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SB-649868

Product Name
SB-649868
CAS No.
380899-24-1
Chemical Name
SB-649868
Synonyms
CS-2650;SB-649868;GSK649868;SB649868; SB 649868;SB-649868, CID25195495;(S)-N-((1-(5-(4-Fluorophenyl)-2-methylthiazole-4-carbonyl)piperidin-2-yl)methyl)benzofuran-4-carboxamide;N-[[(2S)-1-[[5-(4-Fluorophenyl)-2-methyl-4-thiazolyl]carbonyl]-2-piperidinyl]methyl]-4-benzofurancarboxamide;4-Benzofurancarboxamide, N-[[(2S)-1-[[5-(4-fluorophenyl)-2-methyl-4-thiazolyl]carbonyl]-2-piperidinyl]methyl]-;N-[[(2S)-1-[5-(4-FLUOROPHENYL)-2-METHYL-1,3-THIAZOLE-4-CARBONYL]PIPERIDIN-2-YL]METHYL]-1-BENZOFURAN-4-CARBOXAMIDE;GSK 649868,Inhibitor,SB-649868,HCRT Receptor,GSK-649868,Orexin Receptor (OX Receptor),Hypocretin Receptor,SB 649868,inhibit,SB649868
CBNumber
CB62628381
Molecular Formula
C26H24FN3O3S
Formula Weight
477.55
MOL File
380899-24-1.mol
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SB-649868 Property

Boiling point:
725.1±55.0 °C(Predicted)
Density 
1.305±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMF: 15mg/mL; DMF:PBS (pH 7.2) (1:20): 0.04mg/mL; DMSO: 10mg/mL; Ethanol: 0.3mg/mL
form 
A crystalline solid
pka
14.54±0.46(Predicted)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
29477
Product name
SB-649868
Packaging
1mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
29477
Product name
SB-649868
Packaging
25mg
Price
$533
Updated
2024/03/01
Cayman Chemical
Product number
29477
Product name
SB-649868
Packaging
5mg
Price
$139
Updated
2024/03/01
Cayman Chemical
Product number
29477
Product name
SB-649868
Packaging
10mg
Price
$243
Updated
2024/03/01
ChemScene
Product number
CS-7584
Product name
SB-649868
Purity
99.35%
Packaging
1mg
Price
$180
Updated
2021/12/16
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SB-649868 Chemical Properties,Usage,Production

Biological Activity

SB-649868 is an orally active and selective orexin OX1 and OX2 receptor antagonist (at OX1 and OX2 receptors, pKi 9.4 and 9.5, respectively).

in vitro

SB-649868 is identified as one the most in vitro potent dual OX 1 and OX 2 receptor antagonist known at that time (pK i =9.4 and 9.5 at the OX 1 and OX 2 receptor, respectively) . SB-649868 antagonizes orexin-A-induced inositol 1 phosphate (IP1) accumulation with the following pK B value (OX 1 =9.67; OX 2 =9.64). It displaces the [ 3 < /sup> H]ACT-078573 receptor binding with the following pKi values: OX 1 =9.27; OX 2 =8.91. Increasing concentrations of SB-649868 (0.3 nM- 30 nM) induces a rightward shift of the orexin-A CRCs with a depression of the agonist efficacy suggesting a clear non-surmountable behavior. The calculated apparent pK b values are 9.67±0.03 and 9.64±0.07 for OX 1 and OX 2 .

