Synonym
JMV2959; JMV 2959; JMV-2959
IUPAC/Chemical Name
N-[(R)-1-[4-(4-Methoxybenzyl)-5-phenethyl-4H-1,2,4-triazol-3-yl]-2-(1H-indol-3-yl)ethyl]-2-aminoacetamide
InChi Key
OZSZELOMMMKWTM-HHHXNRCGSA-N
InChi Code
InChI=1S/C30H32N6O2/c1-38-24-14-11-22(12-15-24)20-36-28(16-13-21-7-3-2-4-8-21)34-35-30(36)27(33-29(37)18-31)17-23-19-32-26-10-6-5-9-25(23)26/h2-12,14-15,19,27,32H,13,16-18,20,31H2,1H3,(H,33,37)/t27-/m1/s1
SMILES Code
O=C(N[C@@H](C1=NN=C(CCC2=CC=CC=C2)N1CC3=CC=C(OC)C=C3)CC4=CNC5=C4C=CC=C5)CN
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32 nM.
In vivo activity:
Two-way repeated-measures ANOVA analyse indicated that there was significant difference between the group exposed to JMV2959 (6 mg/kg) and the saline group(ANOVA, F(1,15) = 45.46, p < 0.01), which indicated that JMV2959 was able to influence the locomotor activity of the rats and that the CPP score was valid (Figure 2).
Reference: Front Pharmacol. 2021 Nov 29;12:718615. https://pubmed.ncbi.nlm.nih.gov/34912212/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
25.0 |
49.15 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
508.63
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Zhao J, Du X, Chen M, Zhu S. Growth Hormone Secretagogue Receptor 1A Antagonist JMV2959 Effectively Prevents Morphine Memory Reconsolidation and Relapse. Front Pharmacol. 2021 Nov 29;12:718615. doi: 10.3389/fphar.2021.718615. PMID: 34912212; PMCID: PMC8666548.
2. Engel JA, Jerlhag E, Svensson L, Smith RG, Egecioglu E. 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. doi: 10.1007/s00213-015-4054-3. Epub 2015 Aug 29. PMID: 26319159; PMCID: PMC4613889.
In vivo protocol:
1. Zhao J, Du X, Chen M, Zhu S. Growth Hormone Secretagogue Receptor 1A Antagonist JMV2959 Effectively Prevents Morphine Memory Reconsolidation and Relapse. Front Pharmacol. 2021 Nov 29;12:718615. doi: 10.3389/fphar.2021.718615. PMID: 34912212; PMCID: PMC8666548.
2. Engel JA, Jerlhag E, Svensson L, Smith RG, Egecioglu E. 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. doi: 10.1007/s00213-015-4054-3. Epub 2015 Aug 29. PMID: 26319159; PMCID: PMC4613889.
1: Rodriguez JA, Fehrentz JA, Martinez J, Ben Haj Salah K, Wellman PJ. The GHR-R antagonist JMV 2959 neither induces malaise nor alters the malaise property of LiCl in the adult male rat. Physiol Behav. 2018 Jan 1;183:46-48. doi: 10.1016/j.physbeh.2017.10.017. Epub 2017 Oct 19. PubMed PMID: 29056353.
2: Abtahi S, Howell E, Currie PJ. Accumbal ghrelin and glucagon-like peptide 1 signaling in alcohol reward in female rats. Neuroreport. 2018 Aug 15;29(12):1046-1053. doi: 10.1097/WNR.0000000000001071. PubMed PMID: 29927808.
3: Havlickova T, Charalambous C, Lapka M, Puskina N, Jerabek P, Sustkova-Fiserova M. Ghrelin Receptor Antagonism of Methamphetamine-Induced Conditioned Place Preference and Intravenous Self-Administration in Rats. Int J Mol Sci. 2018 Sep 26;19(10). pii: E2925. doi: 10.3390/ijms19102925. PubMed PMID: 30261633; PubMed Central PMCID: PMC6213741.
4: Terrill SJ, Wall KD, Medina ND, Maske CB, Williams DL. Lateral septum growth hormone secretagogue receptor affects food intake and motivation for sucrose reinforcement. Am J Physiol Regul Integr Comp Physiol. 2018 Jul 1;315(1):R76-R83. doi: 10.1152/ajpregu.00339.2017. Epub 2018 Mar 28. PubMed PMID: 29590554; PubMed Central PMCID: PMC6087886.
5: Sustkova-Fiserova M, Charalambous C, Havlickova T, Lapka M, Jerabek P, Puskina N, Syslova K. Alterations in Rat Accumbens Endocannabinoid and GABA Content during Fentanyl Treatment: The Role of Ghrelin. Int J Mol Sci. 2017 Nov 22;18(11). pii: E2486. doi: 10.3390/ijms18112486. PubMed PMID: 29165386; PubMed Central PMCID: PMC5713452.
