2. GPCR/G Protein
  3. Free Fatty Acid Receptor
  4. AM-3189

AM-3189 是一种口服有效且有选择性的 GPR40 激动剂，其在缓冲液和在 100% 人血清中的 EC50 值分别为 33 nM 和 10 μM。AM-3189 对 GPR41 和 GPR43 无显著活性，对 PPAR-α、-δ 和 -γ 无激动活性。AM-3189 通过激活胰腺 β 细胞上的 GPR40，增强葡萄糖刺激的胰岛素分泌。AM-3189 具有极低的中枢神经系统渗透性，在两种人源化 GPR40 小鼠模型中显著降低了血糖水平。AM-3189 可用于研究 2 型糖尿病。

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AM-3189

AM-3189 Chemical Structure

CAS No. : 916219-50-6

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AM-3189 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AM-3189 is an orally active and selective GPR40 agonist with EC50 values in buffer solution and in 100% human serum of 33 nM and 10 μM respectively. AM-3189 shows no significant activity on GPR41 and GPR43, and no agonistic activity on PPAR-α, -δ, and -γ. AM-3189 enhances glucose-stimulated insulin secretion by activating GPR40 on pancreatic β cells. AM-3189 has extremely low penetration into the central nervous system and significantly reduces blood glucose levels in two humanized GPR40 mouse models. AM-3189 can be used for the study of type 2 diabetes[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A9 EC50
7.6 nM
Compound: 4
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
Agonist activity at human GPR40 expressed in mouse A9 cells by inositol phosphate accumulation assay
[PMID: 24900872]
CHO EC50
0.033 μM
Compound: 13k; AM-3189
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 0.01% human serum albumin
[PMID: 26620255]
CHO EC50
10 μM
Compound: 13k; AM-3189
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
Partial agonist activity at human GPR40 expressed in CHO cells measured over 20 secs interval by luminometric analysis in presence of 100% human serum
[PMID: 26620255]
CHO EC50
33 nM
Compound: 4
Agonist activity at human GPR40 expressed in CHO cells by aequorin assay
Agonist activity at human GPR40 expressed in CHO cells by aequorin assay
[PMID: 24900872]
分子量

460.95

Formula

C27H25ClN2O3
CAS 号
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.
纯度 & 产品资料
参考文献

AM-3189 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

AM-3189916219-50-6AM3189AM 3189Free Fatty Acid ReceptorFFARtype 2 diabetesinsulin secretagoguepharmacokineticsCNS penetrationInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-111141
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