MK-5046 |
Catalog No.GC19413
One-Click Copy Product Info
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MK-5046 is a potent, selective, and orally active Bombesin receptor subtype 3 (BRS-3) agonist, with IC50 and EC50 values of 27nM and 25nM, respectively, for human BRS-3.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1022152-70-0
Sample solution is provided at 25 µL, 10mM.
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MK-5046 is a potent, selective, and orally active Bombesin receptor subtype 3 (BRS-3) agonist, with IC50 and EC50 values of 27nM and 25nM, respectively, for human BRS-3[1]. BRS-3 is an orphan G protein-coupled receptor (GPCR) that plays an important role in regulating energy homeostasis, glucose metabolism, and insulin secretion[2]. MK-5046 is commonly used in the treatment of obesity and in studies of BRS-3-related signaling pathways[3,4].
In vitro, treatment of BRS-3-H1299 cells with MK-5046 (0.01, 0.1, 1μM) for 5min dose-dependently and significantly increased HER2 tyrosine phosphorylation (PY1248-HER2) and ERK phosphorylation (P-ERK)[5]. Treatment of serum-starved H1299-BRS3 cells with MK-5046 (10nM) for 24h significantly enhanced cell migration, an effect that could be reversed by the BRS-3 antagonist Bantag-1 or the Hippo pathway inhibitor Verteporfin[6].
In vivo, subcutaneous administration of MK-5046 (5, 25, 50mg/kg/day) for 14 days in diet-induced obesity (DIO) mice resulted in dose-dependent body weight reduction, with a maximum weight loss of approximately 9%[7]. Intravenous administration of MK-5046 (1mg/kg) in anesthetized wild-type mice significantly increased interscapular brown adipose tissue temperature and core body temperature[8].
References:
[1] SEBHAT I K, FRANKLIN C, LO M M C, et al. Discovery of MK-5046, a potent, selective bombesin receptor subtype-3 agonist for the treatment of obesity[J]. ACS Medicinal Chemistry Letters, 2011, 2(1): 43-47.
[2] FENG Y, GUAN X M, LI J, et al. Bombesin receptor subtype-3 (BRS-3) regulates glucose-stimulated insulin secretion in pancreatic islets across multiple species[J]. Endocrinology, 2011, 152(11): 4106-4115.
[3] GONZÁLEZ N, MORENO P, JENSEN R T. Bombesin receptor subtype 3 as a potential target for obesity and diabetes[J]. Expert Opinion on Therapeutic Targets, 2015, 19(9): 1153-1170.
[4] REITMAN M L, DISHY V, MOREAU A, et al. Pharmacokinetics and pharmacodynamics of MK-5046, a bombesin receptor subtype-3 (BRS-3) agonist, in healthy patients[J]. The Journal of Clinical Pharmacology, 2012, 52(9): 1306-1316.
[5] MOODY T W, RAMOS-ALVAREZ I, MANTEY S A, et al. Bombesin receptor subtype-3 regulates tumor growth by HER2 tyrosine phosphorylation in a reactive oxygen species-dependent manner in lung cancer cells[J]. Targets, 2025, 3(1): 7.
[6] GUO M, ZHANG Y, WU L, et al. Dynamic phosphoproteomics of BRS3 activation reveals the Hippo signaling pathway for cell migration[J]. Journal of Proteome Research, 2023, 22(7): 2364-2376.
[7] GUAN X M, METZGER J M, YANG L, et al. Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist[J]. The Journal of Pharmacology and Experimental Therapeutics, 2011, 336(2): 356-364.
[8] LATEEF D M, ABREU-VIEIRA G, XIAO C, et al. Regulation of body temperature and brown adipose tissue thermogenesis by bombesin receptor subtype-3[J]. American Journal of Physiology-Endocrinology and Metabolism, 2014, 306(6): E681-E687.
| Cell experiment [1]: | |
Cell lines | Starved H1299-BRS3 cells |
Preparation Method | 5 × 104 starved cells were plated into the top chamber with FBS-free medium, while a medium containing 10% FBS and drugs was added to the external chamber as a chemoattractant. The starved cells were treated with MK-5046 (10nM), or MK-5046 and Bantag-1, or MK-5046 and Verteporfin for 24h. After incubation, 0.5% crystal violet was used to stain the cells. The upper layer cells that did not pass through the membrane were erased, while the cells that passed through were counted under an Echo Revolve Upside-Down integrated fluorescence microscope. |
Reaction Conditions | 10nM; 24h |
Applications | Treatment with MK-5046 (10nM) significantly enhanced cell migration, but this effect could be reversed by the Bantag-1 or Hippo pathway inhibitor Verteporfin. |
| Animal experiment [2]: | |
Animal models | Diet-induced obesity (DIO) mice |
Preparation Method | DIO mice received continuous subcutaneous infusion of MK-5046 at doses of 5, 25, or 50mg/kg/day for 14 days. Body weight was monitored daily throughout the study period. |
Dosage form | 5, 25, 50mg/kg/day; 14 days; s.c. |
Applications | Treatment with MK-5046 (5, 25, 50mg/kg/day) induced a dose-dependent decrease in body weight in mice, with a maximum weight loss of approximately 9%. |
References: | |
| Cas No. | 1022152-70-0 | SDF | |
| Canonical SMILES | O[C@](CC1=NC(CC2(C(F)(F)F)CC2)=CN1)(C(F)(F)F)C3=CC=C(N4C=CC=N4)C=C3 | ||
| Formula | C20H18F6N4O | M.Wt | 444.37 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2504 mL | 11.2519 mL | 22.5038 mL |
| 5 mM | 450.1 μL | 2.2504 mL | 4.5008 mL |
| 10 mM | 225 μL | 1.1252 mL | 2.2504 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)