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Referencia número: HY-120641

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BMS-955829

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.

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No. CAS: 1375751-08-8
Fòrmula: C₂₂H₁₄F₂N₂O₂
Peso molecular:376.36

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Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

BMS-955829 Chemical Structure

No. CAS: 1375751-08-8

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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Descripciòn

Ver todos los productos específicos de isoformas mGluR :

Cellular Effect

Cell Line	Type	Value	Description	References
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	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	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]

Chemical Information

No. CAS 1375751-08-8
Peso molecular 376.36
Fòrmula C₂₂H₁₄F₂N₂O₂
SMILES

O=C1O[C@H](C2=CC(F)=CC=C2F)[C@@H](C3=CC(C#CC4=CC=CC=C4)=CN=C3)N1
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Yang F, et al. Discovery and Preclinical Evaluation of BMS-955829, a Potent Positive Allosteric Modulator of mGluR5. ACS Med Chem Lett. 2016 Jan 4;7(3):289-93. [Content Brief]

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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BMS-955829

Ver todos los productos específicos de isoformas mGluR

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BMS-955829 Related Classifications

HY-120641 Related Classifications