1. GPCR/G Protein
  2. Orexin Receptor (OX Receptor)

SB-408124 

Cat. No.: HY-70068 Purity: 98.27%
Data Sheet SDS Handling Instructions

SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively; exhibits 50-fold selectivity over OX2 receptor.

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SB-408124 Chemical Structure

SB-408124 Chemical Structure

CAS No. : 288150-92-5

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 68 In-stock
5 mg USD 62 In-stock
10 mg USD 113 In-stock
100 mg USD 727 In-stock
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Description

SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively; exhibits 50-fold selectivity over OX2 receptor. IC50 Value: 57 nM(Ki) Target: OX1 Receptor in vitro: SB-408124 binds hypocretin type 1 receptor (HcrtR1) with pKi values of 7.57. Calcium mobilization studies shows that SB-408124 is a functional antagonist of the OX1 receptor with a affinity of approximately 50-fold selectivity over the OX2 receptor. A recent study indicates that pretreatment of primary cultures of rat astrocytes with SB-401824 before Orexin A administration significantly reduced the stimulatory action of Orexin A on both basal and forskolin-acivated cAMP production. in vivo: SB-408124 (30 μg/10 μL, administered intracerebroventricularly) decreases Orexin-A induced water intake in Wistar rats. Intracerebroventricularly administered Orexin-A (30 μg/10 μL) blocks the vasopressin (VP) level increase induced by either histamine or 2.5% NaCl administration, and this blocking effect is moderated by pretreatment with SB-408124. Intracerebroventricular pretreatment with SB-408124 (50 mM, 5 μL/h) prevents Bicuculline (BIC)-induced increases in endogenous glucose production (EGP).

References
Molecular Weight

356.37

Formula

C₁₉H₁₈F₂N₄O

CAS No.

288150-92-5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.27%

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Product Name:
SB-408124
Cat. No.:
HY-70068
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