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ML-18 is Bombesin receptor subtype 3 (BRS-3) antagonist (IC50 = 4.8 μM). ML-18 binds with lower affinity to the GRPR and NMBR with IC50 values of 16 and more than 100 μM, respectively. ML-18 at 16 μM inhibits the ability of 100 nM BA1 to cause tyrosine phosphorylation of the EGFR and ERK in lung cancer cells.
| Cell Experiment | |
|---|---|
| Cell lines | NCI-H727 or NCI-H1299 cells |
| Preparation method | NCI-H727 or NCI-H1299 cells transfected with BRS-3 are treated with ML-18 (0, 4.8, 16, 48 μM) or gefitinib added. After 2 days, 15 μL of 0.1 % MTT solution added. After 4 h, 150 μL of DMSO is added. After 16 h, the optical density at 570 nm is determined. |
| Concentrations | 0, 4.8, 16, 48 μM |
| Incubation time | 2 days |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 569.65 |
| Formula | C32H35N5O5 |
| CAS Number | 1422269-30-4 |
| Form | Solid |
| Solubility (25°C) | DMSO: ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Bombesin Receptor Products |
|---|
| MK-5046
MK-5046 is an orally active, potent, selective agonist of the orphan G protein-coupled receptor bombesin receptor subtype-3 (BRS-3) that is under evaluation for treatment of obesity. |
| Kuwanone H
Kuwanone H |
| Bombesin
Bombesin is a tetradecapeptide, which plays an important role in the release of gastrin and the activation of G-protein receptors. |
| Ranatensin
Ranatensin is a undecapeptide and a Bombesin Receptor angonist, which could maintain the dynamic balance of animal blood pressure, without cross-tachyphylaxis with Angiotensin amide, Bradykinin, or Norepinephrine. |
| RC-3095 TFA
RC-3095 TFA is a selective bombesin/gastrin releasing peptide receptor (GRPR) antagonist. |
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