VB124
- Product Name
- VB124
- CAS No.
- 2230186-18-0
- Chemical Name
- VB124
- Synonyms
- VB124;VB124 ，S9929;VB124 MCT4 Inhibitor;VB124, 10 mM in DMSO;2-((1-(2-chlorophenyl)-5-(3-cyclopropoxyphenyl)-1H-pyrazol-3-yl)methoxy)-2-methylpropanoic acid;Propanoic acid, 2-[[1-(2-chlorophenyl)-5-[3-(cyclopropyloxy)phenyl]-1H-pyrazol-3-yl]methoxy]-2-methyl-
- CBNumber
- CB99738844
- Molecular Formula
- C23H23ClN2O4
- Formula Weight
- 426.89
- MOL File
- 2230186-18-0.mol
VB124 Property
- Boiling point:
- 613.1±55.0 °C(Predicted)
- Density
- 1.31±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- pka
- 3.56±0.10(Predicted)
- form
- Solid
- color
- White to off-white
- InChI
- InChI=1S/C23H23ClN2O4/c1-23(2,22(27)28)29-14-16-13-21(26(25-16)20-9-4-3-8-19(20)24)15-6-5-7-18(12-15)30-17-10-11-17/h3-9,12-13,17H,10-11,14H2,1-2H3,(H,27,28)
- InChIKey
- PZHRLEZWTVYGMP-UHFFFAOYSA-N
- SMILES
- C(O)(=O)C(OCC1C=C(C2=CC=CC(OC3CC3)=C2)N(C2=CC=CC=C2Cl)N=1)(C)C
VB124 Chemical Properties,Usage,Production
Uses
VB124 is an orally active, potent, and selective MCT4 inhibitor. VB124 can specifically inhibit lactate efflux with IC50s of 8.6 nM and 19 nM for lactate import and export in MDA-MB-231 cells, respectively. VB124 is highly selective for MCT4 over MCT1. VB124 can be used for the research of cardiac hypertrophy, heart failure, and metabolism[1].
Biological Activity
VB124 is an orally active, potent, and selective MCT4 inhibitor. VB124 can specifically inhibit lactate efflux with IC50s of 8.6 nM and 19 nM for lactate import and export in MDA-MB-231 cells, respectively. VB124 is highly selective for MCT4 over MCT1. VB124 can be used for the research of cardiac hypertrophy, heart failure, and metabolism[1]. VB124 (10 μM) inhibits the cell proliferation of MDA-MB-231 cells, and the cell proliferation rate is less than 50%[1].VB124 is highly selective for MCT4 over MCT1, showing very little MCT1 inhibitory activity (lactate export IC50=24 μM) in MCT1-expressing BT20 cells[1]. VB124 (30 mg/kg; p.o.; daily for 28 days) attenuates isoproterenol-induced cardiac hypertrophy in mice[1].VB124 (30 mg/kg; twice per day for 180 days) has no effect on the body, heart, liver, or lung weight of mice, suggesting no overt toxicities[1].
in vivo
VB124 (30 mg/kg; p.o.; daily for 28 days) attenuates isoproterenol-induced cardiac hypertrophy in mice[1].
VB124 (30 mg/kg; twice per day for 180 days) has no effect on the body, heart, liver, or lung weight of mice, suggesting no overt toxicities[1].
| Animal Model: | 12 weeks old C57BL/6 mice[1] |
| Dosage: | 30 mg/kg |
| Administration: | Oral gavage; daily for 28 days (dissolved in 0.5% methylcellulose and 0.1% Tween-20) |
| Result: | Prevented cardiac hypertrophy in mice. |
IC 50
MCT4
References
[1]. Cluntun AA, et.al. The pyruvate-lactate axis modulates cardiac hypertrophy and heart failure. Cell Metab. 2021 Mar 2;33(3):629-648.e10.
VB124 Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from VB124 manufacturers
- Product
- VB124 2230186-18-0
- Price
- US $0.00/mg
- Min. Order
- 1mg
- Purity
- 98%+ HPLC HNMR
- Supply Ability
- 50 g permonth
- Release date
- 2024-03-29