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Progesterone Estrogen/progestogen Receptor Agonist

Name: Progesterone
Brand: Selleck Chemicals
SKU: S1705
Rating: 5 (16 reviews)

Kat.nr.: S1705

Progesterone är ett endogent steroidhormon involverat i menstruationscykeln, graviditet och embryogenes hos människor och andra arter. Denna förening är en potent agonist av den nuclear progesterone receptor (nPR) med Kd på 1 nM; en agonist av de membrane progesterone receptors(mPRs); en antagonist av σ1 receptor.

Progesterone Estrogen/progestogen Receptor Agonist Chemical Structure

Kemisk struktur

Molekylvikt: 314.46

Hoppa till

Kvalitetskontroll (Quality Control)

Batch: Renhet: 99.86%

99.86

Relaterade mål	Adrenergic Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor THR PGES
Övrigt Estrogen/progestogen Receptor Inhibitorer	Elacestrant (RAD1901) Dihydrochloride Vepdegestrant (ARV-471) MPP dihydrochloride Kaempferol Cholesterol PHTPP G15 Licochalcone A Endoxifen HCl Pregnenolone

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Cellinjer	Analystyp	Koncentration	Inkubationstid	Aktivitetsbeskrivning
human T47D cells	Function assay		20 h	Activation of progesterone receptor in human T47D cells after 20 hrs by PRE-tagged luciferase reporter gene assay, EC50=0.1 nM
CV-1 cells	Function assay			Effective concentration for half-maximal activation of human progesterone receptor expressed in CV-1 cells, EC50=1.5 nM
HEK293 cells	Function assay			Agonist activity at human PRGR expressed in HEK293 cells by luciferase reporter gene assay, EC50=2 nM
SF-12 cells	Function assay			Displacement of DHT from human androgen receptor expressed in baculovirus SF-12 cells, Ki=9.5 nM
CHO cells	Function assay			Agonist activity at human TGR5 expressed in CHO cells by luciferase assay, EC50=2.77 μM
human K562/R7 cells	Function assay	1 μM	72 h	Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay, IC50=10.6 μM
A2780 cells	Function assay			Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay, IC50=47.863 μM
HeLa cells	Cytotoxicity assay			Cytotoxicity against human HeLa cells assessed as inhibition of DNA replication by imaging analysis
Klicka för att visa mer experimentella data för cellinjer

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Molekylvikt	314.46	Formel	C₂₁H₃₀O₂	Lagring (från mottagningsdatumet)	3 år-20°Cpulver
CAS-nr	57-83-0	Ladda ner SDF		Lagring av stamlösningar	1 år-80°Ci lösningsmedel 1 månad-20°Ci lösningsmedel
Synonymer	NSC 64377, Pregn-4-ene-3,20-dione,NSC 9704			Smiles	CC(=O)C1CCC2C1(CCC3C2CCC4=CC(=O)CCC34C)C

Löslighet (Solubility)

In vitro
Batch:

DMSO : 40 mg/mL (127.2 mM)
(Fuktkontaminerad DMSO kan minska lösligheten. Använd färk, vattenfri DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble

Molaritetsräknare

Massa	Koncentration	Volym	Molekylvikt
=	×	×

Utspädningsräknare Molekylviktsräknare

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.	2.000mg/ml (6.36mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.	0.330mg/ml (1.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 6.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo-formuleringsräknare (Klar lösning)

Steg 1: Ange information nedan (Rekommenderas: Ett extra djur för att ta hänsyn till förluster under experimentet)

Dosering: mg/kg Djurens medelvikt: g Doseringsvolym per djur:μL Antal djur:

Steg 2: Ange in vivo-formuleringen (Detta är endast räknaren, inte formuleringen. Vänligen kontakta oss först om det inte finns någon in vivo-formulering i löslighetsavsnittet.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Beräkningsresultat:

Arbetskoncentration: mg/ml;

Metod för att bereda DMSO-stamlösning: mg substans förlöst i μL DMSO ( Stamlösningskoncentration mg/mL, Vänligen kontakta oss först om koncentrationen överskrider DMSO-lösligheten för denna batch av substansen. )

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedanμL PEG300, blanda och klarna, tillsätt sedanμL Tween 80, blanda och klarna, tillsätt sedan μL ddH₂O, blanda och klarna.

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedan μL Majsolja, blanda och klarna.

Obs: 1. Se till att vätskan är klar innan du tillsätter nästa lösningsmedel.
2. Se till att tillsätta lösningsmedlet/lösningsmedlen i ordning. Du måste se till att lösningen som erhålls i föregående tillsats är en klar lösning innan du fortsätter att tillsätta nästa lösningsmedel. Fysiska metoder som vortex, ultraljud eller varmt vattenbad kan användas för att underlätta upplösningen.

Verkningsmekanism (Mechanism of Action)

Targets/IC₅₀/Ki	progestogen Receptor
In vitro	Progesterone has biphasic effects on proliferation of breast cancer cells; it stimulates growth in the first cell cycle, then arrests cells at G1/S of the second cycle accompanied by up-regulation of the cyclin-dependent kinase inhibitor, p21. This compound-mediated transcription is further prevented by overexpression of E1A, suggesting that CBP/p300 is required. It drives a series of events where luminal cells probably provide Wnt4 and RANKL signals to basal cells which in turn respond by upregulating their cognate receptors, transcriptional targets and cell cycle markers. This hormone treatment increases the sensitivity of cortical synaptoneurosomes to GABA (i.e., decreased the EC50) and increases the maximal efficacy with which GABA stimulated Cl- transport (i.e., increased the Emax).
In vivo	Progesterone blocks the beneficial effect of estrogen on Abeta accumulation but not on behavioral performance in female 3xTg-AD mice. This compound significantly reduces tau hyperphosphorylation when administered both alone and in combination with estrogen. Progesterone-treated rats are less impaired on a Morris water maze spatial navigation task than rats treated with the oil vehicle. This compound-treated rats also show less neuronal degeneration 21 days after injury in the medial dorsal thalamic nucleus, a structure that has reciprocal connections with the contused area.
Referenser	[1] https://pubmed.ncbi.nlm.nih.gov/9553133/ [2] https://pubmed.ncbi.nlm.nih.gov/20445538/ [3] https://pubmed.ncbi.nlm.nih.gov/8392205/ [4] https://pubmed.ncbi.nlm.nih.gov/18045930/ [5] https://pubmed.ncbi.nlm.nih.gov/7925843/

Klinisk prövningsinformation (Clinical Trial Information)

(data från https://clinicaltrials.gov, uppdaterad den 2024-05-22)

NCT-nummer	Rekrytering	Tillstånd	Sponsor/Samarbetspartners	Startdatum	Faser
NCT06089395	Not yet recruiting	Poor Ovarian Response	Shi Yun\|Capital Medical University\|Dongzhimen Hospital Beijing	June 1 2024	Early Phase 1
NCT06359457	Not yet recruiting	Primary Dysmenorrhea	Cairo University	May 2024	--
NCT06334315	Not yet recruiting	Contraception\|Pharmacogenomic Drug Interaction	Yale University\|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)	May 2024	Phase 4

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