Isonaringin shows anti-Alzheimer’s activity by inhibiting AChE[1].
分子量
580.53
Formula
C27H32O14
CAS 号
108815-81-2
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.
参考文献
[1]. Liu C, et al. Extraction and isolation of acetylcholinesterase inhibitors from Citrus limon peel using an in vitro method. J Sep Sci. 2020;43(8):1531-1543.
Acarbose;(Synonyms: 阿卡波糖; BAY g 5421) 纯度: ge;98.0%
Acarbose (BAY g 5421),降糖药,是一种具有口服活性 α-葡萄糖苷酶 (alpha-glucosidase) 抑制剂 (IC50=11 nM)。Acarbose 能增强磺脲类药物或胰岛素的降血糖作用。
Acarbose Chemical Structure
CAS No. : 56180-94-0
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生物活性
Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin[1][2][3].
体外研究 (In Vitro)
Acarbose (1, 2, and 3 μM) dose- and time-dependently inhibits TNF-α-induced VSMC proliferation and migration. Acarbose (1, 2, and 3 μM) dose-dependently decreases β-galactosidase, Ras expression and increased p-AMPK expression in TNF-α pre-treated A7r5 cells[5].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Acarbose (300 mg/60 kg body weight) decreases the fasting blood glucose, and regulates the glucose tolerance of DM rats without body weight loss. Acarbose significantly suppresses serum IL6 and TNF-α in DM rats[4]. Acarbose (2.5 and 5.0 mg/kg) significantly and dose-dependently decreases the intensity of neointimal IL-6, TNF-α, and iNOS staining, and significantly increases the intensity of neointimal p-AMPK staining. Acarbose (2.5 and 5.0 mg/kg) significantly and dose-dependently decreases neointimal Ras and β-galactosidase expression in HCD-fed rabbits without body weight loss[5].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量
645.60
Formula
C25H43NO18
CAS 号
56180-94-0
中文名称
阿卡波糖
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Yee HS, et al. A review of the safety and efficacy of acarbose in diabetes mellitus. Pharmacotherapy. 1996;16(5):792-805.
[2]. Hanefeld M, et al. Acarbose: oral anti-diabetes drug with additional cardiovascular benefits [published correction appears in Expert Rev Cardiovasc Ther. 2009 Mar;7(3):330]. Expert Rev Cardiovasc Ther. 2008;6(2):153-163.
[3]. Oki T, et al. Evaluation of alpha-glucosidase inhibition by using an immobilized assay system. Biol Pharm Bull. 2000;23(9):1084-1087.
[4]. Zhang Q, et al. Acarbose Reduces Blood Glucose by Activating miR-10a-5p and miR-664 in Diabetic Rats. PLoS One. 2013 Nov 18;8(11):e79697.
[5]. Chan KC, et al. Pleiotropic effects of acarbose on atherosclerosis development in rabbits are mediated via upregulating AMPK signals. Sci Rep. 2016 Dec 7;6:3864
Cell Assay [2]
Cell viability is determined using the MTT assay. Cells are seeded in 24-well culture plates at a density of 2×104 cells/well, incubated for 48 h, treated with acarbose at varying concentrations (0.5, 1.0, 2.0, 3.0, and 5.0 μM) for 24 h; or pre-treated with TNF-α (20 ng/mL) for either 24 h or 48 h to evaluate the dose-dependent effects of acarbose on VSMC growth and viability, cultured with 0.5 mg/mL MTT at 37°C in a humidified atmosphere of 5% CO2 for another 4 h, and solubilized with isopropanol. The viable cell number varies directly with the concentration of formazan product measured spectrophotometrically at 563 nm.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [2]
Twenty-four male New Zealand white rabbits, weighing 2500 g are used. They are individually housed in metal cages in an air-conditioned room (22 ± 2°C, 55 ± 5% humidity), under a 12 h light/12 h dark cycle with free access to food and water. All rabbits are randomLy assigned to four groups of 6 animals each and are fed either standard chow (Group I), high cholesterol diet (HCD; containing 95.7% standard Purina chow + 3% lard oil + 0.5% cholesterol) (Group II), HCD diet and 2.5 mg/kg per day acarbose (Group III), or HCD diet and 5.0 mg/kg per day acarbose (Group IV). At the end of the 25 weeks, all rabbits are sacrificed by exsanguination under deep anesthesia with pentobarbital (30 mg/kg i.v.) injected via the marginal ear vein. Serum is stored at −80°C prior to measurement of serum values. The aortic arch and thoracic aortas are carefully removed to protect the endothelial lining, and are collected and freed of adhering soft tissue.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Yee HS, et al. A review of the safety and efficacy of acarbose in diabetes mellitus. Pharmacotherapy. 1996;16(5):792-805.
