ChemicalBook CAS DataBase List 152239-46-8

152239-46-8

Name	SB 204741
CAS	152239-46-8
Molecular Formula	C14H14N4OS
MDL Number	MFCD00923644
Molecular Weight	286.35
MOL File	152239-46-8.mol

Chemical Properties

Melting point	>195°C (dec.)
storage temp.	2-8°C
solubility	DMSO: ~18 mg/mL, soluble
form	solid
color	orange
Stability:	Hygroscopic
InChI	InChI=1S/C14H14N4OS/c1-9-7-13(20-17-9)16-14(19)15-11-3-4-12-10(8-11)5-6-18(12)2/h3-8H,1-2H3,(H2,15,16,19)
InChIKey	USFUFHFQWXDVMH-UHFFFAOYSA-N
SMILES	N(C1C=CC2=C(C=1)C=CN2C)C(NC1SN=C(C)C=1)=O

Safety Data

Hazard Codes	Xi
Risk Statements	36/37/38 less more
Safety Statements	26-36 less more
WGK Germany	3

Hazard Information

Uses

SB 204741 is a potent, selective SR-2B antagonist.

Definition

ChEBI: 1-(1-methylindol-5-yl)-3-(3-methyl-1,2-thiazol-5-yl)urea is a member of ther class of ureas that is urea in which a hydrogen attached to one of the nitrogens has been replaced by an N-methylindol-5-yl group, while a hydrogen attached to the other nitrogen has been replaced by a 3-methyl-1,2-thiazol-5-yl group. It is a potent and selective antagonist for the 5-hydroxytryptamine 2B (5-HT2B) receptor. It has a role as a receptor modulator and a serotonergic antagonist. It is a member of ureas, a member of indoles and a member of 1,2-thiazoles.

Biological Activity

Potent and selective 5-HT 2B receptor antagonist (pA 2 = 7.95). Displays ≥ 135-fold selectivity over 5-HT 2C (pK i = 5.82), 5-HT 2A (pK i < 5.2), 5-HT 1A , 1D , 1E , 5-HT 3 and 5-HT 4 receptors.

in vivo

SB-204741 (0.25~1.0 mg/kg; i.p.) induces myocardial remodeling and dose dependently improves hemodynamic and ventricular functions following isoproterenol-induced myocardial injury^[1].
SB-204741 bolsters endogenous anti-oxidant enzymes activities, improves cardiac injury markers, NO level and lipid peroxidation level and attenuates TNFα level in isoproterenol-induced myocardial remodeling in rats. SB-204741 (0.5 and 1.0 mg/kg/day) pre-treatment for 28 days significantly amplifies NO level and GSH and SOD activities and attenuates TBARS level following isoproterenol-induced myocardial remodeling. SB-204741 inhibits inflammatory protein expression, upregulates autophagy and HSPs protein expressions in isoproterenol-induced myocardial remodeling in rats. SB-204741 improves myocardial architecture in isoproterenol-induced myocardial remodeling in rats^[1].

Animal Model:	Rats^[1]
Dosage:	0.25~1.0 mg/kg
Administration:	I.p.
Result:	Induced myocardial remodeling.

IC 50

human 5-HT_2B Receptor: 7.1 (pKi)

storage

Store at 2-8℃

Spectrum Detail

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