4-CMTB
目录号 : GC17149
4-CMTB是一种选择性的游离脂肪酸受体2（FFA2/GPR43）激动剂和正变构调节剂。
Cas No.:300851-67-6
Sample solution is provided at 25 µL, 10mM.
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4-CMTB is a selective free fatty acid receptor 2 (FFA2/GPR43) agonist and a positive allosteric modulator[1]. FFA2, also known as GPR43, is a G protein-coupled receptor activated by short-chain fatty acids that plays key roles in metabolism, immune regulation, and inflammatory responses[2]. 4-CMTB is usually used to study the mechanism of action of FFA2 receptors in inflammatory diseases, including asthma, colorectal cancer, intestinal ischemia-reperfusion injury, as well as metabolic diseases such as type 2 diabetes, obesity and insulin resistance[3][4].
In vitro, 4-CMTB (25μM; 48h) reduced cell viability, decreased cell migration and invasion, increased FFAR2/FFAR4 gene expression, yet decreased their protein levels in SW-480 cells[5].
In vivo, 4-CMTB (20mg/kg; i.p.; 30min before OVA challenge) inhibited OVA-induced immune cell accumulation in BALF and reduced mucin production in ovalbumin-induced allergic asthma BALB/c mice[6]. 4-CMTB (10mg/kg; i.p.; administered 30min before DNCB challenge) reversed DNCB-induced atopic dermatitis in BALB/c mice, suppressed ear epidermal hypertrophy, and reduced mast cell infiltration, serum IgE elevation and IL-4/IL-13 expression[7].
References:
[1] Smith NJ, Ward RJ, Stoddart LA, et al. Extracellular loop 2 of the free fatty acid receptor 2 mediates allosterism of a phenylacetamide ago-allosteric modulator. Mol Pharmacol. 2011;80(1):163-173.
[2] Bindels LB, Dewulf EM, Delzenne NM. GPR43/FFA2: physiopathological relevance and therapeutic prospects. Trends Pharmacol Sci. 2013;34(4):226-232.
[3] Brown AJ, Tsoulou C, Ward E, et al. Pharmacological properties of acid N-thiazolylamide FFA2 agonists. Pharmacol Res Perspect. 2015;3(3):e00141.
[4] Lorza-Gil E, Kaiser G, Rexen Ulven E, et al. FFA2-, but not FFA3-agonists inhibit GSIS of human pseudoislets: a comparative study with mouse islets and rat INS-1E cells. Sci Rep. 2020;10(1):16497.
[5] Binienda A, Owczarek K, Sałaga M, Fichna J. Synthetic free fatty acid receptor (FFAR) 2 agonist 4-CMTB and FFAR4 agonist GSK13764 inhibit colon cancer cell growth and migration and regulate FFARs expression in in vitro and in vivo models of colorectal cancer. Pharmacol Rep. 2024;76(6):1403-1414.
[6] Lee JH, Im DS. 4-CMTB Ameliorates Ovalbumin-Induced Allergic Asthma through FFA2 Activation in Mice. Biomol Ther (Seoul). 2021;29(4):427-433.
[7] Kang J, Im DS. FFA2 Activation Ameliorates 2,4-Dinitrochlorobenzene-Induced Atopic Dermatitis in Mice. Biomol Ther (Seoul). 2020;28(3):267-271.
