1. GPCR/G Protein
  2. Bombesin Receptor
  3. MK-5046

MK-5046 

Cat. No.: HY-14342 Purity: 99.67%
Handling Instructions

MK-5046 is a novel BRS-3 agonist, binds to BRS-3 with high affinity (mouse Ki = 1.6 nM, human Ki = 25 nM).

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

MK-5046 Chemical Structure

MK-5046 Chemical Structure

CAS No. : 1022152-70-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 396 In-stock
Estimated Time of Arrival: December 31
5 mg USD 360 In-stock
Estimated Time of Arrival: December 31
10 mg USD 528 Get quote
50 mg USD 1368 Get quote
100 mg USD 2340 Get quote
200 mg   Get quote  
500 mg   Get quote  

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Description

MK-5046 is a novel BRS-3 agonist, binds to BRS-3 with high affinity (mouse Ki = 1.6 nM, human Ki = 25 nM). IC50 value: 1.6 nM (Ki, for mouse), 25 nM (Ki, for human) [1] Target: BRS-3 in vitro: MK-5046 is a novel BRS-3 agonist, with improved BRS-3 potency, specificity, and pharmacokinetic properties that allows in-depth investigation of BRS3 agonism in preclinical species and is also potentially suitable for use in humans. MK-5046 exhibits no appreciable binding activity at the neuromedin B and gastrin-releasing peptide receptors, as well as many other receptors, ion channels, and enzymes. In a cell-based Ca2+ mobilization functional assay, MK-5046 activates human BRS-3 with similar agonist efficacy as the peptide BRS-3 agonist.[1] MK-5046 is a potent, selective bombesin receptor subtype-3 agonist for the treatment of obesity.[2] in vivo: MK-5046 is the first BRS-3 agonist with properties suitable for use in larger mammals. In dogs, MK-5046 treatment produced statistically significant and persistent weight loss, which was initially accompanied by increases in body temperature and heart rate that abated with continued dosing. MK-5046 also effectively reduced body weight in rats and caused modest increases in body temperature, heart rate, and blood pressure. MK-5046 in rodents and dogs and further support BRS-3 agonism as a new approach to the treatment of obesity.[1]

Molecular Weight

444.37

Formula

C₂₀H₁₈F₆N₄O

CAS No.

1022152-70-0

SMILES

O[[email protected]](CC1=NC(CC2(C(F)(F)F)CC2)=CN1)(C(F)(F)F)C3=CC=C(N4C=CC=N4)C=C3

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 : 14.29 mg/mL (32.16 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2504 mL 11.2519 mL 22.5038 mL
5 mM 0.4501 mL 2.2504 mL 4.5008 mL
10 mM 0.2250 mL 1.1252 mL 2.2504 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 1.43 mg/mL (3.22 mM); Clear solution

  • 2.

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

    Solubility: ≥ 1.43 mg/mL (3.22 mM); Clear solution

  • 3.

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

    Solubility: ≥ 1.43 mg/mL (3.22 mM); Clear solution

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

MK-5046MK5046MK 5046Bombesin ReceptorInhibitorinhibitorinhibit

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MK-5046
Cat. No.:
HY-14342
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