1. GPCR/G Protein
    Neuronal Signaling
  2. Orexin Receptor (OX Receptor)
  3. SB-649868

SB-649868 (Synonyms: GSK649868)

製品番号: HY-10806 純度: 99.88%
取扱説明書

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).

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SB-649868 構造式

SB-649868 構造式

CAS 番号 : 380899-24-1

容量 価格(税別) 在庫状況 数量
10 mM * 1  mL in DMSO USD 441 在庫あり
Estimated Time of Arrival: December 31
1 mg USD 180 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 420 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 660 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 1320 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 2340 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 3540 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

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製品説明

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).

IC50 & Target

pKi: 9.4 (OX1), 9.5 (OX2)[1]

体外実験

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) [1]. 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[2].

体内実験

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 (Clp=24 mL/min/kg), short half-life of (<0.6 h) and a low volume of distribution (Vss=1.1 l/kg), coupled with excellent oral bioavailability (F=85%) and good exposure in plasma (Cmax=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 and 10 mg/kg po) [1]. From dissociation kinetic studies using [3H]ACT-078573, the calculated long half-life, (t1/2) supports the non-surmountability profile of SB-649868 (t1/2=35.91 min) at OX1 orexin receptor. The long or moderately long t1/2values for SB-649868 at OX2 orexin receptor (t1/2=8.09 min)[2].

臨床実験
分子量

477.55

分子式

C₂₆H₂₄FN₃O₃S

CAS 番号

380899-24-1

SMILES

O=C(C1=C(C2=CC=C(F)C=C2)SC(C)=N1)N3CCCC[[email protected]]3CNC(C4=C(C=CO5)C5=CC=C4)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (209.40 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0940 mL 10.4701 mL 20.9402 mL
5 mM 0.4188 mL 2.0940 mL 4.1880 mL
10 mM 0.2094 mL 1.0470 mL 2.0940 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献
細胞実験
[2]

Chinese Hamster Ovary (CHO) cells stably transfected with human OX1 orexin receptor are cultured in Dulbecco's modified Eagle's medium F12 Ham, supplemented with 10% fetal bovine serum (FBS), 2 mg/mL glutamine, 600 μg/ml geneticin at 37 °C in an atmosphere of 95% air and 5% CO2. CHO cells stably transfected with human OX2 orexin receptor are cultured in alpha-MEM supplemented with 10% FBS, 100 units/mL penicillin G, 100 units/mL streptomycin and 400 μg/mL geneticin, at 37 °C in an atmosphere of 95% air and 5% CO2. Accumulation of IP1 is measured using IP-One HTRF terbium cryptate-based assay. OX1-CHO cells are seeded into white 384-well plate at the cell density of 1×104 cells per well and cultured for 24 h in the presence of 5 mM sodium butyrate while OX2-CHO cells are seeded at the cell density of 4×104 cells per well and cultured for 24 h in culture medium. After washings Hank's Balanced Salt Solution (HBSS) at room temperature containing 20 mM HEPES pH 7.4, 50 mM, LiCl and 0.1% Bovine Serum Albumin (BSA) cells are pre-incubated for 45 min with antagonist and then treated with agonist for 60 min at 37 °C. Detection reagents, IP1-d2 tracer and anti-IP1-cryptate are diluted in lysis buffer and added to the cells. Following 60 min incubation at room temperature, time-resolved fluorescence at 615 nm and 665 nm are measured with Envision Multilabel flash lamp reader with 100 flashes and 400 μs integration time[2].

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参考文献
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Keywords:

SB-649868GSK649868SB649868SB 649868GSK 649868GSK-649868Orexin Receptor (OX Receptor)Hypocretin ReceptorHCRT ReceptorInhibitorinhibitorinhibit

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製品名:
SB-649868
製品番号:
HY-10806
数量:
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