4-CMTB是一种选择性的游离脂肪酸受体2（FFA2/GPR43）激动剂和正变构调节剂[1]。FFA2，也称为GPR43，是一种由短链脂肪酸激活的G蛋白偶联受体，在代谢、免疫调节和炎症反应中发挥关键作用[2]。4-CMTB通常用于研究FFA2受体在炎症性疾病（包括哮喘、结直肠癌、肠缺血再灌注损伤）以及2型糖尿病、肥胖和胰岛素抵抗等代谢性疾病中的作用机制[3][4]。
体外实验中，4-CMTB（25μM；48小时）降低了SW-480细胞的活力，抑制细胞迁移和侵袭，增加FFAR2/FFAR4基因表达，但降低了它们的蛋白水平[5]。
体内实验中，4-CMTB（20mg/kg；腹腔注射；OVA刺激前30分钟）抑制了卵清蛋白诱导的过敏性哮喘BALB/c小鼠的BALF中免疫细胞积聚，并减少了黏蛋白的产生[6]。4-CMTB（10mg/kg；腹腔注射；DNCB刺激前30分钟给药）逆转了DNCB诱导的BALB/c小鼠特应性皮炎，抑制了耳部表皮增生，并减少了肥大细胞浸润、血清IgE升高以及IL-4/IL-13的表达[7]。
| Cell experiment [1]: | |
Cell lines | Human colorectal adenocarcinoma cell line SW-480 |
Preparation Method | Human colorectal adenocarcinoma cell line, SW-480 (CCL-228) were cultured in RPMI media supplemented with 10% fetal bovine serum (FBS), 2mM L-glutamine, 50U/mL penicillin, and 50µg/mL streptomycin. The cells were cultured in a humidified atmosphere of 5% CO2 at 37℃. All experiments were carried out between passages 5 to 15. Seeding quantities were such that the confluence of the control wells did not exceed 80% at the end of the experiment. Cells were seeded on a 96-well plate at the density of 6,000cells/well and incubated for 24h. Then, cells were incubated with 4-CMTB (25µM) for 48h. MTT assay was used to measure the cytotoxicity. Matrigel BM matrix assay was used for measuring the capacity of cancer cells to motility. And cells were collected for qPCR and western blot analyses. |
Reaction Conditions | 25μM; 48h |
Applications | 4-CMTB reduced cell viability, decreased cell migration and invasion, increased FFAR2/FFAR4 gene expression, yet decreased their protein levels in SW-480 cells. |
| Animal experiment [2]: | |
Animal models | Female five-week-old BALB/c mice |
Preparation Method | Female five-week-old BALB/c mice were housed in the laboratory animal facility provided ad libitum water and food. Mice (22g) were randomly divided into four groups (n=5): phosphate-buffered saline (PBS)-injected control group, ovalbumin (OVA)-injected asthma group, OVA-injected and 10mg/kg 4-CMTB-treated group, and OVA-injected and 20mg/kg 4-CMTB-treated group. Asthma was induced by intraperitoneal injection of OVA and aluminum hydroxide on D0 and D14. Mice were challenged by exposing to nebulized OVA for D28, D29, and D30. 4-CMTB was dissolved in DMSO as a stock solution of 100mM. The stock was diluted in corn oil (50μL) just before the experiment. 4-CMTB was treated via intraperitoneal injection 30min before OVA challenge. We collected bronchoalveolar lavage fluid (BALF) from the lungs on D32, and cell population of BALF cells was analyzed after staining. Tissue sections of lungs from mice of each group were prepared for histological examination. |
Dosage form | 10 or 20mg/kg; i.p.; 30min before OVA challenge |
Applications | 4-CMTB inhibited OVA-induced immune cell accumulation and reduced mucin production in ovalbumin-induced allergic asthma BALB/c mice. |
References: | |
| Cas No. | 300851-67-6 | SDF | |
| 化学名 | (R)-2-(4-chlorophenyl)-3-methyl-N-(thiazol-2-yl)butanamide | ||
| Canonical SMILES | ClC1=CC=C(C=C1)[C@H](C(NC2=NC=CS2)=O)C(C)C | ||
| 分子式 | C14H15ClN2OS | 分子量 | 294.8 |
| 溶解度 | <29.48mg/ml in DMSO; <5.9mg/ml in ethanol | 储存条件 | Store at -20°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3921 mL | 16.9607 mL | 33.9213 mL |
| 5 mM | 678.4 μL | 3.3921 mL | 6.7843 mL |
| 10 mM | 339.2 μL | 1.6961 mL | 3.3921 mL |
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动物平均体重 | g | |
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动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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- Purity: >99.00%
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