17 alpha-Estradiol is a 5α-reductase inhibitor, and it inhibits testosterone metabolism catalyzed by 5 alpha-reductase. Alpha-Estradiol (17 Alpha-estradiol, 10 μM) attenuates LPS-induced inflammatory markers in both C57BL/6J male and female mouse embryonic fibroblast (MEF) cells, primary pre-adipocytes and differentiated 3T3-L1 adipocytes in an ERα-dependent manner, and such effects are through decreased NFκB-p65 and increased ERα protein expression. Alpha-Estradiol (17-alpha-estradiol, 0.01, 0.1, 1 μg) significantly reduces the percentage of central avascular/total retina area of the mouse pups.
|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.
|Solubility||DMSO ≥ 60 mg/mL|
Garcinone E is the most active xanthone from mangosteen, which has potent cytotoxic effect against hepatocellular carcinoma cell lines. Garcinone E might inhibit metastasis of an oral cancer cell line by blocking invasion, migration and MMP production.
GRP-60367 hydrochloride is a first-in-class potent and selective inhibitor of rabies virus (RABV) entry that specifically targets the RABV G protein.
ML382 is a potent and selective MrgX1 (Mas-related G protein-coupled receptor X1, MRGPRX1) positive allosteric modulator with EC50 of 190 nM.
Enpp-1-IN-1, also known as MV 658, is a Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1) inhibitor.
GW280264X is an ADAM17 inhibitor.
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