1. GPCR/G Protein
    Neuronal Signaling
  2. Opioid Receptor
  3. BTRX-335140

BTRX-335140 (Synonyms: CYM-53093)

Cat. No.: HY-124754 Purity: 98.33%
Handling Instructions

BTRX-335140 (CYM-53093) is a potent and selective, 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. BTRX-335140 endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. BTRX-335140 can distribute well into the CNS. ADMET (absorption, distribution, metabolism, excretion, and toxicity) .

For research use only. We do not sell to patients.

BTRX-335140 Chemical Structure

BTRX-335140 Chemical Structure

CAS No. : 2244614-14-8

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2000 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

BTRX-335140 (CYM-53093) is a potent and selective, 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. BTRX-335140 endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. BTRX-335140 can distribute well into the CNS. ADMET (absorption, distribution, metabolism, excretion, and toxicity) [1].

IC50 & Target

IC50: 0.8 nM (κOR); 110 nM (μOR); 6500 nM (δOR)[1]

Clinical Trial
Molecular Weight

453.55

Formula

C₂₅H₃₂FN₅O₂

CAS No.

2244614-14-8

SMILES

CC1=NOC(C2=C(C)C3=CC(CC)=CC(F)=C3N=C2N4CCC(NC5CCOCC5)CC4)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (36.75 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2048 mL 11.0241 mL 22.0483 mL
5 mM 0.4410 mL 2.2048 mL 4.4097 mL
10 mM 0.2205 mL 1.1024 mL 2.2048 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.67 mg/mL (3.68 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

BTRX-335140CYM-53093BTRX335140BTRX 335140CYM53093CYM 53093Opioid ReceptorInhibitorinhibitorinhibit

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Product Name:
BTRX-335140
Cat. No.:
HY-124754
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