Acumapimod is an orally active p38 MAP kinase inhibitor, with an IC50 of less than 1 μM for p38α.
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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
p38 mitogen-activated protein kinases (p38 MAPK, p38) consist of 4 subunits: p38α, p38β, p38γ and p38δ. They play a well-recognized role in regulating intracellular signaling transduction in mammalian cells. p38 MAPK induces a variety of intracellular responses associated with neuropathic pain and other chronic pain[2]. Acumapimod（BCT197） is an orally active inhibitor of p38α MAPK (IC50 <1 μM). When examining BCT197 in vivo, and comparing to vehicle-treated animals, reduced weight loss, improvement in survival and lack of impaired viral control was observed at BCT197 concentrations relevant to those being used in clinical trials of acute exacerbations of chronic obstructive pulmonary disease; at higher concentrations of BCT197 these effects were reduced. BCT197 improved survival and weight loss compared to vehicle, but to a lesser degree than either oseltamivir or dexamethasone. It was also demonstrated that both dexamethasone and the higher dose of BCT197 increased viral load 7 days p.i. The lower dose of BCT197, which is more clinically relevant, remained comparable to vehicle treatment[3]. BCT197 was found to be a low clearance drug (1.76 L/h),with linearity in oral drug clearance (CL/F) demonstrated over the entire dose range tested (0.1–75 mg). No relevant differences in relative bioavailability between these formulations were seen. BCT197 exhibited an apparent absorption plateau, with a tendency to less than dose-proportional increase in peak drug concentration (Cmax)[4].
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