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STEARDA

Cat. No. M7335
STEARDA Structure
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Biological Activity

STEARDA is a endogenous fatty acid dopamide that displays 'entourage' effects on endovanilloids NADA and anandamide. Inactive at TRPV1 and CB1 receptors (at concentrations up to 5 μM) and does not inhibit AMT or FAAH (IC50 > 25 μM). However, potentiates TRPV1-mediated effects of NADA in vitro and in vivo; enhances effects on intracellular Ca2+ (EC50 lowered 3-fold) and nociception. Also inhibits arachidonate 5-lipoxygenase (IC50 = 16 nM).

Chemical Information
Molecular Weight 419.64
Formula C26H45NO3
CAS Number 105955-10-0
Solubility (25°C) ethanol 2.1 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] Chan, et al. Biochem Biophys Res Commun. Identification of a new class of ETA selective endothelin antagonists by pharmacophore directed screening.

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