2. Neuronal Signaling Anti-infection
  3. Amyloid-β HIV
  4. Carbenoxolone

Carbenoxolone 是甘草次酸的半合成衍生物，由于其抗炎特性，被广泛用于消化不良和消化性溃疡的治疗。 Carbenoxolone，半通道和间隙连接蛋白抑制剂，具有治疗慢性肝病的治疗潜力 Carbenoxolone 抑制 Aβ42 聚集，是抗 AD 治疗潜力的合适候选者 Carbenoxolone 是小分子 Pannexin1 (Panx1，是一种 ATP 释放通道) 抑制剂，通过调节第一个细胞外环来减弱 Panx1 通道活性。 Carbenoxolone 是 11β-羟基类固醇脱氢酶 1 型 (11β-HSD1) 抑制剂。 Carbenoxolone 具有抗 DENV 感染的抗病毒活性，靶点针对病毒本身。

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Carbenoxolone

Carbenoxolone Chemical Structure

CAS No. : 5697-56-3

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规格 是否有货
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100 mg   询价  
250 mg   询价  

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Carbenoxolone 的其他形式现货产品:

Other Forms of Carbenoxolone:

Carbenoxolone 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Carbenoxolone, a semi-synthetic derivative of glycyrrhetinic acid, has previously been used for the management of dyspepsia and peptic ulcer because of its anti-inflammatory properties[3]. Carbenoxolone, a general hemichannel and gap junction inhibitor, has the therapeutic potential of carbenoxolone in the treatment of chronic liver disease[2]. Carbenoxolone is a suitable candidate for the inhibition of Aβ42 aggregation and the therapeutic potential of Cbx against AD[1]. Carbenoxolone is small molecule Pannexin1 (Panx1,is an ATP release channel) inhibitor, attenuate Panx1 channel activity through modulation of the first extracellular loop[4]. Carbenoxolone is an 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor[5]. Carbenoxolone has antiviral activity against DENV infection targeting the virus itself[6].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
3T3-L1 EC50
> 500 μM
Compound: 4; CBX
Cytotoxicity against mouse 3T3L1 cells measured after 72 hrs by celltiter-glo luminescent cell viability assay
Cytotoxicity against mouse 3T3L1 cells measured after 72 hrs by celltiter-glo luminescent cell viability assay
[PMID: 31294974]
CHO IC50
0.5 μM
Compound: Carbenoxolone
Inhibition of human 11beta-HSD1 expressed in CHO cells after 3 hrs by HTRF cortisol assay
Inhibition of human 11beta-HSD1 expressed in CHO cells after 3 hrs by HTRF cortisol assay
[PMID: 21093259]
CHO IC50
250 nM
Compound: Carbenoxolone
Inhibition of mouse 11beta-HSD1 expressed in CHO cells after 3 hrs by HTRF cortisol assay
Inhibition of mouse 11beta-HSD1 expressed in CHO cells after 3 hrs by HTRF cortisol assay
[PMID: 21093259]
CHO-K1 IC50
0.5 μM
Compound: carbenoxolone
Inhibition of human 11beta-HSD1 expressed in CHO-K1 cells using cortisone as substrate after 3 hrs by HTRF assay
Inhibition of human 11beta-HSD1 expressed in CHO-K1 cells using cortisone as substrate after 3 hrs by HTRF assay
[PMID: 24900439]
CHO-K1 IC50
1630 nM
Compound: Carbenoxolone
Inhibition of human 11beta-HSD1 expressed in CHOK1 cells using XL665-labeled cortisol as substrate measured after 24 hrs by HTRF assay
Inhibition of human 11beta-HSD1 expressed in CHOK1 cells using XL665-labeled cortisol as substrate measured after 24 hrs by HTRF assay
[PMID: 31759849]
CHO-K1 IC50
243 nM
Compound: Carbenoxolone
Inhibition of mouse 11beta-HSD1 expressed in CHOK1 cells using XL665-labeled cortisol as substrate measured after 24 hrs by HTRF assay
Inhibition of mouse 11beta-HSD1 expressed in CHOK1 cells using XL665-labeled cortisol as substrate measured after 24 hrs by HTRF assay
[PMID: 31759849]
HEK293 EC50
82 nM
Compound: Carbenoxolone
Inhibition of mouse 11beta-HSD2 expressed in HEK293 cells assessed as [3H]cortisol production after 60 mins by SPA
Inhibition of mouse 11beta-HSD2 expressed in HEK293 cells assessed as [3H]cortisol production after 60 mins by SPA
[PMID: 22440625]
HEK293 IC50
0.17 μM
Compound: 4; CBX
Inhibition of 11beta-HSD2 (unknown origin) expressed in HEK293 cells using cortisone as substrate measured after 2 hrs in presence of NAD+ by HTRF assay
Inhibition of 11beta-HSD2 (unknown origin) expressed in HEK293 cells using cortisone as substrate measured after 2 hrs in presence of NAD+ by HTRF assay
[PMID: 31294974]
HEK293 IC50
206 nM
Compound: carbenoxolone
Inhibition of mouse 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay
Inhibition of mouse 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay
[PMID: 22360639]
HEK293 IC50
82 nM
Compound: carbenoxolone
Inhibition of mouse microsomal 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay
Inhibition of mouse microsomal 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay
[PMID: 19564108]
RAW264.7 IC50
11.42 μM
Compound: Carbenoxolone
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of HMGB1-induced NO production pretreated with compounds for 15 mins followed by HMGB1 stimulation measured after 24 hrs by Griess reagent based assay
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of HMGB1-induced NO production pretreated with compounds for 15 mins followed by HMGB1 stimulation measured after 24 hrs by Griess reagent based assay
[PMID: 34800877]
RAW264.7 IC50
6.64 μM
Compound: Carbenoxolone
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production
[PMID: 34973341]
RAW264.7 IC50
7.62 μM
Compound: Carbenoxolone
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of HMGB1-induced NO production
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of HMGB1-induced NO production
[PMID: 34973341]
分子量

570.76

Formula

C34H50O7
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

Carbenoxolone 相关分类

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Help & FAQs
  • 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.

Keywords:

Carbenoxolone5697-56-3Amyloid-βHIVβ-amyloid peptideAβAbetaHuman immunodeficiency virusInhibitorinhibitorinhibit

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