Product Details
Product Name:
SB-674042 |
CAS No.:
483313-22-0 |
Purity:
99.9% |
Supply Ability:
10g |
Release date:
2024/11/19 |
Product Introduction
Bioactivity
Name | SB-674042 |
Description | SB-674042 is a potent, selective dual antagonist of the non-peptide orexigenic peptides OX1 and OX2 receptors, with IC50 values of 3.76 nM and 531 nM, respectively. SB-674042 is suitable for the treatment of depression. |
In vitro | [(3)H]SB-674042 is a specific, high-affinity radioligand for the OX(1) receptor. Specific binding of [(3)H]SB-674042 was saturable in both whole cell and membrane formats. Analyses suggested a single high-affinity site, with K(d) values of 3.76+/-0.45 and 5.03+/-0.31 nM[1]。Treatment of cells co-expressing the orexin-1 and CB1 receptors with the orexin-1 receptor antagonist SB-674042 also resulted in re-localization of both receptors to the cell surface. Treatment with SB-674042 also reduced the potency of a CB1 receptor agonist to phosphorylate ERK1/2 only when the two receptors were co-expressed[4]. |
In vivo | In the Stress Alternatives Model (SMA) in mice, administration of SB-674042 at a dose of 0.3 nM/0.3 μL via icv (intracerebroventricular injection) reduces contextual and cue fear freezing responses in Stay animals[2]. |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 20 mg/mL (44.59 mM), Sonication is recommended.
|
Keywords | SB 674042 | SB-674042 |
Inhibitors Related | L-368,899 hydrochloride | IPSU | MK-3697 | Filorexant | Orexin B, rat, mouse Acetate | OXA (17-33) acetate | PF3274167 | ACT-462206 | Seltorexant | TCS 1102 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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