Daidzein is an inactive analogue of genistein, a tyrosine kinase inhibitor and an estrogen receptor activator.
|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||10 mM in DMSO|
Daidzein stimulates collagen synthesis by activating the TGF-β/smad signal pathway.
Zhao D, et al. Australas J Dermatol. 2015 Feb;56(1):e7-14. PMID: 24645968.
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Benzamide is an inhibitor of poly(ADP-ribose) polymerase with an IC50 of 3.3 μM.
Picolinamide is a strong inhibitor of poly (ADP-ribose) synthetase of nuclei from rat pancreatic islet cells.
|Niraparib (MK-4827) tosylate
Niraparib (MK-4827) tosylate is an excellent PARP1 and PARP2 inhibitor with IC50 of 3.8 and 2.1 nM, respectively.
NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles, showing 150-fold selectivity for PARP-1 over PARP-2 (Kd 0.009 μM vs 1.39 μM, respectively).
E7449 is an orally bioavailable, brain penetrable, small molecule dual inhibitor of PARP1/2 that also inhibits PARP5a/5b, otherwise known as tankyrase1 and 2 (TNKS1/2), important regulators of canonical Wnt/β-catenin signaling. It has IC50 values of 1.0 and 1.2 nM for PARP1 and 2, respectively.
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