1. GPCR/G Protein Neuronal Signaling
  2. mGluR
  3. BMS-955829

BMS-955829 是一种口服有效和选择性的 mGluR5 阳性变构调节剂,EC50 为 2.6 nM。BMS-955829 无内在激动活性且谷氨酸折叠移位低 (2.4)。BMS-955829 能有效改善啮齿类动物的认知和执行功能缺陷。BMS-955829 可用于精神分裂症等认知障碍疾病的研究。

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BMS-955829

BMS-955829 Chemical Structure

CAS No. : 1375751-08-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BMS-955829 is an orally active and selective mGluR5 positive allosteric modulator with an EC50 of 2.6 nM. BMS-955829 has no intrinsic agonist activity and a low glutamate fold shift (2.4). BMS-955829 can effectively improve cognitive and executive function deficits in rodents. BMS-955829 can be used in the research of cognitive impairment diseases such as schizophrenia[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
2.6 nM
Compound: 12; BMS-955829
Positive allosteric modulation of human mGluR5A transfected in HEK293 cells assessed as potentiation of L-glutamate-induced calcium release incubated for 10 mins by FLIPR assay
Positive allosteric modulation of human mGluR5A transfected in HEK293 cells assessed as potentiation of L-glutamate-induced calcium release incubated for 10 mins by FLIPR assay
[PMID: 27496211]
HEK293 EC50
2.6 nM
Compound: 4; BMS-955829
Positive allosteric modulation of human mGlu5A receptor expressed in HEK293 cells coexpressing rat glutamate-aspartate transporter assessed as potentiation of L-glutamate-induced Ca2+ signal incubated for 60 mins by calcium 4 dye based FLIPR assay
Positive allosteric modulation of human mGlu5A receptor expressed in HEK293 cells coexpressing rat glutamate-aspartate transporter assessed as potentiation of L-glutamate-induced Ca2+ signal incubated for 60 mins by calcium 4 dye based FLIPR assay
[PMID: 26985317]
HEK293 EC50
> 30 μM
Compound: 4; BMS-955829
Agonist activity at human mGlu5A receptor expressed in HEK293 cells coexpressing rat glutamate-aspartate transporter assessed as induction of Ca2+ release by calcium 4 dye based FLIPR assay
Agonist activity at human mGlu5A receptor expressed in HEK293 cells coexpressing rat glutamate-aspartate transporter assessed as induction of Ca2+ release by calcium 4 dye based FLIPR assay
[PMID: 26985317]
HEK293 EC50
> 3000 nM
Compound: 12; BMS-955829
Agonist activity at human mGluR5A transfected in HEK293 cells assessed as induction of calcium release by FLIPR assay
Agonist activity at human mGluR5A transfected in HEK293 cells assessed as induction of calcium release by FLIPR assay
[PMID: 27496211]
HEK293 IC50
3 nM
Compound: BMS-955829
Displacement of [3H]-MethoxyPEPy from human mGlu5 receptor expressed in HEK293 cell membranes after 8 hrs by micro beta scintillation counting analysis
Displacement of [3H]-MethoxyPEPy from human mGlu5 receptor expressed in HEK293 cell membranes after 8 hrs by micro beta scintillation counting analysis
[PMID: 27994742]
分子量

376.36

Formula

C22H14F2N2O2

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
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  • 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.

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产品名称:
BMS-955829
目录号:
HY-120641
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