2. GPCR/G Protein
  3. GHSR
  4. L-692429

L-692429 (MK-0751) is a benzolactam derivative and a nonpeptidyl growth hormone secretagogue (GHS) agonist. L-692429 binds to G protein-coupled receptor with a Ki of 63 nM.

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L-692429 Chemical Structure

L-692429 Chemical Structure

CAS No. : 145455-23-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 538 In-stock
Solution
10 mM * 1 mL in DMSO USD 538 In-stock
Solid
5 mg USD 480 In-stock
10 mg USD 800 In-stock
25 mg USD 1550 In-stock
50 mg USD 2400 In-stock
100 mg USD 3500 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of L-692429:

L-692429 Related Antibodies

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GHSR1a

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  • Purity & Documentation

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Description

L-692429 (MK-0751) is a benzolactam derivative and a nonpeptidyl growth hormone secretagogue (GHS) agonist. L-692429 binds to G protein-coupled receptor with a Ki of 63 nM[1][2].

IC50 & Target

Growth hormone secretagogue (GHS)[1][3]
Cellular Effect
Cell Line Type Value Description References
Pituitary gland cell ED50
125 nM
Compound: 1
Compound was evaluated for its potency using rat pituitary cell assay
Compound was evaluated for its potency using rat pituitary cell assay
10.1016/S0960-894X(97)10115-9
Pituitary gland cell EC50
60 nM
Compound: L-692429
In vitro for growth hormone release by using rat pituitary cell assay.
In vitro for growth hormone release by using rat pituitary cell assay.
10.1016/0960-894X(96)00394-0
In Vitro

L-692429 stimulates intracellular calcium release, inositol phosphate (IP) turnover, cAMP-responsive element binding protein (CREB) activity, serum-responsive element activity and bioluminescence resonance energy transfer (BRET) activity with EC50 values of 26 nM, 47 nM, 60 nM, 63 nM and 58 nM, respectively[2].
HeLa-T4 cells transiently expressing the flag epitope-tagged growth hormone secretagogue (GHS) receptor are treated with L-692429. The release of intracellular calcium is measured using fluorometry with the calcium indicator dye fluo-3/AM. Untransfected HeLa-T4 cells are unresponsive to L-692429 treatment, whereas HeLa-T4 cells transiently expressing GHS receptors demonstrate an increase in fluorescent emission after L-692429 treatment. A significant increase in luciferase activity after L-692429 treatment is seen, suggesting that activation of the GHS receptor stimulates the MAPK pathway[3].

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

L-692429 Related Antibodies
In Vivo

When tested in anesthetized rats (Wistar rats), L-756867 inhibits L-692429 (100 μg/kg)-stimulated GH secretion in a dose-dependent manner. Complete inhibition is observed at an i.v. dose of 100 μg/kg of L-756867[1].

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

509.60

Formula

C29H31N7O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(C)(N)CC(N[C@H]1C(N(CC2=CC=C(C3=CC=CC=C3C4=NNN=N4)C=C2)C5=CC=CC=C5CC1)=O)=O
Shipping

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

DMSO : 50 mg/mL (98.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9623 mL 9.8116 mL 19.6232 mL
5 mM 0.3925 mL 1.9623 mL 3.9246 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Dosing volume
(per animal)

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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

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9623 mL 9.8116 mL 19.6232 mL 49.0581 mL
5 mM 0.3925 mL 1.9623 mL 3.9246 mL 9.8116 mL
10 mM 0.1962 mL 0.9812 mL 1.9623 mL 4.9058 mL
15 mM 0.1308 mL 0.6541 mL 1.3082 mL 3.2705 mL
20 mM 0.0981 mL 0.4906 mL 0.9812 mL 2.4529 mL
25 mM 0.0785 mL 0.3925 mL 0.7849 mL 1.9623 mL
30 mM 0.0654 mL 0.3271 mL 0.6541 mL 1.6353 mL
40 mM 0.0491 mL 0.2453 mL 0.4906 mL 1.2265 mL
50 mM 0.0392 mL 0.1962 mL 0.3925 mL 0.9812 mL
60 mM 0.0327 mL 0.1635 mL 0.3271 mL 0.8176 mL
80 mM 0.0245 mL 0.1226 mL 0.2453 mL 0.6132 mL
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L-692429 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:

L-692429145455-23-8MK-0751L692429L 692429MK0751MK 0751GHSRGrowth hormone secretagogue receptorGhrelin receptorBenzolactamnonpeptidylGHsecretagogueCREBBRETSREIPMAPKInhibitorinhibitorinhibit

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