Basic information Safety Supplier Related

SB 204741

Basic information Safety Supplier Related

SB 204741 Basic information

Product Name:
SB 204741
Synonyms:
  • SB 204741
  • N-(1-METHYL-1H-5-INDOLYL)-N'-(3-METHYL-5-ISOTHIAZOLYL)UREA
  • N-(1-METHYL-1H-INDOLYL-5-YL)-N''-(3-METHYL-5-ISOTHIAZOLYL)UREA
  • 1-(1-Methyl-1H-indol-5-yl)-3-(3-Methylisothiazol-5-yl)urea
  • 3-(3-METHYL-1,2-THIAZOL-5-YL)-1-(1-METHYLINDOL-5-YL)UREA
  • 1-(1-methyl-5-indolyl)-3-(3-methyl-5-isothiazolyl)urea
  • Urea, N-(1-methyl-1H-indol-5-yl)-N'-(3-methyl-5-isothiazolyl)-
  • human,inhibit,SB204741,5-HT Receptor,Inhibitor,remodeling,Serotonin Receptor,selective,SB 204741,isoproterenol-induced,affinity,SB-204741,5-hydroxytryptamine Receptor,myocardial
CAS:
152239-46-8
MF:
C14H14N4OS
MW:
286.35
Product Categories:
  • API
Mol File:
152239-46-8.mol
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SB 204741 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
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Safety Information

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

MSDS

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SB 204741 Usage And Synthesis

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is a member of ther class of ureas that is urea in which a hydrogen attached to one of the nitrogens has been replaced by an N-methylindol-5-yl group, while a hydrogen attached to the other nitrogen has been replaced by a 3-methyl-1,2-thiazol-5-yl group.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-HT2B Receptor: 7.1 (pKi)

storage

Room temperature

SB 204741Supplier

Chengdu Saint - Kay Biotechnology Co., Ltd. Gold
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028-85157043 15882256948
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676046971@qq.com
3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801 18930552037
Email
3bsc@sina.com
Syntechem Co.,Ltd
Tel
Email
info@syntechem.com
ChemStrong Scientific Co.,Ltd
Tel
0755-0755-66853366 13670046396
Email
sales@chem-strong.com
EMMX Biotechnology LLC
Tel
888-539-0666
Email
info@emmx.com
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