[CAS NO. 2448414-54-6] JMV 2959 hydrochloride
PRODUCTS SPECIFICATIONS [2448414-54-6]
DESCRIPTION [2448414-54-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 545.08 |
| Molecular Formula | C30H33ClN6O2 |
| SMILES | O=C(N[C@@H](C1=NN=C(CCC2=CC=CC=C2)N1CC3=CC=C(OC)C=C3)CC4=CNC5=C4C=CC=C5)CN.[H]Cl |
2 Publications Citing Use of MCE
Summary
JMV 2959 hydrochloride is a growth hormone secretagogue receptor type 1a ( GHS-R 1a ) antagonist with an IC 50 of 32±3 nM in LLC-PK 1 cells.
IC50 & Target
IC50: 32±3 nM (GHS-R 1a , in LLC-PK 1 cells) [1]
In Vitro
JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R 1a ) antagonist with an IC 50 of 32 nM. JMV 2959 does not induce any intracellular calcium mobilization by itself. The dissociation constant of the receptor/JMV 2959 complex is determined by the Schild method. This experiment reveals a dissociation constant Kb of 19±6 nM [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Intraperitoneal (i.p.) administration of Ghrelin (0.033, 0.1, and 0.33 mg/kg) does not alter the acoustic startle responses (ASR) or prepulse inhibition (PPI) in rats. Conversely, i.p. injection of JMV 2959 (1, 3, and 6 mg/kg), dose dependently decrease the ASR and increase PPI. Pretreatment with JMV 2959 at a dose with no effect on ASR or PPI per se, completely blocks Phencyclidine (PCP)-induced (2 mg/kg) deficits in PPI while pretreatment with the highest dose of Ghrelin does not potentiate or alter PPI responses of a sub-threshold dose of PCP (0.75 mg/kg) [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 250 mg/mL ( 458.65 mM ; Need ultrasonic)
H 2 O : 25 mg/mL ( 45.86 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
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1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (183.46 mM); Clear solution; Need ultrasonic
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2.
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3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.82 mM); Clear solution
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4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.82 mM); Clear solution
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.