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SB 203580 hydrochloride

Cat. No. M7249
SB 203580 hydrochloride Structure
Synonym:

Adezmapimod hydrochloride ; RWJ 64809 hydrochloride

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Biological Activity

SB 203580 hydrochloride is a water-soluble salt of SB 203580. Selective inhibitor of p38 mitogen-activated protein kinase (IC50 values are 50 and 500 nM for SAPK2a/p38 and SAPK2b/p38β2 respectively). Displays 100-500-fold selectivity over LCK, GSK3β and PKBα. Shown to inhibit interleukin-2-induced T cell proliferation, cyclooxygenase-1 and -2, and thromboxane synthase.

Chemical Information
Molecular Weight 413.89
Formula C21H16FN3OS.HCl
CAS Number 869185-85-3
Solubility (25°C) Water 10.35 mg/mL (with gentle warming)
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] Coleman, et al. Br J Pharmacol. Comparison of the actions of U-46619, a prostaglandin H2-analogue, with those of prostaglandin H2 and thromboxane A2 on some isolated smooth muscle preparations.

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  Catalog
Abmole Inhibitor Catalog




Keywords: SB 203580 hydrochloride, Adezmapimod hydrochloride ; RWJ 64809 hydrochloride supplier, p38 MAPK, inhibitors, activators


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