ChemicalBook > CAS DataBase List > SB-649868

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;SB-649868, 10 mM in DMSO;(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
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)
color: White to off-white

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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

Uses

SB-649868 is a potent and selective orally active orexin (OX) 1 and OX2 receptor antagonist (pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively).

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 )

References

[1] Di Fabio R, et al. Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2receptor antagonist useful for treatment of sleep disorders. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5562-7. DOI:10.1016/j.bmcl.2011.06.086
[2] Faedo S, et al. Functional and binding kinetic studies make a distinction between OX1 and OX2 orexin receptorantagonists. Eur J Pharmacol. 2012 Oct 5;692(1-3):1-9. DOI:10.1016/j.ejphar.2012.07.007

SB-649868 Preparation Products And Raw materials

Raw materials

Preparation Products

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SB-649868 Suppliers

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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

SB-649868, 10 mM in DMSO

380899-24-1