country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Art. -Nr.: HY-122608

Copy Link Print Information

Samelisant free base

(Synonyms: SUVN-G3031 free base)

Samelisant (SUVN-G3031) free base is a potent and selective histamine H3 receptor (H3R) inverse agonist with good brain penetration and oral bioavailability. Samelisant free base has a similar binding affinity towards human (hH3R; K_i=8.7 nM) and rat (rH3R;K_i=9.8 nM) H3R indicating no inter-species differences. Samelisant free base can be used for the research of sleep-related disorders.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 1394808-82-2
Formel: C₂₁H₃₁N₃O₃
Molecular Weight:373.49

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (269 KB)

Samelisant free base Chemical Structure

CAS. Nr.: 1394808-82-2

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

Samelisant free base displays inverse agonist activity and it exhibits very high selectivity towards H3R. The pEC₅₀ value of histamine (8.5) for human H3 receptor increases to 8.2, 7.3 and 6.2 after treatment with 1, 10 and 100 nM of Samelisant, respectively. The pEC₅₀ value of histamine (8.2) for rat H3 receptor increases to 7.9, 7.4 and 6.4 after treatment with 1, 10 and 100 nmol/L of Samelisant, respectively^[1].
Samelisant free base binds to the orthosteric site in a reversible manner with K_b values of 1.3 nM and 1.1 nM deduced from pA₂ value for human and rat H3R, respectively^[1].
Samelisant free base also modulates dopamine and norepinephrine levels in the cerebral cortex while it has no effects on dopamine levels in the striatum or nucleus accumbens^[1].

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

In Vivo

Treatment with Samelisant (10 and 30 mg/kg, p.o.) free base produces a significant increase in wakefulness with a concomitant decrease in non-rapid eye movement sleep (NREM) sleep in orexin knockout mice subjected to sleep electroencephalography (EEG)^[1].
Samelisant free base also produces a significant decrease in direct rapid eye movement (REM) sleep onset (DREM) episodes, demonstrating its anticataplectic effects in an animal model relevant to narcolepsy^[1].
Samelisant free base treatment in mice produces a dose-dependent increase in tele-methylhistamine levels indicating the activation of histaminergic neurotransmission^[1].

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

Animal Model:

Male Wistar rats or male C57BL6J mice^[1]
Dosage:

1, 3, 10, and 30 mg/kg
Administration:

Oral administration
Result:

Produced a dose-dependent increase in t-MH levels in the frontal cortex, hypothalamus and cerebrospinal fluid (CSF) of male Wistar rats. Produced a significant increase in t-MH levels of the frontal cortex, striatum and hypothalamus in mice.

Chemical Information

CAS. Nr. 1394808-82-2
Molecular Weight 373.49
Formel C₂₁H₃₁N₃O₃
SMILES

O=C(NC1=CC=C(OC2CCN(C3CCC3)CC2)C=C1)CN4CCOCC4
Synonyms

SUVN-G3031 free base
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Nirogi R, et al. Samelisant (SUVN-G3031), a potent, selective and orally active histamine H3 receptor inverse agonist for the potential treatment of narcolepsy: pharmacological and neurochemical characterisation. Psychopharmacology (Berl). 2021 Jun;238(6) [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

Minimum order quantity

100 mg

Angebot einholen Auf Lager

Other size

Angebot einholen

Amount: USD 0.00

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

Samelisant free base

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

Samelisant free base Related Classifications

HY-122608 Related Classifications