Name: Levonorgestrel
Brand: Selleck Chemicals
SKU: S1727
Rating: 5 (5 reviews)

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Kvalitetskontroll (Quality Control)

Batch: Renhet: 99.95%

99.95

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

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

Molekylvikt	312.45	Formel	C₂₁H₂₈O₂	Lagring (från mottagningsdatumet)	3 år-20°Cpulver
CAS-nr	797-63-7	Ladda ner SDF		Lagring av stamlösningar	1 år-80°Ci lösningsmedel 1 månad-20°Ci lösningsmedel
Synonymer	D-Norgestrel			Smiles	CCC12CCC3C(C1CCC2(C#C)O)CCC4=CC(=O)CCC34

Löslighet (Solubility)

In vitro
Batch:

DMSO : 62 mg/mL (198.43 mM)
(Fuktkontaminerad DMSO kan minska lösligheten. Använd färk, vattenfri DMSO.)

Ethanol : 5 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.
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.
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	Progesterone receptor
In vitro	Levonorgestrel suppresses the stimulation of progesterone secretion induced by oLH, dibutyryl-cAMP and Pregnenolone in rats luteal cells. This compound also inhibits constrictions evoked by either a high potassium (K(+)) solution or phorbol myristate acetate (PMA) in the absence and presence of extracellular calcium (Ca(2+)). It depresses contractions evoked by Ca(2+) and reduces (45)Ca(2+) influx in depolarized veins. The chemical increases levels of cyclic AMP and inhibits PMA-induced activation of protein kinase C in veins. It causes endothelium-independent relaxations of jugular veins via inhibition of Ca(2+) entry and of protein kinase Cactivation. Its inhibition of both estrogen-induced pituitary weight increment and hyperprolactinemia is reduced by mifepristone, whereas Flutamide is unable to block this compound's effects
In vivo	Levonorgestrel down-regulates the mRNA expression of follicle-stimulating hormone receptor (FSHR), luteinizing hormone receptor (LHR), estrogen receptor (ER) β and progesterone receptor (PR) in the ovary, and ERα and PR in the uterus of Mongolian gerbils. This compound causes a significant upregulation of the mRNA expression of the gene encoding luteinising hormone β-subunit (lhβ) and the suppression of the mRNA expression of the gene encoding follicle-stimulating hormone β-subunit (fshβ) in the pituitary of both male and female roach. It disrupts the reproductive system of pubertalroach by affecting the pituitary gonadotropin expression and the sex steroid levels in pubertal roach (Rutilus rutilus).
Referenser	[1] https://pubmed.ncbi.nlm.nih.gov/8049144/ [2] https://pubmed.ncbi.nlm.nih.gov/10952682/ [3] https://pubmed.ncbi.nlm.nih.gov/1854838/ [4] https://pubmed.ncbi.nlm.nih.gov/21791876/ [5] https://pubmed.ncbi.nlm.nih.gov/24893273/

Klinisk prövningsinformation (Clinical Trial Information)

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

NCT-nummer	Rekrytering	Tillstånd	Sponsor/Samarbetspartners	Startdatum	Faser
NCT06380205	Recruiting	Healthy Participants	Incyte Corporation	May 7 2024	Phase 1
NCT06188026	Recruiting	Healthy Volunteers (Non-alcoholic Steatohepatitis)	Novo Nordisk A/S	December 18 2023	Phase 1
NCT05896384	Recruiting	Healthy	Boehringer Ingelheim	December 7 2023	Phase 1
NCT05700812	Recruiting	IUD\|IUD Insertion Complication\|IUD; Complications	University of California Davis	February 1 2023	Not Applicable
NCT05671653	Terminated	Obesity	Pfizer	January 19 2023	Phase 1

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Levonorgestrel Estrogen/progestogen Receptor Agonist

Molekylvikt: 312.45