| Identification | Back Directory | [Name]
SB408124 | [CAS]
288150-92-5 | [Synonyms]
CS-1990
SB 408124
SB 408214
SB408124 USP/EP/BP
SB 408124; SB408124
SB-408124, CID4331799
SB-408124 >=98% (HPLC), solid
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 | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C19H18F2N4O | [MDL Number]
MFCD06411575 | [MOL File]
288150-92-5.mol | [Molecular Weight]
356.37 |
| Chemical Properties | Back Directory | [Boiling point ]
430.3±45.0 °C(Predicted) | [density ]
1.371 | [storage temp. ]
2-8°C
| [solubility ]
DMSO: ~24 mg/mL
| [form ]
solid
| [pka]
12.12±0.43(Predicted) | [color ]
olive-green
| [InChI]
1S/C19H18F2N4O/c1-11-8-17(15-9-12(20)10-16(21)18(15)22-11)24-19(26)23-13-4-6-14(7-5-13)25(2)3/h4-10H,1-3H3,(H2,22,23,24,26) | [InChIKey]
JTARFZSNUAGHRB-UHFFFAOYSA-N | [SMILES]
CN(C)c1ccc(NC(=O)Nc2cc(C)nc3c(F)cc(F)cc23)cc1 |
| Safety Data | Back Directory | [Hazard Codes ]
Xi | [Risk Statements ]
36/37/38 | [Safety Statements ]
26-36 | [WGK Germany ]
3
| [Storage Class]
11 - Combustible Solids | [Hazard Classifications]
Eye Irrit. 2
Skin Irrit. 2
STOT SE 3 |
| Hazard Information | Back Directory | [Uses]
SB 408124 is a novel OX-1 antagonist. | [Definition]
ChEBI: 1-(6,8-difluoro-2-methyl-4-quinolinyl)-3-[4-(dimethylamino)phenyl]urea is a member of quinolines and an organohalogen compound. | [Biological Activity]
Selective non-peptide orexin OX 1 receptor antagonist (K b values are 21.7 and 1405 nM for human OX 1 and OX 2 receptors respectively). Blocks orexin-A induced grooming following oral administration in vivo . | [in vivo]
SB-408124 (30 μg/10 μl; i.c.v.; male Wistar rats) decreases Orexin-A induced water intake in Wistar rats[2]. | [IC 50]
OX1 Receptor: 57 nM (Ki, in whole cell ); OX1 Receptor: 27 nM (Ki, in cell membrane) | [storage]
Store at RT | [References]
[1] langmead cj1, jerman jc, brough sj, scott c, porter ra, herdon hj.characterisation of the binding of [3h]-sb-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor. br j pharmacol. 2004 jan;141(2):340-6.
[2] woldan-tambor a1, biegańska k, wiktorowska-owczarek a, zawilska jb. activation of orexin/hypocretin type 1 receptors stimulates camp synthesis in primary cultures of rat astrocytes. pharmacol rep. 2011;63(3):717-23.
[3] kis gk1, molnár ah, daruka l, gardi j, rákosi k, lászló f, lászló fa, varga c.the osmotically and histamine-induced enhancement of the plasma vasopressin level is diminished by intracerebroventricularly administered orexin in rats. pflugers arch. 2012 apr;463(4):531-6. |
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| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
|