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GPR35 agonist 4 

Cat. No. M30771
GPR35 agonist 4  Structure
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Biological Activity

GPR35 agonist 4 (compound 10) is a potent GPR35 agonist with an pEC50 of 5.86. GPR35 agonist 4 shows high potency human and rat GPR35. Mutation of arginine 3.36 eliminates agonist function of GPR35 agonist 4.

Chemical Information
Molecular Weight 279.27
Formula C12H9NO5S
CAS Number 871085-49-3
Form Solid
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Di Wang, et al. Acta Pharm Sin B. Functional metabolomics reveal the role of AHR/GPR35 mediated kynurenic acid gradient sensing in chemotherapy-induced intestinal damage

[2] Dominik Thimm, et al. J Med Chem. 6-Bromo-8-(4-[(3)H]methoxybenzamido)-4-oxo-4H-chromene-2-carboxylic Acid: a powerful tool for studying orphan G protein-coupled receptor GPR35

[3] Haibei Hu, et al. PLoS One. Label-free phenotypic profiling identified D-luciferin as a GPR35 agonist

[4] Huayun Deng, et al. J Med Chem. Discovery of 2-(4-methylfuran-2(5H)-ylidene)malononitrile and thieno[3,2-b]thiophene-2-carboxylic acid derivatives as G protein-coupled receptor 35 (GPR35) agonists

[5] Yasuhito Taniguchi, et al. Pharmacology. 5-Nitro-2-(3-phenylpropylamino)benzoic acid is a GPR35 agonist

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