in vivo

Pharmacokinetic studies in the male CD rat, performed at 1 mg/kg, iv and 3 mg/kg, po, demonstrate an excellent pharmacokinetic profile for a hypnotic agent featuring moderate clearance in plasma (Cl p =24 mL/min/kg), short half-life of (<0.6 h) and a low volume of distribution (V ss =1.1 l/kg), coupled with excellent oral bioavailability (F=85%) and good exposure in plasma (C max =333 ng/mL). A brain to blood ratio (B/B) of 0.1:1 is observed 1 h after iv administration, a value in line with the expected partition between the two compartments based on the lower tissue binding observed in vitro in brain tissues (fraction unbound/brain=5.28%) with respect to plasma proteins (fraction unbound/plasma=1.34%). SB-649868, administered orally 3 h before OX-A injection at doses of 1, 3 and 10 mg/kg, causes a dose-dependent reduction of OX-A induced grooming as measured by total time spent grooming and number of grooming bouts ( p <0.01 at 3 a nd 10 mg/kg po) . From dissociation kinetic studies using [ 3 H]ACT-078573, the calculated long half-life, (t 1/2 ) supports the non-surmountability profile of SB-649868 (t 1/2 =35.91 min) at OX 1 orexin receptor. The long or moderately long t 1/2 < /sub> values for SB-649868 at OX 2 orexin receptor (t 1/2 =8.09 min).

target

pKi: 9.4 (OX 1 ), 9.5 (OX 2 )

SB-649868 Preparation Products And Raw materials

Raw materials

Preparation Products

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SB-649868 Suppliers

China 30 United States 6 USA 1 Global 37
Nanjing Norris-Pharm Technology Co., Ltd
Tel
13901585132
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+86-25-52131256
Email
799750417@qq.com
Country
China
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8888
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MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4863
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58
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4153
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55
Shanghai Changyan Chem & Tech Co., Ltd.
Tel
021-021-20242659 18930833303
Fax
+86 (21) 2024-2659
Email
order@changyanchem.com
Country
China
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5008
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ShangHai Biochempartner Co.,Ltd
Tel
17754423994 17754423994
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QQ:2853530913
Email
2853530910@QQ.com
Country
China
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8011
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Jinan Yaoyan Pharmaceutical Co., Ltd.
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Fax
-
Email
jnyaoyan@163.com
Country
China
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3069
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58
Nanjing Qishi Biotechnology Co. Ltd.
Tel
19822610310
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3122922726@qq.com
Country
China
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1346
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58
Fan De(Beijing) Biotechnology Co., Ltd.
Tel
15911056312
Email
liming@bio-fount.com
Country
China
ProdList
9730
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58
Nanjing Meihao Pharmaceutical Technology Co., Ltd.
Tel
meitaochem@126.com
Email
meitaochem@126.com
Country
China
ProdList
19105
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58
InvivoChem
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+1-708-310-1919 +1-13798911105
Fax
708-557-7486
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sales@invivochem.cn
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United States
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380899-24-1, SB-649868Related Search:

Sb-742457 SBI-0206965 SB9200 GSK-CXCR2 SBI-993 SB1317 SB 203580 SB 204741 SB1317

  • SB-649868
  • N-[[(2S)-1-[[5-(4-Fluorophenyl)-2-methyl-4-thiazolyl]carbonyl]-2-piperidinyl]methyl]-4-benzofurancarboxamide
  • N-[[(2S)-1-[5-(4-FLUOROPHENYL)-2-METHYL-1,3-THIAZOLE-4-CARBONYL]PIPERIDIN-2-YL]METHYL]-1-BENZOFURAN-4-CARBOXAMIDE
  • SB-649868, CID25195495
  • SB649868; SB 649868
  • CS-2650
  • 4-Benzofurancarboxamide, N-[[(2S)-1-[[5-(4-fluorophenyl)-2-methyl-4-thiazolyl]carbonyl]-2-piperidinyl]methyl]-
  • (S)-N-((1-(5-(4-Fluorophenyl)-2-methylthiazole-4-carbonyl)piperidin-2-yl)methyl)benzofuran-4-carboxamide
  • GSK649868
  • GSK 649868,Inhibitor,SB-649868,HCRT Receptor,GSK-649868,Orexin Receptor (OX Receptor),Hypocretin Receptor,SB 649868,inhibit,SB649868
  • 380899-24-1