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BTRX-335140

Cat. No. M21654
BTRX-335140 Structure
Synonym:

CYM-53093

Size Price Availability Quantity
5mg USD 340  USD340 In stock
10mg USD 640  USD640 In stock
25mg USD 1040  USD1040 In stock
50mg USD 1980  USD1980 In stock
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Quality Control & Documentation
Biological Activity

BTRX-335140 is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats.

Orally administered BTRX-335140 (CYM-53093) showed robust efficacy in antagonizing KOR agonist-induced prolactin secretion and in tail-flick analgesia in mice.

Chemical Information
Molecular Weight 453.55
Formula C25H32FN5O2
CAS Number 2244614-14-8
Solubility (25°C) DMSO ≥ 10 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] Tanya L Wallace, et al. Neurobiol Stress. Kappa opioid receptor antagonism protects working memory performance from mild stress exposure in Rhesus macaques

[2] Elyssa B Margolis, et al. PLoS One. Differential effects of novel kappa opioid receptor antagonists on dopamine neurons using acute brain slice electrophysiology

[3] Miguel Guerrero, et al. J Med Chem. Design and Synthesis of a Novel and Selective Kappa Opioid Receptor (KOR) Antagonist (BTRX-335140)

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  Catalog
Abmole Inhibitor Catalog




Keywords: BTRX-335140, CYM-53093 supplier, Opioid Receptor, inhibitors, activators


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