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JMV 2959

Cat. No. M11344
JMV 2959 Structure
Size Price Availability Quantity
10mg USD 190  USD190 In stock
25mg USD 400  USD400 In stock
50mg USD 650  USD650 In stock
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Quality Control & Documentation
Biological Activity

JMV 2959 is a growth hormone secretin receptor type 1A (GHS-R1A) antagonist that acts on LC-PK1 cells and inhibits GHS-R1A with an IC50 value of 32±3 nM.

Chemical Information
Molecular Weight 508.61
Formula C30H32N6O2
CAS Number 925238-89-7
Form Solid
Solubility (25°C) DMSO ≥ 200 mg/mL
Storage 4°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] David P Dunn, et al. Neurosci Lett. Role of mesolimbic ghrelin in the acquisition of cocaine reward

[2] Juan A Rodriguez, et al. Physiol Behav. The GHR-R antagonist JMV 2959 neither induces malaise nor alters the malaise property of LiCl in the adult male rat

[3] Jrgen A Engel, et al. Psychopharmacology (Berl). Blockade of growth hormone secretagogue receptor 1A signaling by JMV 2959 attenuates the NMDAR antagonist, phencyclidine-induced impairments in prepulse inhibition

[4] Paul J Wellman, et al. Front Neurosci. Ghrelin and ghrelin receptor modulation of psychostimulant action

[5] Aline Moulin, et al. Amino Acids. The 1,2,4-triazole as a scaffold for the design of ghrelin receptor ligands: development of JMV 2959, a potent antagonist

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