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Ghrelin Receptor Antagonist, JMV 2959

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Synonym(s):
Ghrelin Receptor Antagonist, JMV 2959, Growth hormone secretagogue receptor antagonist, (R)-N-(2-(1H-indol-3-yl)-1-(4-(4-methoxybenzyl)-5-phenethyl-4H-1,2,4-triazol-3-yl)ethyl)-2-aminoacetamide hydrochloride, GHSR1a Antagonist, GH secretagogue receptor antagonist, JMV2959
Empirical Formula (Hill Notation):
C30H32N6O2 · xHCl
Molecular Weight:
508.61 (free base basis)

assay

≥97% (HPLC)

Quality Level

form

powder

potency

32 nM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

beige

solubility

DMSO: 100 mg/mL
water: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

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Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

assay

≥97% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

form

powder

form

solid

form

solid

form

oil

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

color

beige

color

white

color

white

color

light yellow

General description

A 1, 2, 4-triazole derived compound that acts as a potent ghrelin receptor (GHS-R1a) antagonist (IC50 = 32 nM in a binding assay, dissociation constant Kb = 19 nM). Shown to reduce hexarelin-induced food intake [hexarelin (80 µg/kg, cumulative food intake (g of food/100 g of body weight) at 6 h by acute administration (sc) of JMV 2959 (160 µg/kg)] in rats without affecting the basal food intake. Also suppresses ghrelin and fasting-induced food intake at the level of the central nervous system. Reported to suppress genes up-regulated by ghrelin. Does not affect intracellular Ca2+ mobilization.

Biochem/physiol Actions

Primary Target
Ghrelin receptor

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Physical form

Supplied as a hydrochloride salt.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Moulin, A., et al. 2013. Amino Acids44, 301.
Mary, S., et al. 2012. Proc Natl Acad Sci USA109, 8304.
Salome, N., et al. 2009. Eur J Pharmacol.612, 167,.
Moulin, A., et al. 2007. J Med Chem50, 579.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk_germany

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable


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