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

AR 231453 是有效的、特異性的、具有口服活性的 GPR119 激動(dòng)劑。AR 231453 可刺激細(xì)胞增殖，改善胰島 β 細(xì)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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規(guī)格 價(jià)格 是否有貨 數(shù)量
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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25 mg ￥1600
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50 mg ￥2240
In-stock
100 mg ￥3440
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200 mg   詢價(jià)  
500 mg   詢價(jià)  

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MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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].

細(xì)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]
體外研究
(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.
體內(nèi)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 號(hào)
性狀

固體

顏色

Light yellow to yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 25 mg/mL (49.45 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.70%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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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產(chǎn)品名稱：
AR 231453
目錄號(hào)：
HY-15564
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