mRNA expressions of iNOS and IL-1β[2].

References:
[1].  Garvey EP, Oplinger JA, Tanoury GJ, et al. Potent and selective inhibition of human nitric oxide synthases. Inhibition by non-amino acid isothioureas. J Biol Chem. 1994 Oct 28;269(43):26669-76.
[2].  Wang D, Wei J, Hsu K, et al. Effects of nitric oxide synthase inhibitors on systemic hypotension, cytokines and inducible nitric oxide synthase expression and lung injury following endotoxin administration in rats. J Biomed Sci. 1999 Jan;6(1):28-35.

Chemical Properties

Cas No. 157254-60-9 SDF
化学名 S,S'-1,4-phenylene-bis(1,2-ethanediyl)bis-isothiourea, dihydrobromide
Canonical SMILES N/C(SCCC1=CC=C(CCS/C(N)=N/[H])C=C1)=N/[H].Br.Br
分子式 C12H18N4S2 • 2HBr 分子量 444.2
溶解度 ≤20mg/ml in DMSO;20mg/ml in dimethyl formamide 储存条件 Store at -20°C
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1 mM 2.2512 mL 11.2562 mL 22.5124 mL
5 mM 0.4502 mL 2.2512 mL 4.5025 mL
10 mM 0.2251 mL 1.1256 mL 2.2512 mL
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