[2]. Hanefeld M, et al. Acarbose: oral anti-diabetes drug with additional cardiovascular benefits [published correction appears in Expert Rev Cardiovasc Ther. 2009 Mar;7(3):330]. Expert Rev Cardiovasc Ther. 2008;6(2):153-163.
[3]. Oki T, et al. Evaluation of alpha-glucosidase inhibition by using an immobilized assay system. Biol Pharm Bull. 2000;23(9):1084-1087.
[4]. Zhang Q, et al. Acarbose Reduces Blood Glucose by Activating miR-10a-5p and miR-664 in Diabetic Rats. PLoS One. 2013 Nov 18;8(11):e79697.
[5]. Chan KC, et al. Pleiotropic effects of acarbose on atherosclerosis development in rabbits are mediated via upregulating AMPK signals. Sci Rep. 2016 Dec 7;6:3864
1-Naphthaleneacetic acid (1-Naphthylacetic acid), a synthetic auxin, can promote plant growth. 1-Naphthaleneacetic acid is also an inhibitor of PLA2, with an IC50 of 13.16 μM[1][2].
IC50 Target[1]
PLA2
13.16 mu;M (IC50)
体外研究 (In Vitro)
1-Naphthaleneacetic acid (0.7-14 μM) inhibits the activity of PLA2, with the Ki and IC50 of 6.87 μM and 13.16 μM, respectively[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
186.21
Formula
C12H10O2
CAS 号
86-87-3
中文名称
1-萘乙酸;α-萘乙酸;1-萘基乙酸;α-萘醋酸; 萘乙酸
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Dileep KV, et, al. Crystal structure of phospholipase A 2 in complex with 1-naphthaleneacetic acid. IUBMB Life. 2018 Oct;70(10):995-1001.
[2]. Gómez DA, et al. Effect of 1-naphthaleneacetic acid on organic acid exudation by the roots of white lupin plants grown under phosphorus-deficient conditions. J Plant Physiol. 2014 Sep 15;171(15):1354-61.
Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 antagonist with an IC50 vakue of ~1 nM.
IC50 Target[1]
CXCR4
~1 nM (IC50)
体外研究 (In Vitro)
Motixafortide (BKT140) displays selective toxicity toward AmL and MM cells. Treatment with Motixafortide (BKT140) can overcome IL-6 dependent proliferation and survival of ARH77 MM cells. Motixafortide (BKT140) specifically triggers CXCR4-dependent cell death in leukemia and MM cells. Motixafortide (BKT140) stimulates apoptotic cell death in leukemia and MM cells[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Subcutaneous injections of Motixafortide (BKT140) significantly reduces, in a dose-dependent manner, the growth of human acute myeloid leukemia and multiple myeloma xenografts. Tumors from animals treated with Motixafortide (BKT140) are smaller in size and weights, had larger necrotic areas and high apoptotic scores[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Solubility: 110 mg/mL (50.94 mM); Clear solution; Need ultrasonic
*以上所有助溶剂都可在 MCE 网站选购。
参考文献
[1]. Peled A, et al. The high-affinity CXCR4 antagonist BKT140 is safe and induces a robust mobilization of human CD34+ cellsin patients with multiple myeloma. Clin Cancer Res. 2014 Jan 15;20(2):469-79.
