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Encequidar

Cat. No. M14249
Encequidar Structure
Synonym:

HM30181; HM30181A

Size Price Availability Quantity
5mg USD 118  USD118 In stock
10mg USD 172  USD172 In stock
50mg USD 520  USD520 In stock
100mg USD 800  USD800 In stock
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Quality Control & Documentation
Biological Activity

Encequidar (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein.

Chemical Information
Molecular Weight 688.73
CAS Number 849675-66-7
Solubility (25°C) DMSO 2.4 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] 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

[2] Wen Wee Ma, et al. A phase Ib study of Oraxol (oral paclitaxel and encequidar) in patients with advanced malignancies

[3] Christopher G C A Jackson, et al. Oral paclitaxel with encequidar compared to intravenous paclitaxel in patients with advanced cancer: A randomised crossover pharmacokinetic study

[4] Michael P Smolinski, et al. Discovery of Encequidar, First-in-Class Intestine Specific P-glycoprotein Inhibitor

[5] Dolly Sharma, et al. Cost of home vs clinic administration of paclitaxel in metastatic breast cancer

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


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