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Cat. No.: HY-W1058476

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GPR35 agonist 6

GPR35 agonist 6 is a potent and selective agonist targeting GPR35, with an EC₅₀ of 12.1 nM against human GPR35. GPR35 agonist 6 activates the human splice variant GPR35b with comparable efficacy, showing an EC₅₀ of 22.1 nM. GPR35 agonist 6 also exhibits weak GPR55 antagonistic activity, with an IC₅₀ of 21.7 μM, and its agonistic activity towards GPR35 is significantly stronger than its antagonistic activity towards GPR55. GPR35 agonist 6 initiates GPR35 downstream signaling by inducing β-arrestin recruitment. GPR35 agonist 6 is used to investigate GPR35-mediated diseases, such as gastrointestinal lesions and gastric cancer.

For research use only. We do not sell to patients.

CAS No.: 1443367-20-1
Formula: C₁₈H₁₂BrNO₆
Molecular Weight:418.20

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

GPR35 agonist 6 Chemical Structure

CAS No.: 1443367-20-1

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

Biological Activity
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- In Vitro
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Biological Activity

Description

All Arrestin Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	21.7 μM Compound: 85	Antagonist activity at human GPR55 expressed in CHO cells assessed as inhibition of lysophosphotidylinositol-induced beta-arrestin recruitment preincubated for 30 mins followed by lysophosphotidylinositol induction by beta-galactosidase reporter gene assa Antagonist activity at human GPR55 expressed in CHO cells assessed as inhibition of lysophosphotidylinositol-induced beta-arrestin recruitment preincubated for 30 mins followed by lysophosphotidylinositol induction by beta-galactosidase reporter gene assa	[PMID: 23713606]
CHO	EC₅₀	0.0221 μM Compound: 85	Agonist activity at human GPR35b expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay Agonist activity at human GPR35b expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay	[PMID: 23713606]
CHO	EC₅₀	1.4 μM Compound: 85	Agonist activity at rat GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay Agonist activity at rat GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay	[PMID: 23713606]
CHO	EC₅₀	0.0121 μM Compound: 85	Agonist activity at human GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay Agonist activity at human GPR35 expressed in CHO cells assessed as induction of beta-arrestin recruitment after 90 mins by beta-galactosidase reporter gene assay	[PMID: 23713606]

In Vitro

GPR35 agonist 6 (Compound 85) potently activates human GPR35 in CHO cells with an EC₅₀ of 12.1 nM; it activates human GPR35b in CHO cells with an EC₅₀ of 22.1 nM; and it activates rat GPR35 in CHO cells with an EC₅₀ of 1.40 μM^[1].
GPR35 agonist 6 exhibits extremely weak activation of murine GPR35 in CHO cells at a concentration of 10 μM, indicating that its potency is lower than that of human GPR35^[1].
GPR35 agonist 6 exhibits no agonistic activity against human GPR55, but acts as a weak antagonist with an IC₅₀ of 21.7 μM, and shows over 1700-fold higher selectivity for human GPR35 over GPR55^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 1443367-20-1
Molecular Weight 418.20
Formula C₁₈H₁₂BrNO₆
SMILES

O=C(O)C=1OC=2C(=CC(Br)=CC2C(=O)C1)NC(=O)C3=CC=C(OC)C=C3
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Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Funke M, et al. 8-Benzamidochromen-4-one-2-carboxylic acids: potent and selective agonists for the orphan G protein-coupled receptor GPR35. Journal of medicinal chemistry. 2013 Jun 27;56(12):5182-97. [Content Brief]

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Help & FAQs

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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