1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Anti-infection Apoptosis NF-κB Metabolic Enzyme/Protease
  2. Histamine Receptor Parasite MDM-2/p53 NF-κB FOXO Bacterial
  3. Conessine dihydrobromide

Conessine dihydrobromide 是一种口服有效且能透过血脑屏障的选择性组胺 H3 受体拮抗剂。Conessine dihydrobromide 对大鼠和人 H3 受体的 pKi 为 7.61 和 8.27。Conessine dihydrobromide 是 Pseudomonas aeruginosa 中多药物外排泵系统的抑制剂,可增强抗生素的活性。Conessine dihydrobromide 具有抗疟疾活性。Conessine dihydrobromide 也可用于肌肉萎缩的研究。

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Conessine dihydrobromide Chemical Structure

Conessine dihydrobromide Chemical Structure

CAS No. : 5913-82-6

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Conessine dihydrobromide 的其他形式现货产品:

Other Forms of Conessine dihydrobromide:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Conessine dihydrobromide is an orally active and BBB-penetrable selective histamine H3 receptor antagonist. The pKi values of Conessine dihydrobromide for rat and human H3 receptors are 7.61 and 8.27, respectively. Conessine dihydrobromide is an inhibitor of the multidrug efflux pump system in Pseudomonas aeruginosa and can enhance the activity of antibiotics. Conessine dihydrobromide has antimalarial activity. Conessine dihydrobromide can also be used in the research of muscle atrophy[1][2][3][4][5].

体外研究
(In Vitro)

Conessine (2.5-20 μM; 24 h) dihydrobromide 在 HEK293 细胞中,可抑制 p53、NF-κB 和 FoxO3a 依赖的转录[1]
Conessine (10 μM) dihydrobromide 在 Dexamethasone (HY-14648) 处理的 C2C12 肌管细胞中,降低了 MuRF1 和 atrogin-1 水平[1]
Conessine (72 h) dihydrobromide 具有抗疟原虫活性,在裂殖体成熟法和 pLDH 测定法中的 IC50 分别为 1.9 和 1.3 μg/mL[2]
Conessine (74 h) dihydrobromide 对 L-6 细胞具有透毒性,IC50 为 14 μg/mL[2]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Conessine (10-50 mg/kg; 口服; 4 天) dihydrobromide 显著降低感染 P. berghei 小鼠的寄生虫血症[2]
Conessine (0.1-10 mg/kg; 皮下注射; 单剂量) dihydrobromide 能在小鼠中加剧乙醇诱导的精神刺激作用[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c mice aged 4-6 weeks old (22-26 g) were infected with Plasmodium berghei[2]
Dosage: 10, 20 and 50 mg/kg
Administration: Oral administration; 4 days
Result: Significantly reduced parasitaemia in infected mice. The parasite inhibition rates were 88.95% at 10 mg/kg, 56.6% at 20 mg/kg, and 50.99% at 50 mg/kg on day 7. The mean survival time of mice in the 10 mg/kg group was 13.3 days, in the 20 mg/kg group was 11.6 days, and in the 50 mg/kg group was 11.5 days.
Affected the liver and kidney function of mice, as shown by the changes in the levels of alkaline phosphatase (ALP), bilirubin, urea, and creatinine in serum.
Animal Model: Male Swiss mice (30-35 g) treated ethanol[3]
Dosage: 0.1, 1 and 10 mg/kg
Administration: Subcutaneously; single dose
Result: Exacerbated ethanol effects on locomotor activity in a dose-dependent manner.
Had reinforcing proprieties per se in the conditionedplace preference (CPP) procedure at dose of 10 mg/kg, but it did not alter the acquisition of ethanol CPP.
Blocked ethanol effects on dopaminergic and noradrenergic neurotransmission.
分子量

518.41

Formula

C24H42Br2N2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Conessine dihydrobromide
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HY-107566A
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