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EC5026 (BPN-19186)

Cat. No. M10464
EC5026 (BPN-19186) Structure
Synonym:

BPN-19186

Size Price Availability Quantity
5mg USD 85  USD85 In stock
10mg USD 140  USD140 In stock
50mg USD 420  USD420 In stock
100mg USD 700  USD700 In stock
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Quality Control & Documentation
Biological Activity

EC5026 (BPN-19186) is a first-in-class, potent and orally active soluble inhibitor of Epoxide Hydrolase (sEH). EC5026 has the potential to relieve pain by stabilizing natural analgesic and anti-inflammatory mediators. In vivo, EC5026 (BPN-19186) has already shown efficacy for treating pain with no apparent adverse or addictive effects in laboratory animals and relieving naturally occurring pain in dogs, cats and horses.

Chemical Information
Molecular Weight 405.39
Formula C18H23F4N3O3
CAS Number 1809885-32-2
Form Solid
Solubility (25°C) DMSO ≥ 100 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] Sandra Codony, et al. J Med Chem. From the Design to the In Vivo Evaluation of Benzohomoadamantane-Derived Soluble Epoxide Hydrolase Inhibitors for the Treatment of Acute Pancreatitis

[2] Bruce D Hammock, et al. J Med Chem. Movement to the Clinic of Soluble Epoxide Hydrolase Inhibitor EC5026 as an Analgesic for Neuropathic Pain and for Use as a Nonaddictive Opioid Alternative

Related Epoxide Hydrolase Products
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UC-1728

UC-1728 is a potent rabbit soluble epoxide hydrolase (sEH) inhibitor, with an IC50 of 2 nM on rabbit liver.

BI-1935 

BI-1935 is a potent soluble epoxide hydrolase (sEH) inhibitor. BI-1935 can be used for the research of cardiovascular disease.

AR-9281

AR9281 (APAU) is a potent, selective and orally active soluble epoxide hydrolase (s-EH) inhibitor. AR-9281 can inhibits human sEH (HsEH) and murine sEH (MsEH) with IC50 values of 13.8 nM and 1.7 nM, respectively. AR9281 can be used for the research of inflammation, hypertension and type 2 diabetes.

SWE101 

SWE101 (compound 22 b) is a potent soluble epoxide hydrolase (sEH)-P inhibitor with IC50s of 4 μM and 2.8 μM for human and rat sEH-P, respectively. SWE101 does not inhibit neither hydrolase nor phosphatase activity of the mouse sEH.

  Catalog
Abmole Inhibitor Catalog




Keywords: EC5026 (BPN-19186), BPN-19186 supplier, Epoxide Hydrolase, inhibitors, activators


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