1. GPCR/G Protein Neuronal Signaling
  2. GPR119
  3. AR 231453

AR 231453 是有效的、特异性的、具有口服活性的 GPR119 激动剂。AR 231453 可刺激细胞增殖,改善胰岛 β 细胞的功能。

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AR 231453 Chemical Structure

AR 231453 Chemical Structure

CAS No. : 733750-99-7

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Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ¥712
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5 mg ¥640
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10 mg ¥960
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50 mg ¥2240
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100 mg ¥3440
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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AR 231453 is a potent, specific and orally available GPR119 agonist. AR 231453 can stimulate β-cell replication and improve islet graft function s[1][2].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
0.003 mM
Compound: 1, AR231453
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
[PMID: 24751443]
HEK293 EC50
0.7 μM
Compound: 2; AR231453
Agonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assay
Agonist activity at CREB-LBD and GAL4-DBD fused human GPR119 expressed in HEK293 cells by luciferase reporter gene assay
[PMID: 27560285]
HEK293 EC50
4.78 nM
Compound: AR231543
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
Agonist activity at recombinant human GPR119 expressed in HEK293 cells after 24 hrs by steady-glo luciferase assay
[PMID: 31630858]
体外研究
(In Vitro)

AR 231453 is inactive at all other GPCRs tested (more than 230, including all known pancreatic islet receptors), indicating that it is highly selective for GPR119[1].
AR 231453 potently stimulats cAMP accumulation (EC50 = 4.7 nM) with a maximal efficacy similar to that seen with forskolin. AR 231453 significantly enhancesinsulin release in HIT-T15 cells, with an EC50 of 3.5 nM[1].
AR 231453 also stimulates insulin release in isolated mouse islets at glucose concentrations ranging from 8-17 mM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

AR231453 (20 mg/kg, orally) markedly improves oral glucose tolerance in a dose-dependent fashion, with efficacy similar to maximally effective doses of the sulfonylurea glyburide[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mice[1].
Dosage: 20 mg/kg.
Administration: Orally, once.
Result: Improved glucose tolerance in mice.
分子量

505.52

Formula

C21H24FN7O5S

CAS 号
性状

固体

颜色

Light yellow to yellow

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 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 25 mg/mL (49.45 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9782 mL 9.8908 mL 19.7816 mL
5 mM 0.3956 mL 1.9782 mL 3.9563 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.70%

参考文献

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9782 mL 9.8908 mL 19.7816 mL 49.4540 mL
5 mM 0.3956 mL 1.9782 mL 3.9563 mL 9.8908 mL
10 mM 0.1978 mL 0.9891 mL 1.9782 mL 4.9454 mL
15 mM 0.1319 mL 0.6594 mL 1.3188 mL 3.2969 mL
20 mM 0.0989 mL 0.4945 mL 0.9891 mL 2.4727 mL
25 mM 0.0791 mL 0.3956 mL 0.7913 mL 1.9782 mL
30 mM 0.0659 mL 0.3297 mL 0.6594 mL 1.6485 mL
40 mM 0.0495 mL 0.2473 mL 0.4945 mL 1.2364 mL
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.

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产品名称:
AR 231453
目录号:
HY-15564
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