2. GPCR/G Protein
  3. GHSR
  4. JMV 2959

JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32 nM.

For research use only. We do not sell to patients.

JMV 2959 Chemical Structure

JMV 2959 Chemical Structure

CAS No. : 925238-89-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 121 In-stock
Solution
10 mM * 1 mL in DMSO USD 121 In-stock
Solid
5 mg USD 110 In-stock
10 mg USD 190 In-stock
25 mg USD 410 In-stock
50 mg USD 660 In-stock
100 mg USD 1060 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of JMV 2959:

JMV 2959 Related Antibodies

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GHSR1a

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32 nM.

IC50 & Target

IC50: 32 nM (GHS-R1a)
Cellular Effect
Cell Line Type Value Description References
LLC-PK1 IC50
32 nM
Compound: 1, JMV 2959
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
Displacement of 125I-[His9]-ghrelin from human GHSR1a expressed in LLC-PK1 cells by competitive binding assay
[PMID: 25435152]
In Vitro

JMV 2959 is a growth hormone secretagogue receptor type 1a (GHS-R1a) antagonist with an IC50 of 32 nM. JMV 2959 does not induce any intracellular calcium mobilization by itself[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

JMV 2959 Related Antibodies
In Vivo

When administered alone, it does not increase food intake and does not significantly stimulate growth hormone (GH) release[1]. JMV 2959 dose dependently decreases the startle response (F(3.42)=4.4, p<0.01) and increases %prepulse inhibition (PPI) (F(3.42)=3.9, p<0.05) in the prepulse inhibition paradigm. The alteration in the startle response is mainly due to a 27% decrease in the startle seen in the highest dose of JMV 2959 (6 mg/kg) compare to vehicle (p<0.05)[2]. 6 mg/kg JMV 2959 induces a significant suppression of locomotion on days 1 to 7 relative to baseline day 0 (F(7,49)=2.21, p<0.05). Results also reveal a significant interaction between JMV 2959 treatment and day (F(1,14)=4.397, p<0.05)[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

508.61

Formula

C30H32N6O2
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (49.15 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9661 mL 9.8307 mL 19.6614 mL
5 mM 0.3932 mL 1.9661 mL 3.9323 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 5 mg/mL (9.83 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Animal Administration
[2]

Two-hundred-gram male Sprague-Dawley rats are used in the study. The animals (n=15) are randomly assigned to an initial treatment dose or vehicle and subsequently receive all the different doses tested in a counter balanced design. Each test is separated by a 3- to 4-day-long washout period. The rats are given the injection of JMV 2959 (or vehicle) 17 min prior to being placed in the startle cages (i.e., 25 min prior to the first pulse). The doses of JMV 2959 used for the dose response are 1, 3, and 6 mg/kg[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9661 mL 9.8307 mL 19.6614 mL 49.1536 mL
5 mM 0.3932 mL 1.9661 mL 3.9323 mL 9.8307 mL
10 mM 0.1966 mL 0.9831 mL 1.9661 mL 4.9154 mL
15 mM 0.1311 mL 0.6554 mL 1.3108 mL 3.2769 mL
20 mM 0.0983 mL 0.4915 mL 0.9831 mL 2.4577 mL
25 mM 0.0786 mL 0.3932 mL 0.7865 mL 1.9661 mL
30 mM 0.0655 mL 0.3277 mL 0.6554 mL 1.6385 mL
40 mM 0.0492 mL 0.2458 mL 0.4915 mL 1.2288 mL
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JMV 2959 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JMV 2959925238-89-7JMV2959JMV-2959GHSRGrowth hormone secretagogue receptorGhrelin receptorInhibitorinhibitorinhibit

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