MCH(human, mouse, rat) (TFA)

Cat# HY-P1205A-10mg

Size : 10mg

Marca : MedChemExpress


Description

MCH (human, mouse, rat) TFA is a cyclic neuropeptide mainly synthesized by neurons in the lateral hypothalamic area. MCH (human, mouse, rat) TFA also serves as an endogenous ligand for the melanin-concentrating hormone receptor (MHC receptor), with a binding IC50 of 0.3 nM and 1.5 nM for human MCH-1R and MCH-2R, respectively; its functional EC50 values are 3.9 nM and 88.7 nM. MCH (human, mouse, rat) TFA acts not only as an orexigenic signal but also as a key integrating and regulatory hormone for energy homeostasis and sleep-wake cycles. MCH (human, mouse, rat) TFA can be used in studies related to obesity, sleep disorders, and other associated conditions[1][2][3][4].

IC50 & Target

Binding IC50: 0.3 nM (MCH1R)
IC50: 1.5 nM (MCH1R)[1]

In Vitro

MCH (human, mouse, rat) TFA potently displaces the binding of [125I]Phe13-Tyr19-MCH to MCH-2R on the membranes of transfected COS-7 and CHO cells, with an IC50 of 1.5 nM[2].
MCH (human, mouse, rat) (60 min) TFA dose-dependently activates calcium mobilization in CHO cells stably expressing human MCH-2R, with an EC50 of 0.1 nM[2].
MCH (human, mouse, rat) (30 s) TFA induces a robust, dose-dependent intracellular calcium response in HEK293-AEQ17 cells stably expressing human MCH-2R, with an EC50 of 31 nM[2].
MCH (human, mouse, rat) (1 h) TFA potently stimulates inositol phosphate turnover in HEK293-AEQ17 cells stably expressing human MCH-2R, with an EC50 of 2.7 nM[2].
MCH (human, mouse, rat) TFA reduces the release of α-MSH and secretion of CART in rodent hypothalamic tissue explants, and induces the release of NPY and AgRP[3].
MCH (human, mouse, rat) TFA induces dose-dependent GIRK currents in Xenopus laevis oocytes co-expressing SLC-1 receptors and GIRK channels[4].
MCH (human, mouse, rat) TFA induces calcium-mediated chloride currents in Xenopus laevis oocytes expressing the SLC-1 receptor by activating the phospholipase C pathway[4].
MCH (human, mouse, rat) TFA exerts inhibitory effects on primary cultured rat LH neurons, including reducing spontaneous firing frequency, suppressing glutamatergic synaptic transmission, and decreasing the amplitude of VDCC via a Gi/o-dependent pathway, with an IC50 of 7.84 nM, and it does not induce GIRK currents[4].

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

In Vivo

Administration of MCH (human, mouse, rat) (into the medial preoptic area) TFA reduces the active maternal behavioral components in lactating rats[1].
Levels of MCH (human, mouse, rat) TFA are upregulated in fasted rats, leptin-deficient ob/ob obese mice, fa/fa rats, and diet-induced obese rats[2].
TFA form of MCH (human, mouse, rat) (administered intracerebroventricularly; acute single injection; chronic infusion) exerts orexigenic effects in Wistar rats and Sprague-Dawley rats, including increased acute food intake and obesity induced by chronic infusion[3].
TFA form of MCH (human, mouse, rat) (intracerebral/intracerebroventricular; chronic administration) increases food intake, body weight and obesity in mice, while overexpression of this substance in the lateral hypothalamus induces obesity and insulin resistance[4].
TFA form of MCH (human, mouse, rat) (administered intracerebrally; administered intracerebroventricularly; administered locally in the hypothalamus; acutely administered) stimulates food intake in rats[4].
MCH (human, mouse, rat) TFA regulates memory retention in rats[4].

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

Masse moléculaire

2500.86

Formule

C107H161F3N30O28S4

Appearance

Solid

Color

White to off-white

Sequence

Asp-Phe-Asp-Met-Leu-Arg-Cys-Met-Leu-Gly-Arg-Val-Tyr-Arg-Pro-Cys-Trp-Gln-Val (Disulfide bridge:Cys7-Cys16)

Sequence Shortening

DFDMLRCMLGRVYRPCWQV (Disulfide bridge:Cys7-Cys16)

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvant et solubilité
In Vitro: 

DMSO : 100 mg/mL (39.99 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 0.3999 mL 1.9993 mL 3.9986 mL
5 mM 0.0800 mL 0.3999 mL 0.7997 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 (1.00 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 (1.00 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.
Pureté et documentation
Références