Protosappanin A (PTA), an immune agent, is a major biphenyl compound isolated from Caesalpinia sappan L that inhibits the JAK2/STAT3-dependent inflammatory pathway by down-regulating the phosphorylation of JAK2 and STAT3.
|Solubility (25°C)||DMSO ≥ 200 mg/mL|
|Storage||4°C protect from light dry|
|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 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.
 Li-Xi Liao, et al. ACS Chem Neurosci. Protosappanin A Maintains Neuronal Mitochondrial Homeostasis through Promoting Autophagic Degradation of Bax
 Qiang Huang, et al. Int J Clin Exp Pathol. Protosappanin a inhibits osteoclastogenesis via reducing oxidative stress in RAW264.7 cells
 Jian Wu, et al. Pharmacol Res. Protosappanin A protects against experimental autoimmune myocarditis, and induces metabolically reprogrammed tolerogenic DCs
 Li-Chao Wang, et al. Chin J Nat Med. Protosappanin A exerts anti-neuroinflammatory effect by inhibiting JAK2-STAT3 pathway in lipopolysaccharide-induced BV2 microglia
 Jian Wu, et al. Naunyn Schmiedebergs Arch Pharmacol. Protosappanin A induces immunosuppression of rats heart transplantation targeting T cells in grafts via NF-kappaB pathway
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GDC046 (Compound 3) is a potent, selective, and orally bioavailable inhibitor of TYK2 with Ki of 4.8 nM, 83.8 nM, 27.6 nM and 253 nM for TYK2, JAK1, JAK2, and JAK3, respectively.
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