TC-SP 14 is a potent and selective S1P1 agonist (EC50 values are 0.042 and 3.47 μM for human S1P1 and S1P3 respectively). Attenuates immune response to antigen challenge and reduces circulating blood lymphocyte counts in a rodent model of delayed-type hypersensitivity. Orally bioavailable.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 22.52 mg/mL (with gentle warming)|
The preclinical pharmacology of "Arimidex" (anastrozole; ZD1033)-a potent, selective aromatase inhibitor.
Dukes, et al. J Steroid Biochem Mol Biol. 1996;58: 439. PMID: 8903429.
|Related GPCR19/TGR5 Products|
|TGR5 Receptor Agonist
TGR5 Receptor Agonist is a potent TGR5(GPCR19) agonist which showed improved potency in the U2-OS cell assay (pEC50 = 6.8) and in melanophore cells (pEC50 = 7.5).
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