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Hexamethonium Bromide

SKU: orb1224665

Description

Hexamethonium Bromide is a selective antagonist of neuronal-type nicotinic AChR in ganglia.(In Vitro):Pemetrexed (LY231514) disodium is a novel classical antifolate, the antitumor activity of which may result from simultaneous and multipie inhibition of several key folate-requiring enzymes via its polyglutamated metabolites. Pemetrexed (LY231514) is one of the best substrates that is known for the enzyme FPGS (Km=1.6 μM and Vmax/Km=621). It is likely that polyglutamation and the polyglutamated metabolites of LY231514 play profound roles in determining both the selectivity and the antitumor activity of this novel agent. Whereas LY23l5l4 only moderately inhibits TS (Ki=340 nM, recombinant mouse), the pentaglutamate of LY23l5l4 is 100-fold more potent (Ki=3.4 nM), making LY231514 one of the most potent folate-based TS inhibitors.(In Vivo):The group of mice treated with PC61 plus Pemetrexed demonstrates statistically longer survival than other groups. In a survival analysis, significantly better survival is observed in the group of mice treated with PC61 plus Pemetrexed compare with those treated with PC61 alone, rat IgG plus Pemetrexed, or no treatment.

Images & Validation

Key Properties

CAS Number55-97-0
MW362.19
Purity>98% (HPLC)
FormulaC12H30Br2N2
SMILESC[N+](CCCCCC[N+](C)(C)C)(C)C.[Br-].[Br-]
TargetAChR
SolubilityWater: 73 mg/mL (201.55 mM)

Bioactivity

In Vivo
Hexamethonium Bromide (0.2-25 mg/kg; i. v.) significantly reduces therenal sympathetic nerve activity (RSNA), mean arterial pressure (MAP) and heart rate (HR) in the Wistar rats and the spontaneously hypertensive rats (SHRs). Hexamethonium Bromide (0.2-1.0 mg/kg; i. v.) treatments show no significant differences in the RSNA, MAP or HR between Wistar rats and SHRs. Hexamethonium Bromide (5.0-25 mg/kg; i. v.) results in a greater reduction in the RSNA and MAP in SHRs compared with Wistar rats. Animal model: Male normotensive Wistar rats (280-320 g), SHRs. Dosage: 0.2 mg/kg, 1.0 mg/kg, 5.0 mg/kg, 25 mg/kg. Administration: Intravenous injection. Result: Significantly reduced the RSNA, MAP and HR in the Wistar rats and the SHRs.
In Vitro
Hexamethonium Bromide (100 μM; 60 minutes) abolishes epibatidine-induced depolarisations of smooth muscle cells. The α3β4α5 receptors have greater sensitivity to Hexamethonium Bromide than the other potential ganglionic models, α3β4, α3β2, and α3β2α5.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Hexamethionium bromide | Esametina | Simpatoblock | Vegolysen

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Hexamethonium Bromide (orb1224665)

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1 g
$ 80.00
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