Chaperone-mediated autophagy (CMA) contributes to cellular quality control and the cellular response to stress through the selective degradation of cytosolic proteins in lysosomes. Decrease in CMA activity occurs in aging and in age-related disorders. Signaling through the retinoic acid receptor alpha (RARα) inhibits CMA. AR7, an RARα antagonist, significantly activates CMA activity in mouse fibroblasts. A marked increase in CMA-activating potency is found when AR7 and GR1 are combined, supporting their cooperative effect. Treatment with the transcriptional repressor Actinomycin D partially reduces the stimulatory effect of AR7 on CMA, consistent with transcriptional changes contributing to the upregulation of CMA
|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|
ABA-stimulated SoDOG1 expression is after-ripening inhibited during early imbibition of germinating Sisymbrium officinale seeds.
Carrillo-Barral N, et al. Physiol Plant. 2015 Dec;155(4):457-71. PMID: 26046653.
Effects of AR7 Joint Complex on arthralgia for patients with osteoarthritis: results of a three-month study in Shanghai, China.
Xie Q, et al. Nutr J. 2008 Oct 27;7:31. PMID: 18954461.
Humanized vascular endothelial growth factor (VEGF) antibody (bevacizumab; Avastin) is a highly effective monoclonal antibody against metastatic colorectal cancer and several other advanced late stage cancers.
MCC950 is a potent, selective NLRP3 inhibitor with IC50 of 7.5 nM and 8.1 nM in BMDMs and HMDMs, respectively.
MAK683, an epigenetic drug for nasopharyngeal carcinoma, which is more prevalent in China than elsewhere, has entered Phase I clinical trials.
MTX-211 is a enamide hydrate.
GSK369796 shows antimalerial activity with IC50 values of 11.2 nM for 3D7 strain, 12.6 nM for HB3 strain, 17.6 nM for K1 strain.
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