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

BTRX-335140 (Synonyms: CYM-53093)

Cat. No.: HY-124754 Purity: 99.71%
Handling Instructions

BTRX-335140 (CYM-53093) 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. BTRX-335140 endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. BTRX-335140 distributes well into the CNS and can be used for the research of neuropathy.

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
Solution
10 mM * 1 mL in DMSO USD 424 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 424 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 385 In-stock
Estimated Time of Arrival: December 31
10 mg USD 660 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2200 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

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Description

BTRX-335140 (CYM-53093) 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. BTRX-335140 endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. BTRX-335140 distributes well into the CNS and can be used for the research of neuropathy[1].

IC50 & Target

κ Opioid Receptor/KOR

0.8 nM (IC50)

μ-opioid receptor

110 nM (IC50)

δ-opioid receptor

6500 nM (IC50)

In Vitro

BTRX-335140 (0-10 μM; 4 h) shows selective antagonist activity towards Kappa Opioid Receptor[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: OPRK1-BLA U2OS cells
Concentration: 0-10 μM
Incubation Time: 4 hours
Result: Exibited antagonist activity to KOR, DOR and MOR with IC50 values of 0.8, 110 and 6500 nM respectively, and showed selective antagonist activity to KOR.
In Vivo

BTRX-335140 (0.01-3 mg/kg; p.o. once) reduces U69,593- stimulated plasma prolactin secretion to levels of without U69,593 treatment[1].
BTRX-335140 (1 mg/kg; i.p. once) blocks U-50488-induced antinociception from hot water[1].
1.19 Pharmacokinetic Parameters of BTRX-335140 in rodents[1].

Rats
IV 1 mg/kg
Mice
IV 3 mg/kg
Rats
PO 5 mg/kg
Mice
PO 10 mg/kg
CL (mL/min/kg) 105 66.5
t1/2 (h) 1.81 1.91 6.19 2.57
AUC0-t (h•ng/mL) 153 725 265 232
Vss (L/kg) 13.8 7.72
F (%) 30.2 12

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rat PRL model[1]
Dosage: 0.01, 0.03, 0.1, 0.3, 1 and 3 mg/kg
Administration: Oral gavage; 0.01-3 mg/kg once
Result: Effectively decreased the high level prolactin caused by U69,593 even at a dosage of 0.1 mg/kg.
Animal Model: Adult male ICR mice with tail dipped into 50°C hot water[1]
Dosage: 1 mg/kg
Administration: Intraperitoneal injection; 1 mg/kg once
Result: Blocked the U-50488-induced antinociception at 1 h but not at 24 h pretreatment time and showed a medication-like duration of action in blocking the KOR.
Clinical Trial
Molecular Weight

453.55

Formula

C25H32FN5O2

CAS No.
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

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1 mg/mL (2.20 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1 mg/mL (2.20 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.71%

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