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> Dinoprost [551-11-1]

Dinoprost [551-11-1]

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Referencia HY-12956-10mg

embalaje : 10mg

Marca : MedChemExpress

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Descripciòn

Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour[1][2].

IC50 & Target[1][2]

FP Receptor

 

Human Endogenous Metabolite

 

Cellular Effect
Cell Line Type Value Description References
CHO IC50
>10000 nM
Compound: PGF2
Affinity for Prostaglandin I2 receptor expressed in CHO cells
Affinity for Prostaglandin I2 receptor expressed in CHO cells
[PMID: 10715159]
CHO IC50
>10000 nM
Compound: PGF2
Affinity for Prostanoid EP2 receptor expressed in CHO cells
Affinity for Prostanoid EP2 receptor expressed in CHO cells
[PMID: 10715159]
CHO IC50
>10000 nM
Compound: PGF2
Affinity for Prostanoid TP receptor expressed in CHO cells
Affinity for Prostanoid TP receptor expressed in CHO cells
[PMID: 10715159]
CHO IC50
>10 μM
Compound: PGF2
Affinity for Prostaglandin I2 receptor expressed in CHO cells
Affinity for Prostaglandin I2 receptor expressed in CHO cells
[PMID: 10715159]
CHO IC50
322 nM
Compound: PGF2
Affinity for Prostanoid EP3 receptor expressed in CHO cell line
Affinity for Prostanoid EP3 receptor expressed in CHO cell line
[PMID: 10715159]
CHO IC50
4200 nM
Compound: PGF2
Affinity for Prostanoid EP4 receptor expressed in CHO cells
Affinity for Prostanoid EP4 receptor expressed in CHO cells
[PMID: 10715159]
COS-7 IC50
380 nM
Compound: PGF2
Affinity for Prostanoid EP1 receptor expressed in COS-7 cells.
Affinity for Prostanoid EP1 receptor expressed in COS-7 cells.
[PMID: 10715159]
COS-7 IC50
7 nM
Compound: PGF2
Affinity for human Prostanoid FP receptor expressed in COS-7 cells
Affinity for human Prostanoid FP receptor expressed in COS-7 cells
[PMID: 10715159]
HEK293 IC50
4500 nM
Compound: PGF2
Affinity for human Prostaglandin D2 receptor expressed in HEK293 cells
Affinity for human Prostaglandin D2 receptor expressed in HEK293 cells
[PMID: 10715159]
K562 IC50
>700 μM
Compound: 1
In vitro antiproliferative activity was measured on human leukemia K562 cells
In vitro antiproliferative activity was measured on human leukemia K562 cells
10.1016/S0960-894X(00)80372-8
NIH3T3 EC50
24.5 nM
Compound: PGF2alpha
Agonist activity at FP receptor in Swiss mouse 3T3 cells assessed as [3H]-IP accumulation by scintillation counting
Agonist activity at FP receptor in Swiss mouse 3T3 cells assessed as [3H]-IP accumulation by scintillation counting
[PMID: 19101156]
NIH3T3 EC50
24.5 nM
Compound: PGF2 alpha
Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells
Efficacy for stimulation of prostanoid FP receptor-linked phosphoinositide turnover in Swiss 3T3 mouse fibroblast cells
[PMID: 15357985]
Oocyte IC50
0.287 μM
Compound: Prostaglandin F2alpha
TP_TRANSPORTER: inhibition of PGD2 uptake in Xenopus laevis oocytes
TP_TRANSPORTER: inhibition of PGD2 uptake in Xenopus laevis oocytes
[PMID: 10973807]
In Vitro

Dinoprost (Prostaglandin F2α; 1 μM; for 24 hours) induces ER stress, autophagy, and apoptosis in goat luteal cells[1].
Dinoprost (1 μM; for 24 hours) significantly increases the expression of GRP78 and UPR sensors[1].

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

Dinoprost Related Antibodies

Apoptosis Analysis[1]

Cell Line: Goat luteal cells
Concentration: 1 μM
Incubation Time: For 24 hours
Result: Significantly increased the apoptotic rate (15.62±3.12%).

Cell Autophagy Assay[1]

Cell Line: Goat luteal cells
Concentration: 1 μM
Incubation Time: For 24 hours
Result: There was extensive overlap between LC3 and LAMP1 in luteal cells and autophagolysosomes were formed in goat luteal cells.

Western Blot Analysis[1]

Cell Line: Goat luteal cells
Concentration: 1 μM
Incubation Time: For 24 hours
Result: The expression of GRP78 and UPR sensors including cleaved ATF6, phosphorylated-EIF2S1, EIF2S1, ATF4, phosphorylated-IRE1, autophagy-related protein LC3-II, and pro-apoptosis factor cleaved Caspase3 increased significantly in the cells.
Ensayo clínico
Peso molecular

354.48

Fòrmula

C20H34O5
No. CAS
Appearance

<25°C Solid,>35°C Liquid

Color

White to light brown

SMILES

CCCCC[C@H](O)/C=C/[C@H]1[C@H](O)C[C@H](O)[C@@H]1C/C=C\CCCC(O)=O
Structure Classification
Initial Source
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
In Vitro: 

DMSO : 100 mg/mL (282.10 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 2.8210 mL 14.1052 mL 28.2103 mL
5 mM 0.5642 mL 2.8210 mL 5.6421 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.

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 (7.05 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 (7.05 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.
Pureza y Documentación
Referencias

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