288150-92-5
SB408124
CAS: 288150-92-5
Molecular Formula: C19H18F2N4O
288150-92-5 - Names and Identifiers
| Name | SB408124 |
| Synonyms | CS-1990 SB408124 SB 408124 SB408124 SB-408124, CID4331799 1-(6,8-difluoro-2-methylquinolin-4-yl)-3-(4-(dimethylamino)phenyl)urea N-(6,8-DIFLUORO-2-METHYL-4-QUINOLINYL)-N'-[4-(DIMETHYLAMINO)PHENYL]UREA Urea, N-(6,8-difluoro-2-methyl-4-quinolinyl)-N'-[4-(dimethylamino)phenyl]- SB 4081241-(6,8-difluoro-2-methylquinolin-4-yl)-3-(4-(dimethylamino)phenyl)urea |
| CAS | 288150-92-5 |
| EINECS | 604-604-1 |
288150-92-5 - Physico-chemical Properties
| Molecular Formula | C19H18F2N4O |
| Molar Mass | 356.37 |
| Density | 1.371 |
| Boling Point | 430.3±45.0 °C(Predicted) |
| Solubility | DMSO: ~24mg/mL |
| Appearance | solid |
| Color | olive-green |
| pKa | 12.12±0.43(Predicted) |
| Storage Condition | Sealed in dry,2-8°C |
| MDL | MFCD06411575 |
| Use | SB-408124 |
| In vitro study | SB-408124 binds to the hypocumin type 1 receptor (HcrtR1) with an Ki of 7.57 nM. Calcium mobilization studies have shown that SB-408124 is a functional antagonist of the OX1 receptor with specific affinity, SB-408124 50-fold more selective for the OX1 receptor than for the Orexin-2 receptor as measured in radioligand binding assays. Recent studies have shown that pretreatment of primary cultured rat astrocytes with SB-401824 followed by treatment with Orexin A significantly reduced the stimulation of Orexin A on basal and forskolin-activated cAMP production. |
| In vivo study | Treatment of Wistar rats with 30 μg/10 μL SB-408124 intracerebroventricular administration reduced Orexin-A-induced water intake. Intraventricular administration of Orexin-A (30 μg/10 μL) blocked the increase in vasopressin (VP) levels induced by histamine or 2.5% NaCl treatment, pretreatment with SB-408124 can modulate this blocking effect. SB-408124((50 mM, 5 μl/h) intracerebroventricular administration blocked the increase in endogenous glucose production (EGP) induced by Bicuculline(BIC). |
288150-92-5 - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
| WGK Germany | 3 |
288150-92-5 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.806 ml | 14.03 ml | 28.061 ml |
| 5 mM | 0.561 ml | 2.806 ml | 5.612 ml |
| 10 mM | 0.281 ml | 1.403 ml | 2.806 ml |
| 5 mM | 0.056 ml | 0.281 ml | 0.561 ml |
Last Update：2024-01-02 23:10:35
288150-92-5 - Reference Information
| biological activity | SB408124 is a non-peptide OX1 receptor antagonist that acts on whole cells and membranes, ki was 57 nM and 27 nM, respectively, which was 50 times more selective than the OX2 receptor. |
Last Update：2024-04-09 20:48:19
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