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SB-649868
CAS No. 380899-24-1
SB-649868( SB 649868 | SB649868 )
Catalog No. M14316 CAS No. 380899-24-1
A potent, selective, orally bioavailable, dual orexin OX1/OX2R antagonist with pKi of 9.4 and 9.5 respectively.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 293 | In Stock |
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| 10MG | 461 | In Stock |
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| 25MG | 750 | In Stock |
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| 50MG | 1035 | In Stock |
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| 100MG | 1395 | In Stock |
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| 200MG | Get Quote | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameSB-649868
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NoteResearch use only, not for human use.
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Brief DescriptionA potent, selective, orally bioavailable, dual orexin OX1/OX2R antagonist with pKi of 9.4 and 9.5 respectively.
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DescriptionA potent, selective, orally bioavailable, dual orexin OX1/OX2R antagonist with pKi of 9.4 and 9.5 respectively; displays >1,000-fold selectivity for the orexin target receptors in a broad panel of GPCRs, ion channels and enzymes; demonstrates high effectivity in pre-clinical model of sleep disorders.Sleep Disorder Phase 2 Discontinued(In Vitro):SB-649868 is identified as one the most in vitro potent dual OX1 and OX2 receptor antagonist known at that time (pKi=9.4 and 9.5 at the OX1 and OX2 receptor, respectively) . SB-649868 antagonizes orexin-A-induced inositol 1 phosphate (IP1) accumulation with the following pKB value (OX1=9.67; OX2=9.64). SB-649868 displaces the [3H]ACT-078573 receptor binding with the following pKi values: OX1=9.27; OX2=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 pKb values are 9.67±0.03 and 9.64±0.07 for OX1 and OX2.
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In VitroSB-649868 is identified as one the most in vitro potent dual OX1 and OX2 receptor antagonist known at that time (pKi=9.4 and 9.5 at the OX1 and OX2 receptor, respectively) . SB-649868 antagonizes orexin-A-induced inositol 1 phosphate (IP1) accumulation with the following pKB value (OX1=9.67; OX2=9.64). SB-649868 displaces the [3H]ACT-078573 receptor binding with the following pKi values: OX1=9.27; OX2=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 pKb values are 9.67±0.03 and 9.64±0.07 for OX1 and OX2.
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In Vivo——
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SynonymsSB 649868 | SB649868
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PathwayGPCR/G Protein
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TargetOrexin Receptor
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RecptorOrexin Receptor
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Research AreaNeurological Disease
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IndicationSleep Disorder
Chemical Information
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CAS Number380899-24-1
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Formula Weight477.554
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Molecular FormulaC26H24FN3O3S
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 100 mg/mL (209.40 mM)
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SMILESO=C(C1=C2C=COC2=CC=C1)NC[C@H]3N(C(C4=C(C5=CC=C(F)C=C5)SC(C)=N4)=O)CCCC3
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Chemical Name(S)-N-((1-(5-(4-fluorophenyl)-2-methylthiazole-4-carbonyl)piperidin-2-yl)methyl)benzofuran-4-carboxamide
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Renzulli C, et al. Drug Metab Dispos. 2011 Feb;39(2):215-27.
2. Bettica P, et al .Neuropsychopharmacology. 2012 Apr;37(5):1224-33.
3. Piccoli L, et al. Neuropsychopharmacology. 2012 Aug;37(9):1999-2011.
4. Di Fabio R, et al. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5562-7.
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