1. GPCR/G Protein
    Neuronal Signaling
  2. Orexin Receptor (OX Receptor)
  3. SB-674042

SB-674042 

Cat. No.: HY-10898 Purity: 99.52%
COA Handling Instructions

SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd=5.03 nM), exhibits 100-fold selectivity for OX1 over OX2 receptors with IC50 values of 3.76 nM and 531 nM, respectively.

For research use only. We do not sell to patients.

SB-674042 Chemical Structure

SB-674042 Chemical Structure

CAS No. : 483313-22-0

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Solution
10 mM * 1 mL in DMSO USD 144 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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Estimated Time of Arrival: December 31
Solid
5 mg USD 131 In-stock
Estimated Time of Arrival: December 31
10 mg USD 218 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE SB-674042

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SB-674042 is a potent and selective non-peptide orexin OX1 receptor antagonist (Kd=5.03 nM), exhibits 100-fold selectivity for OX1 over OX2 receptors with IC50 values of 3.76 nM and 531 nM, respectively[1][4].

IC50 & Target[1][4]

OX1 Receptor

3.76 nM (IC50)

OX2 Receptor

531 nM (IC50)

OX1 Receptor

1.1 nM (Ki)

OX2 Receptor

129 nM (Ki)

In Vitro

SB-674042 ([3H]) (0.2-24 nM; 2 h) shows high-affinity and serves as a radio ligand suitable for labelling human OX1 receptors stably expressed in CHO cells[1].
SB-674042 (5 μM; 4 ℃ for 30 min, and 37 ℃ for 3 h) reduces the potency of CB1 receptor agonist (Rimonabant Hydrochloride, HY-14137) to phosphorylate ERK1/2 in HEK293 cells co-expressing the orexin-1 and CB1 receptors[2].
SB-674042 (1 μM; 24 h) eradicates the increase in mTOR phosphorylation in response to Orexin-A (HY-106224) (1 nM-1 μM; 24 h) in INS-1 cells, indicating activation of the mTOR pathway induced by orexin-A was dependent on the activated OX1 receptor[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[3]

Cell Line: INS-1 cells
Concentration: 1 μM
Incubation Time: 24 hours; accompanied with 1 μM Orexin-A for 24 hour
Result: Decreased the phosphorylation level of mTOR induced by Orexin-A.
In Vivo

SB-674042 (0.3 nM/0.3 μL; icv; single dose) reduces contextual and cues fear freezing responses in Stay animals in Stress Alternatives Model (SMA) in mice[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Stress-induced mice model (male C57BL/6NHsd mice, 22-26 g)[4]
Dosage: 0.3 nM/0.3 μL
Administration: Intracerebroventricular injection; subjected mice to 4 days of social aggression (days 1-4)
Result: Resulted 39.4% Escape and 60.6% Stay phenotypes among mice.
Molecular Weight

448.51

Formula

C24H21FN4O2S

CAS No.
SMILES

FC1=C(C2=C(C(N3[[email protected]](CC4=NN=C(C5=CC=CC=C5)O4)CCC3)=O)N=C(C)S2)C=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (55.74 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2296 mL 11.1480 mL 22.2960 mL
5 mM 0.4459 mL 2.2296 mL 4.4592 mL
10 mM 0.2230 mL 1.1148 mL 2.2296 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 1.43 mg/mL (3.19 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.43 mg/mL (3.19 mM); Clear solution

  • 3.

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

    Solubility: ≥ 1.43 mg/mL (3.19 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
SB-674042
Cat. No.:
HY-10898
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