[2]. Beider K, et al. CXCR4 antagonist 4F-benzoyl-TN14003 inhibits leukemia and multiple myeloma tumor growth. Exp Hematol. 2011 Mar;39(3):282-92.
Cell Assay [2]
Hematopoietic cancer cells are incubated with different concentrations of Motixafortide (BKT140) or AMD3100 for 24 hours. Motixafortide (BKT140) is treated with 1M hydrochloric acid (HCL) to achieve a pH of 2.7 to 3 at room temperature for 30 minutes and the pH is adjusted to 7 using concentrated NaOH. Proteinase K is added to Motixafortide (BKT140) at a final concentration of 100 mg/mL, incubated at 37°C for 1 hour, and inactivated by heat treatment (65°C for 30 minutes). After incubation, cells are stained with propidium iodide and the percent of viable PI-negative cells in culture is determined[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration [2]
Mice: Severe combined immune-deficient (SCID)/beige mice (C.B-17/IcrHsd-SCID-bg) are used in the study. NB4 cells resuspended in PBS are injected subcutaneously into the flanks of the mice (200 μL per mouse containing 5×106 cells). Tumor growth is monitored daily, and mice are randomized to drug-treated or control PBS-treated groups (10 mice per group) when the tumor size (width×length) reaches 0.04 cm2. BKT140 is administered subcutaneously at a dose of 200 μg per mouse each day for 5 days[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Peled A, et al. The high-affinity CXCR4 antagonist BKT140 is safe and induces a robust mobilization of human CD34+ cellsin patients with multiple myeloma. Clin Cancer Res. 2014 Jan 15;20(2):469-79.
[2]. Beider K, et al. CXCR4 antagonist 4F-benzoyl-TN14003 inhibits leukemia and multiple myeloma tumor growth. Exp Hematol. 2011 Mar;39(3):282-92.
Bromobimane is essentially nonfluorescent and converts into fluorescent products when reacts with small thiols.
体外研究 (In Vitro)
Bromobimanes in solution (aqueous or organic solvents of medium polarity) react with small thiols [e.g., the tripeptide thiol glutathione (GSH)], and with reactive protein thiol groups (e.g., hemoglobin). The reactions of bromobimanes with thiols are second order and dependent on pH, the active nucleophile being the thiolate anion. The reaction of bromobimane with a thiolate converts the nonfluorescent agent into water-soluble fluorescent products. The neutral agents mBBr and bBBr are moderately soluble in mediumpolarity organic solvents (acetonitrile, dichloromethane), and slightly soluble in water. The quaternary salt, qBBr, and the anionic bromobimane, SBBr, are soluble in water, but less soluble in organic solvents. Bromobimanes are yellow[1]. The highly selective, rapid reactivity of bromobimanes toward thiols, the stability and fluorescence yield of the thiol derivatives, the ease of separation of the derivatives by reversed-phase HPLC, and the availability of both cell-penetrating and nonpenetrating forms, make the use bromobimanes an extremely powerful approach to the analysis of low molecular weight biothiols[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
271.11
Formula
C10H11BrN2O2
CAS 号
71418-44-5
中文名称
溴二胺;单溴二胺
运输条件
Room temperature in continental US; may vary elsewhere.
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 MCE 网站选购。
参考文献
[1]. Kosower EM, et al. Bromobimane probes for thiols. Methods Enzymol. 1995;251:133-48.
[2]. Newton GL, et al. Determination of biothiols by bromobimane labeling and high-performance liquid chromatography. Methods Enzymol. 1995;251:148-66.
Cell Assay [2]
The stock mBBr solution is prepared by weight at 100-180 mM in acetonitrile. The stock solution of SBBr is prepared by weight at 50 mM in dimethyl sulfoxide (DMSO) or at 2 mM in the 20 mM Tris-methane sulfonate. The thiol is added to a final concentration of 1 mM to a solution of 2 mM mBBr or SBBr, 20 mM Tris-methane sulfonate, pH 8.0. The mixture is incubated in the dark for 15 min at room temperature and then methanesulfonic acid is added to 25 mM from a 5 M stock solution[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Kosower EM, et al. Bromobimane probes for thiols. Methods Enzymol. 1995;251:133-48.
