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Encequidar mesylate

Cat. No. M14250
Encequidar mesylate Structure
Synonym:

HM30181 mesylate; HM30181A mesylate

Size Price Availability Quantity
5mg USD 110  USD110 In stock
10mg USD 170  USD170 In stock
50mg USD 490  USD490 In stock
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Quality Control & Documentation
Biological Activity

Encequidar mesylate (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor.

Chemical Information
Molecular Weight 784.83
CAS Number 849675-87-2
Solubility (25°C) DMSO 25 mg/mL
Storage 2-8°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

References

[1] Patrick M Boland, et al. A dose regimen-finding study to evaluate the safety, tolerability, pharmacokinetics, and activity of oratecan in subjects with advanced malignancies

[2] Hope S Rugo, et al. Open-Label, Randomized, Multicenter, Phase III Study Comparing Oral Paclitaxel Plus Encequidar Versus Intravenous Paclitaxel in Patients With Metastatic Breast Cancer

[3] Jimmy He, et al. Population pharmacokinetics for oral paclitaxel in patients with advanced/metastatic solid tumors

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Keywords: Encequidar mesylate, HM30181 mesylate; HM30181A mesylate supplier, P-glycoprotein, inhibitors, activators


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