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HCAR2 agonist 1

Cat. No. M43061
HCAR2 agonist 1 Structure
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Biological Activity

HCAR2 agonist 1 is a Gi protein-biased allosteric modulator of HCAR2.

Chemical Information
Molecular Weight 428.53
Formula C26H28N4O2
CAS Number 1066676-21-8
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] Xin Pan et al. Cell Discov. Structural insights into ligand recognition and selectivity of the human hydroxycarboxylic acid receptor HCAR2

[2] Chunyou Mao et al. Nat Commun. Orthosteric and allosteric modulation of human HCAR2 signaling complex

[3] Lin Cheng et al. Signal Transduct Target Ther. Orthosteric ligand selectivity and allosteric probe dependence at Hydroxycarboxylic acid receptor HCAR2

[4] Michela Perrone et al. Neuropharmacology. Potential role of the hydroxyl carboxylic acid receptor type 2 (HCAR2) in microglia pathophysiology: A possible cross-talk with C-X-C chemokine receptor 1 (CXCR1)

[5] Nagendra Singh et al. Immunity. Activation of Gpr109a, receptor for niacin and the commensal metabolite butyrate, suppresses colonic inflammation and carcinogenesis

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