| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
IC50: 32±3 nM (GHS-R1a, in LLC-PK1 cells)[1]
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| ln Vitro |
With an IC50 of 32 nM, JMV 2959 is an antagonist of growth hormone secretagogue receptor type 1a (GHS-R1a). By itself, JMV 2959 is unable to cause any intracellular calcium mobilization. The Schild method is used to determine the receptor/JMV 2959 complex's dissociation constant. The dissociation constant Kb, as determined by this experiment, is 19±6 nM[1].
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| ln Vivo |
Ghrelin (0.033, 0.1, and 0.33 mg/kg) administered intraperitoneally (ip) has no effect on rats' prepulse inhibition (PPI) or auditory startle reactions (ASR). On the other hand, dose-dependently increasing PPI and decreasing ASR is seen with intraperitoneal injection of JMV 2959 (1, 3, and 6 mg/kg). While pretreatment with the highest dose of Ghrelin does not potentiate or change PPI responses of a sub-threshold dose of PCP (0.75 mg/kg), pretreatment with JMV 2959 at a level that has no effect on ASR or PPI per se entirely inhibits Phencyclidine (PCP)-induced (2 mg/kg) deficits in PPI[2].
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| References |
[1]. Moulin A, et al. The 1,2,4-triazole as a scaffold for the design of ghrelin receptor ligands: development of JMV 2959, a potent antagonist. Amino Acids. 2013 Feb;44(2):301-14.
[2]. Engel JA, et al. Blockade of growth hormone secretagogue receptor 1A signaling by JMV 2959 attenuates the NMDAR antagonist, phencyclidine-induced impairments in prepulse inhibition. Psychopharmacology (Berl). 2015 Dec;232(23):4285-92 |
| Molecular Formula |
C30H33CLN6O2
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| Molecular Weight |
545.08
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| CAS # |
2448414-54-6
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| Related CAS # |
JMV 2959;925238-89-7
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| Solubility (In Vitro) |
DMSO: 250 mg/mL (458.65 mM)
H2O: 25 mg/mL (45.86 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.82 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.82 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (183.46 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8346 mL | 9.1730 mL | 18.3459 mL | |
| 5 mM | 0.3669 mL | 1.8346 mL | 3.6692 mL | |
| 10 mM | 0.1835 mL | 0.9173 mL | 1.8346 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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