[2]. Newton GL, et al. Determination of biothiols by bromobimane labeling and high-performance liquid chromatography. Methods Enzymol. 1995;251:148-66.
DAB (3,3′ Diaminobenzidine Tetrahydrochloride) 是有机化合物,具有化学和热力学稳定性,可用于核酸和蛋白的免疫组化染色。
DAB Chemical Structure
CAS No. : 7411-49-6
规格
价格
是否有货
数量
500 mg
¥400
In-stock
1 g
¥650
In-stock
5 g
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询价
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10 g
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* Please select Quantity before adding items.
生物活性
DAB (3,3′ Diaminobenzidine Tetrahydrochloride) is an organic compound that is both chemically and thermodynamically stable; DAB has been used in immunohistochemical staining of nucleic acids and proteins.
分子量
360.11
Formula
C12H18Cl4N4
CAS 号
7411-49-6
运输条件
Room temperature in continental US; may vary elsewhere.
Magnolin, a major component of Magnolia flos (Shin-Yi), inhibits the Ras/ERKs/RSK2 signaling axis by targeting the active pocket of ERK1 and ERK2 with IC50s of 87 nM and 16.5 nM, respectively.
IC50 & Target[1]
ERK2
16.5 nM (IC50)
ERK1
87 nM (IC50)
体外研究 (In Vitro)
Magnolin is a natural compound abundantly found in Magnolia flos, which has been traditionally used in oriental medicine to treat headaches, nasal congestion and anti-inflammatory reactions. Magnolin targets the active pockets of ERK1 and ERK2, which are important signaling molecules in cancer cell metastasis. Magnolin inhibits NF-κB transactivation activity by suppressing the ERKs/RSK2 signaling pathway. Magnolin inhibits the production of tumor necrosis factor-α (TNF-α) and prostaglandin E2 (PGE2) by inhibiting extracellular signal-regulated kinases (ERKs), which are key signaling molecules in the regulation of cell proliferation, transformation and cancer cell metastasis. JB6 Cl41 cell migration enhanced by EGF treatment is dramatically suppressed by Magnolin treatment in a dose-dependent manner. Magnolin inhibits ERK1/2/RSK2 signaling-mediated IκBα phosphorylation at Ser32, resulting in the inhibition of NF-κB activation and cell migration[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
416.46
Formula
C23H28O7
CAS 号
31008-18-1
中文名称
木兰苷
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Lee CJ, et al. Magnolin inhibits cell migration and invasion by targeting the ERKs/RSK2 signaling pathway. BMC Cancer. 2015 Aug 8;15:576.
Cell Assay [1]
JB6 Cl41 (7×104), A549 (7×104) and NCI-H1975 (7×104) cells, and RSK2+/+ (7×104) and RSK2-/- (7×104) MEFs are seeded into culture-inserts and cultured overnight. The cells are treated with mitomycin-C (10 μg/mL) for 2 h, and the culture-inserts are removed to offer a cell-free gap. The cells are treated with the indicated doses of Magnolin (15, 30, and 60 μM) either in the presence or absence of EGF for 12 or 24 h, and cell migration is observed under a light microscope. The migrated area is measured using the Image J computer software program. To measure the Magnolin effect on cancer cell invasion, a matrigel-coated invasion chamber is used. Briefly, A549 or NCI-H1975 (2.5×104) cells are seeded into an insert chamber with FBS-free media supplemented with the indicated doses of Magnolin(15, 30, and 60 μM), and cultured in 24-well plates supplemented with complete media for the appropriate time period. The cells are fixed with 4 % formaldehyde, permeabilized with methanol and stained with crystal violet. The stained cells are observed under a light microscope and those that have migrated are counted[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[1]. Lee CJ, et al. Magnolin inhibits cell migration and invasion by targeting the ERKs/RSK2 signaling pathway. BMC Cancer. 2015 Aug 8;15:576.