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Genipin Sale

(Synonyms: 京尼平; (+)-Genipin) 目录号 : GN10116

An inhibitor of UCP2 activity

Genipin Chemical Structure

Cas No.:6902-77-8

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥673.00
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50mg
¥612.00
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100mg
¥910.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Kinase experiment:

Briefly, the peptide substrate N-acetyl-Asp-Glu-Val-Asp-ρ-nitroanilide (Ac-DEVD-ρNA) is added to the cell lysates in assay buffer (50 mM HEPES, pH 7.4, 100 mM NaCl, 0.1% CHAPS, 10 mM dithiothreitol, 1 mM EDTA, 10% glycerol) and incubated at 37°C. The cleavage of the substrate is monitored at 405 nm.

References:

[1]. Ma C, et al. Genipin stimulates glucose transport in C2C12 myotubes via IRS-1 and calcium- dependent mechanism. J Endocrinol. 2012 Dec 20.
[2]. Parton LE, et al. Glucose sensing by POMC neurons regulates glucose homeostasis and is impaired in obesity. Nature. 2007 Sep 13;449(7159):228-32.
[3]. Kim BC, et al. Genipin-induced apoptosis in hepatoma cells is mediated by reactive oxygen species/c-Jun NH2-terminal kinase-dependent activation of mitochondrial pathway. Biochem Pharmacol. 2005 Nov 1;70(9):1398-407.
[4]. Ye D, et al. Genipin normalizes depression-like behavior induced by prenatal stress through inhibiting DNMT1. Epigenetics. 2018 Mar 9:1-22.

产品描述

IC50: 88.41 M for hepatitis C virus

Genipin, a compound derived from Gardenia jasminoides Ellis fruits, has been used over the years in traditional Chinese medicine to treat symptoms of type 2 diabetes.

In vitro: Previous study indicated genipin could stimulate the glucose uptake in a time- and dose-dependent manner. Genipin promoted glucose transporter 4 translocation to the cell surface in myotubes. Moreover, in the cytoplasm in C2C12 myotubes, genipin increased ATP levels, then shut down KATP channels, and finally increased the calcium concentration. In addition, genipin-stimulated glucose uptake could be blocked by wortmannin and calcium chelator EGTA, two PI3-K inhibitors. Furthermore, in C2C12 myotubes, genipin increased the level of reactive oxygen species and ATP [1].

In vivo: In rat liver after infusion of genipin, the biliary secretion of Mrp2 substrates, the subcellular localization, and mRNA level of Mrp2 were assessed. Results showed that in the CMVs, genipin treatment increased the protein mass of Mrp2 but not the mRNA level. Such effects were not observed in Mrp2-deficient rats. In addition, a marked increase in Mrp2 density in the canalicular membrane and microvilli was observed in the genipin-treated liver tissue sections [2].

Clinical trial: N/A

References:
[1] Ma CJ,Nie AF,Zhang ZJ,Zhang ZG,Du L,Li XY,Ning G.  Genipin stimulates glucose transport in C2C12 myotubes via an IRS-1 and calcium-dependent mechanism. J Endocrinol.2013 Feb 25;216(3):353-62.
[2] Shoda J,Miura T,Utsunomiya H,Oda K,Yamamoto M,Kano M,Ikegami T,Tanaka N,Akita H,Ito K,Suzuki H,Sugiyama Y.  Genipin enhances Mrp2 (Abcc2)-mediated bile formation and organic anion transport in rat liver. Hepatology.2004 Jan;39(1):167-78.

Chemical Properties

Cas No. 6902-77-8 SDF
别名 京尼平; (+)-Genipin
化学名 methyl (1R,4aS,7aS)-1-hydroxy-7-(hydroxymethyl)-1,4a,5,7a-tetrahydrocyclopenta[c]pyran-4-carboxylate
Canonical SMILES COC(=O)C1=COC(C2C1CC=C2CO)O
分子式 C11H14O5 分子量 226.23
溶解度 ≥ 9.8 mg/mL in DMSO, ≥ 101.6 mg/mL in EtOH, ≥ 5.97 mg/mL in Water 储存条件 4°C, protect from light
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 4.4203 mL 22.1014 mL 44.2028 mL
5 mM 0.8841 mL 4.4203 mL 8.8406 mL
10 mM 0.442 mL 2.2101 mL 4.4203 mL
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