Product Details
| Product Name:
BTRX-335140 |
CAS No.:
2244614-14-8 |
| Purity:
98.45% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | BTRX-335140 |
| Description | BTRX-335140 (CYM-53093) is a potent and selective orally active κ-opioid receptor (KOR) antagonist with antagonistic activity against κOR, μOR, and δOR with IC50 values of 0.8, 110, and 6500 nM, respectively. |
| In vitro | METHODS: Tango OPRK1-bla U2OS cells were used to express KORs associated with the GAL4-VP16 transcription factor through the TEV protease locus.
RESULTS Navacaprant (BTRX-335140) showed antagonistic activity against κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM and 6.5 μM, respectively.[1] |
| In vivo | METHODS: Mice were injected with BTRX-335140 (CYM-53093) (1 mg/kg, i.p.) 1 h and 24 h prior to the injection of U-50488 (15 mg/kg, i.v.) and tail-wagging latencies were measured at baseline, 30 min and 60 min after the agonist injection, while the mice were administered BTRX-335140 (CYM-53093) (3, 10, and 30 mg/kg) (3, 10, and 30 mg/kg) orally alone. 53093) (3, 10, and 30 mg/kg) alone, while mice were orally administered BTRX-335140 (CYM-53093) to assess the ability of BTRX-335140 (CYM-53093) to antagonize the antinociceptive effects of U-50488.
RESULTS BTRX-335140 (CYM-53093) (1 mg/kg, i.p.) blocked U-50488-induced antinociception within 1 h. The delayed tail-flash response induced by oral administration of BTRX-335140 (CYM-53093) (1 mg/kg) alone did not show any significant change in the tail-flash response induced by oral BTRX-335140 (CYM-53093) (1 mg/kg) at 1 h post-dosing in rats. 335140 (CYM-53093) (3, 10 and 30 mg/kg) also blocked U-50488-induced antinociception in a dose-dependent manner. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 5.5 mg/mL (12.13 mM), Sonication is recommended.
|
| Keywords | BTRX335140 | CNS | CYM53093 | U69593 | BTRX 335140 | Inhibitor | U2OS | Opioid Receptor | inhibit | neurobehavioral disorder | BTRX-335140 | CYM 53093 | oral |
| Inhibitors Related | Docusate sodium | Bevenopran | Mirtazapine | Sinomenine | (-)-Menthol | Matrine | SCH 221510 | Progesterone | Naltrexone hydrochloride | Trimebutine | Mianserin hydrochloride | Amentoflavone |
| Related Compound Libraries | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$107.00/1mg |
VIP5Y
|
TargetMol Chemicals Inc.
|
2024-11-19 |
United States