SB408124
Modify Date: 2024-01-05 17:17:10
SB408124 structure
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Common Name | SB408124 | ||
|---|---|---|---|---|
| CAS Number | 288150-92-5 | Molecular Weight | 356.369 | |
| Density | 1.4±0.1 g/cm3 | Boiling Point | 430.3±45.0 °C at 760 mmHg | |
| Molecular Formula | C19H18F2N4O | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | 214.0±28.7 °C | |
| Symbol |
GHS07 |
Signal Word | Warning | |
Use of SB408124SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively; exhibits 50-fold selectivity over OX2 receptor.IC50 Value: 57 nM(Ki)Target: OX1 Receptorin vitro: SB-408124 binds hypocretin type 1 receptor (HcrtR1) with pKi 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 vasopressin (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). |
| Name | 1-(6,8-difluoro-2-methylquinolin-4-yl)-3-[4-(dimethylamino)phenyl]urea |
|---|---|
| Synonym | More Synonyms |
| Description | SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively; exhibits 50-fold selectivity over OX2 receptor.IC50 Value: 57 nM(Ki)Target: OX1 Receptorin vitro: SB-408124 binds hypocretin type 1 receptor (HcrtR1) with pKi 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 vasopressin (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). |
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| Related Catalog | |
| References |
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Boiling Point | 430.3±45.0 °C at 760 mmHg |
| Molecular Formula | C19H18F2N4O |
| Molecular Weight | 356.369 |
| Flash Point | 214.0±28.7 °C |
| Exact Mass | 356.144867 |
| PSA | 57.26000 |
| LogP | 4.53 |
| Appearance of Characters | solid | olive-green |
| Vapour Pressure | 0.0±1.0 mmHg at 25°C |
| Index of Refraction | 1.697 |
| Storage condition | 2-8°C |
| Water Solubility | DMSO: ~24 mg/mL |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H315-H319-H335 |
| Precautionary Statements | P261-P305 + P351 + P338 |
| Personal Protective Equipment | dust mask type N95 (US);Eyeshields;Gloves |
| Hazard Codes | Xi: Irritant; |
| Risk Phrases | R36/37/38 |
| Safety Phrases | 26-36 |
| RIDADR | NONH for all modes of transport |
| WGK Germany | 3 |
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A major role for perifornical orexin neurons in the control of glucose metabolism in rats.
Diabetes 58(9) , 1998-2005, (2009) The hypothalamic neuropeptide orexin influences (feeding) behavior as well as energy metabolism. Administration of exogenous orexin-A into the brain has been shown to increase both food intake and blo... |
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Hypocretin/orexin type 1 receptor in brain: role in cardiovascular control and the neuroendocrine response to immobilization stress.
Am. J. Physiol. Regul. Integr. Comp. Physiol. 292(1) , R382-7, (2007) Hypocretin/orexin acts pharmacologically in the hypothalamus to stimulate stress hormone secretion at least in part by an action in the hypothalamic paraventricular nucleus, where the peptide's recept... |
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Modulation of respiratory activity by hypocretin-1 (orexin A) in situ and in vitro.
Adv. Exp. Med. Biol. 669 , 109-13, (2010) Release of hypocretins (orexins) by neurons in the lateral hypothalamus is an important contributor to arousal state, thermoregulation, feeding behavior, and has recently been proposed to play a role ... |
| 1-(6,8-Difluoro-2-methyl-4-quinolinyl)-3-[4-(dimethylamino)phenyl]urea |
| MFCD06411575 |
| S1545_Selleck |
| SB-408,124 |
| Urea, N-(6,8-difluoro-2-methyl-4-quinolinyl)-N'-[4-(dimethylamino)phenyl]- |
| 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 |
| SB-408124 |