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H4R antagonist 3

Cat. No. M41848
H4R antagonist 3 Structure
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Biological Activity

H4R antagonist 3 is a histamine-4 receptor antagonist with an EC50 of <10 mM.

Chemical Information
Molecular Weight 372.91
Formula C19H21ClN4S
CAS Number 1003091-20-0
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] Shuying Zhou et al. Dermatology. Biological Therapies for Atopic Dermatitis: A Systematic Review

[2] Hsiangkuo Yuan et al. Headache. Histamine and Migraine

[3] Gomathi Nagarajan et al. J Recept Signal Transduct Res. Effect of H4R antagonist N-(2-aminoethyl)-5-chloro-1H-indol-2-carboxamides and 5-chloro-2-(piperazin-1-ylmethyl)-1H-benzimidazole on histamine and 4-methylhistamine-induced mast cell response

[4] Huaqing Liu et al. J Med Chem. cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia

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