AR420626 - CAS:1798310-55-0

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AR420626

目录号 : KCM12065 CAS No. : 1798310-55-0 纯度 : ≥95%

Data Sheet 产品使用指南

Free fatty acid receptor 3 (FFAR3; GPR41) is a G protein-coupled receptor activated by short chain fatty acids (SCFAs). It is expressed in adipose tissue, the gastrointestinal tract, and the peripheral nervous system, and it is involved in SCFA-dependent energy regulation. AR420626 is a selective agonist of FFAR3 (GPR41; IC = 117 nM) that does not activate the related receptor FFAR2 (GPR43) at concentrations up to 100 µM. At 10 µM, it can stimulate a 1.26-fold increased release of glucagon-like peptide-1 from colonic crypt cultures.

规格	价格	是否有货	数量
1mg		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock
50mg		In-stock
10 mM * 1 mL in DMSO		In-stock

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生物活性

AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3) (IC50=117 nM). AR420626 has anti-inflammatory, anticancer and antidiabetic activities. AR420626 improves neurogenic diarrhea by inhibiting nAChR mediated neural pathways. AR420626 inhibits the growth of HepG2 xenografts and inhibits the proliferation of hepatoma cells by inducing apoptosis. AR420626 also suppresses allergic asthma and eczema and has the ability to activate GPR41 to increase Ca2+ signal-mediated glucose uptake and improve diabetes[1][2][3].

体外研究

AR420626 (10 μM) can inhibit the contraction of rat proximal colon circular muscle strips induced by 100 μM nicotine and the relaxation of rat proximal colon circular muscle strips induced by 10 μM nicotine [1].
AR420626 (10 μM) reversed NO mediated cyclic muscle relaxation induced by Serotonin (100 μM) [1].
AR420626 (10 and 25 µM; 48 h) inhibited the proliferation of HLE and HepG2 cells at a concentration of 25 µM for 48 h, and induced apoptosis of HepG2 and HLE cells by inhibiting HDAC induced TNF - α [2].
AR420626 (25 µM; 1, 3, 12, and 24 h) induced mTOR phosphorylation in HepG2 cells and HLE cells 1 hour after administration and continued for 24 hours [2].
AR420626 (0.25, 0.5, and 1 µM; 1 h) increases Ca2+influx and GLUT4 translocation by activating CaMKII, CREB, and p38 in C2C12 myotubes, thereby increasing basal and insulin stimulated glucose uptake.

Cell Proliferation Assay

Cell Line:

HepG2 cells and HLE cells

Concentration:

10, 25 µM

Incubation Time:

24, 48 and 72 h

Result:

Inhibited the proliferation of HepG2 cells at 25 µM for 24 h, 10 µM and 25 µM for 48 h and 72 h, and inhibited the proliferation of HLE cells at 25 µM for 48 h, 10 µM and 25 µM for 72 h.

Western Blot Analysis

Cell Line:

HCC cells

Concentration:

10, 25 µM

Incubation Time:

48 h

Result:

Increased the expression of cleaved caspase-3 in a dose-dependent manner.
Increased cleaved caspase-8 in HCC cells in a dose-dependent manner and slightly increased cleaved caspase-9 in HepG2 cells at 25 µM.

Western Blot Analysis

Cell Line:

HCC cells

Concentration:

25 µM

Incubation Time:

1, 3, 12 and 24 h

Result:

Reduced the levels of HDAC 4-7 at 1 h and gradually decreased to 24h, reduced the levels of HDAC 1-3 at 24h, and reduced the levels of HDAC8 at 1h and gradually decreased to 24h in HepG2 cells.
Upregulated histone H3 acetylation level at 3 h and gradually increased to 24 h in HepG2 cells.

