BRS-3 receptor agonist-2

Cat. No.: HY-W681071: Fiche technique Instruction de manipulation
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BRS-3 receptor agonist-2 (compound 2) is a potent BRS-3 receptor agonist, with an EC₅₀ of 2.5 nM for mouse BRS-3 receptor.

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BRS-3 receptor agonist-2 Chemical Structure

CAS No. : 1021937-07-4

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Activité biologique
Pureté et documentation
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Description

BRS-3 receptor agonist-2 (compound 2) is a potent BRS-3 receptor agonist, with an EC₅₀ of 2.5 nM for mouse BRS-3 receptor^[1].

IC₅₀ & Target

EC50: 2.5 nM (mouse BRS-3 receptor)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	18 nM Compound: 9	Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting	[PMID: 20219372]
CHO	IC₅₀	2.4 nM Compound: 9	Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from rat BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from rat BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting	[PMID: 20219372]
CHO	IC₅₀	6.9 nM Compound: 9	Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from mouse BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from mouse BRS-3 expressed in NFAT-CHO cells after 2 hrs by scintillation counting	[PMID: 20219372]
CHO	IC₅₀	6400 nM Compound: 9	Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human GRP-R expressed in NFAT-CHO cells after 2 hrs by scintillation counting Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human GRP-R expressed in NFAT-CHO cells after 2 hrs by scintillation counting	[PMID: 20219372]
CHO	IC₅₀	7000 nM Compound: 9	Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human NMB-R expressed in NFAT-CHO cells after 2 hrs by scintillation counting Displacement of [125I]D-Tyr6-betaAla11-Phe13-Nle14-bombesin from human NMB-R expressed in NFAT-CHO cells after 2 hrs by scintillation counting	[PMID: 20219372]
HEK293	EC₅₀	2.8 nM Compound: 9	Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay	[PMID: 20219372]
HEK293	EC₅₀	47 nM Compound: 9	Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay	[PMID: 20219372]
HEK293	EC₅₀	78 nM Compound: 9	Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin Agonist activity at mouse BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin	[PMID: 20219372]
HEK293	EC₅₀	99 nM Compound: 9	Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin Agonist activity at human BRS-3 expressed in HEK293 cells coexpressing AEQ over 10 mins by aequorin bioluminescence assay relative to D-Tyr6-betaAla11-Phe13-Nle14-bombesin	[PMID: 20219372]

Masse moléculaire

333.47

Formule

C₂₂H₂₇N₃

CAS No.

1021937-07-4

SMILES

CCC(C)(CC1=CN=C(N1)CCC2=CC=C(C3=NC=CC=C3)C=C2)C

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Chobanian HR, et, al. Discovery of MK-7725, A Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity. ACS Med Chem Lett. 2012 Jan 21;3(3):252-6. [Content Brief]