SB408124

Alias: SB-408124; SB 408124; SB408124
Cat No.:V1307 Purity: ≥98%
SB408124 (SB-408124; SB 408124) is a potent, novel,selective, non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively, it exhibits 50-fold selectivity over OX2 receptor.
SB408124 Chemical Structure CAS No.: 288150-92-5
Product category: OX Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of SB408124:

  • SB408124 HCl
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

SB408124 (SB-408124; SB 408124) is a potent, novel, selective, non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively, it exhibits 50-fold selectivity over OX2 receptor. In primary astrocyte cultures from the rat cerebral cortex, pretreatment with SB408124 significantly reduced the orexin A a stimulating effect on basal-induced cAMP production and forskolin.

Biological Activity I Assay Protocols (From Reference)
Targets
OX1 Receptor ( Ki = 57 nM ); OX Receptor ( Ki = 27 nM )
ln Vitro

In vitro activity: SB-408124 binds to the hypocretin type 1 receptor (HcrtR1) with pKi values of 7.57. SB-408124 is a functional antagonist of the OX1 receptor with an affinity of roughly 50-fold selectivity over the OX2 receptor, according to calcium mobilization studies.[1] According to a recent study, pretreating primary rat astrocyte cultures with SB-401824 prior to Orexin A administration significantly lowered Orexin A's stimulatory effect on basal and forskolin-acivated cAMP production.[2]

ln Vivo
SB-408124 (30 μg/10 μL) reduces the amount of water induced by Orexin-A in Wistar rats. Orexin-A (30 μg/10 μL) given intracerebroventricularly inhibits the rise in vasopressin (VP) levels brought on by either histamine or 2.5% NaCl administration; this inhibitory effect is mitigated by SB-408124 pretreatment. [3] SB-408124 (50 mM, 5 μL/h) administered intracerebroventricularly precludes increases in endogenous glucose production (EGP) brought on by bicuculline (BIC). [4]
Animal Protocol
Dissolved in saline; 30 μg/10 μL; Intracerebroventricularly (i.c.v.) injected into the lateral ventricle of the rat.
Male Wistar rats
References

[1]. Br J Pharmacol . 2004 Jan;141(2):340-6.

[2]. Pharmacol Rep . 2011;63(3):717-23.

[3]. Pflugers Arch . 2012 Apr;463(4):531-6.

[4]. Diabetes . 2009 Sep;58(9):1998-2005.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H18F2N4O
Molecular Weight
356.37
Exact Mass
356.14
Elemental Analysis
C, 64.04; H, 5.09; F, 10.66; N, 15.72; O, 4.49
CAS #
288150-92-5
Appearance
Solid powder
SMILES
CC1=CC(=C2C=C(C=C(C2=N1)F)F)NC(=O)NC3=CC=C(C=C3)N(C)C
InChi Key
JTARFZSNUAGHRB-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H18F2N4O/c1-11-8-17(15-9-12(20)10-16(21)18(15)22-11)24-19(26)23-13-4-6-14(7-5-13)25(2)3/h4-10H,1-3H3,(H2,22,23,24,26)
Chemical Name
1-(6,8-difluoro-2-methylquinolin-4-yl)-3-[4-(dimethylamino)phenyl]urea
Synonyms
SB-408124; SB 408124; SB408124
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 36~50 mg/mL (101.0~101.0 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In Vivo)
30% propylene glycol, 5% Tween 80, 65% D5W: 30mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.8061 mL 14.0304 mL 28.0607 mL
5 mM 0.5612 mL 2.8061 mL 5.6121 mL
10 mM 0.2806 mL 1.4030 mL 2.8061 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • SB408124
    Total, specific and nonspecific binding of [3H]SB-674042 to (a) CHO-K1 whole cells stably expressing the OX1 receptor and (b) membranes from CHO-K1 cells expressing the OX1 receptor in SPA format, with increasing radioligand concentration.Br J Pharmacol.2004 Jan;141(2):340-6.
  • SB408124
    Time course for association and dissociation of [3H]SB-674042 binding to CHO-K1_OX1 whole cells.Br J Pharmacol.2004 Jan;141(2):340-6.
  • SB408124
    Competition for [3H]SB-674042 binding to CHO-K1_OX1 whole cells by orexin-A, orexin-B, SB-334867, SB-408124 and SB-410220.



    SB408124
    Competition for [3H]SB-674042 binding to membranes from CHO-K1_OX1 cells in SPA format by SB-334867, SB-408124 and SB-410220.Br J Pharmacol.2004 Jan;141(2):340-6.
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