RT-PCR

Cell Line:

HCC cells

Concentration:

10, 25 µM

Incubation Time:

1, 3, 12 and 24 h

Result:

Increased the TNF-α mRNA level in HepG2 cells from 1 to 24 hours, reaching a peak at around 24 hours at a dose of 25µM, the TNF-α mRNA level in HLE cells from 1 to 24 hours was dose-dependent, reaching a peak at around 3 hours.

体内研究

AR420626 (0.1 mg/kg; intraperitoneal injection, single dose injection) can significantly inhibit serotonin induced defecation in male Sprague Dawley rats [1].
AR420626 (0.1 mg/kg, intraperitoneal injection; Day 0-4; 0.2 mg/kg, Intraperitoneal injection; On days 7-11, the growth of male SHO nude mice transplanted with HepG2 was inhibited.
AR420626 (0.1 mg/kg, intraperitoneal injection; Administration of modeling agent 30 minutes before induction inhibited the immune response in bronchoalveolar lavage fluid (BALF) of BALB/c mice induced by Ovalbumins and suppressed the immune response in lung tissue; And inhibit the skin inflammatory immune response, cervical lymph node immune response, and development of eczema symptoms induced by 1-chloro-2,4-dinitrobenzene (DNCB) in BALB/c mice.
AR420626 (13.32 and 26.64 μ g/kg, intraperitoneal injection; Once a day for 7 days) at a dose of 26.64 μ g/kg, the plasma insulin level and skeletal muscle glycogen content of male ICR mice with Streptozotocin induced diabetes and C57BL/6 mice with high fat diet induced diabetes were increased to improve glucose tolerance.

Animal Model:	HepG2 xenograft model in male SHO nude mice
Dosage:	0.1 mg/kg on days 0-4 after tumors reach 500-1000 mm³ 0.2 mg/kg on days 7-11 after tumors reach 500-1000 mm³
Administration:	Intraperitoneal injection (i.p.)
Result:	Inhibited the growth of HepG2 xenograft mice, and still had an inhibitory effect on the weight of mice after stopping administration.

Animal Model:	Ovalbumin (OVA)-induced asthma induction in BALB/c mice
Dosage:	0.1 mg/kg
Administration:	Intraperitoneal injection 30 min before OVA sensitization (D0 and D14) or 30 min before OVA challenge (D28, D29, and D30)
Result:	Suppressed the increased IL-4 and IL-17A levels. Suppressed the increase in the number of eosinophils and total immune cells in bronchoalveolar lavage fluid (BALF). Inhibited the increase of cytokine (IL-4, IL-13, IFN-γ and IL-17a) levels.

Animal Model:	1-chloro-2, 4-dinitrobenzene (DNCB)-induced eczema model in BALB/c mice
Dosage:	0.1 mg/kg
Administration:	Intraperitoneal injection 30 min before the DNCB challenge from day 19
Result:	Reduced the number of accumulated immune cells and mast cells, inhibited acanthosis and epidermal thickening and mast cell accumulation, and inhibited IL-17A, TSLP and IL-8 levels. Inhibited immune responses in the cervical lymph nodes, size enlargement, and expression of inflammatory cytokines and chemokines, but did not enhance the proportion of CD4+FoxP3+ Treg cells.

分子式

C₂₁H₁₈Cl₂N₂O₃

分子量

417.3

CAS号

1798310-55-0

中文名称

AR420626

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 20 mg/mL (47.93 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3964 mL	11.9821 mL	23.9641 mL
5 mM	0.4793 mL	2.3964 mL	4.7928 mL
10 mM	0.2396 mL	1.1982 mL	2.3964 mL

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂：10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: 2 mg/mL (4.79 mM); Suspended solution; Need ultrasonic

此方案可获得 2 mg/mL (4.79 mM) 的均匀悬浊液，悬浊液可⽤于⼝服和腹腔注射。

以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2.

请依序添加每种溶剂：10% DMSO → 90% corn oil

Solubility: ≥ 2 mg/mL (4.79 mM); Clear solution

此方案可获得 ≥ 2 mg/mL (4.79 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。