SB408124 - Moligand™, 10mM in DMSO , Antagonist of OX 1 receptor;Antagonist of OX 2 receptor, CAS No.288150-92-5, Antagonist of OX 1 receptor;Antagonist of OX 2 receptor

CAS: 288150-92-5 Cat. No.: S409055 分子式: C₁₉H₁₈F₂N₄O 分子量: 356.37 EC番号: 636-686-9 PubChem CID: 4331799

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

1-(6,8-difluoro-2-methylquinolin-4-yl)-3-(4-(dimethylamino)phenyl)urea

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

Information

SB408124 is a non-peptide antagonist forOX1 receptorwithKiof 57 nM and 27 nM in both whole cell and membrane, respectively, exhibits 50-fold selectivity over OX2 receptor.
In vitro

SB-408124 binds hypocretin type 1 receptor (HcrtR1) with pK_i values of 7.57. Calcium mobilization studies shows that SB-408124 is a functional antagonist of the OX1 receptor with a affinity of approximately 50-fold selectivity over the OX2 receptor. A recent study indicates that pretreatment of primary cultures of rat astrocytes with SB-401824 before Orexin A administration significantly reduced the stimulatory action of Orexin A on both basal and forskolin-acivated cAMP production.

In vivo

SB-408124 (30 μg/10 μL, administered intracerebroventricularly) decreases Orexin-A induced water intake in Wistar rats. Intracerebroventricularly administered Orexin-A (30 μg/10 μL) blocks the Vasotocin (VP) level increase induced by either histamine or 2.5% NaCl administration, and this blocking effect is moderated by pretreatment with SB-408124. Intracerebroventricular pretreatment with SB-408124 (50 mM, 5 μL/h) prevents Bicuculline (BIC)-induced increases in endogenous glucose production (EGP).
Cell Data

cell lines：LNCaP and PC-3 cell lines

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

同義語

1-(6,8-difluoro-2-methylquinolin-4-yl)-3-(4-(dimethylamino)phenyl)urea

仕様と純度

Moligand™, 10mM in DMSO

生化学的・生理学的メカニズム

SB408124 is a non-peptide antagonist for OX1 receptor with K_i of 57 nM and 27 nM in both whole cell and membrane, respectively, exhibits 50-fold selectivity over OX2 receptor.

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

等級

Moligand™

アクションタイプ

ANTAGONIST

作用メカニズム

Antagonist of OX 1 receptor;Antagonist of OX 2 receptor

名前と識別子

• 異性体SMILES: CC1=CC(=C2C=C(C=C(C2=N1)F)F)NC(=O)NC3=CC=C(C=C3)N(C)C
• WGKドイツ: 3
• PubChem CID: 4331799
• 分子量: 356.37

関連ターゲット（人間）

CYP1A2 Tchem Cytochrome P450 1A2 (1 Activities)

Discover Target: CYP1A2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HCRTR1 Tclin Orexin receptor type 1 (3 Activities)

Discover Target: HCRTR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

化学的性質と物理的性質

• 溶解度: Solubility (25°C) In vitro DMSO: 57 mg/mL (199.1 mM)