NBI-27914 hydrochloride, IC-0296160
Product Introduction
NBI-27914 hydrochloride is a potent, selective, and orally active non-peptide antagonist of the corticotropin-releasing factor receptor 1 (CRF1). It exhibits high affinity for CRF1 with a Ki value in the low nanomolar range and demonstrates excellent selectivity over the CRF2 receptor subtype. By selectively blocking CRF1 signaling, NBI-27914 hydrochloride effectively inhibits the downstream release of adrenocorticotropic hormone (ACTH) and attenuates the hypothalamic-pituitary-adrenal (HPA) axis response to stress. This compound has been extensively utilized in preclinical research to investigate the role of CRF1 in stress-related disorders, anxiety, depression, and neuroendocrine regulation. In vivo studies have demonstrated that oral administration of NBI-27914 hydrochloride reduces stress-induced behaviors and normalizes HPA axis hyperactivity in rodent models, making it a valuable tool for studying the physiological and pathological roles of central CRF1 signaling.
Product Features
1. High Affinity and Selectivity: Potent and selective antagonist for CRF1 with nanomolar binding affinity and minimal cross-reactivity with CRF2.
2. Orally Bioavailable: Demonstrates good oral bioavailability, enabling convenient in vivo administration in rodent models for behavioral and neuroendocrine studies.
3. Functional Antagonism: Effectively blocks CRF-stimulated cAMP accumulation and ACTH release in vitro and in vivo.
4. Extensive Preclinical Validation: Widely cited in literature for investigating stress responses, anxiety-related behaviors, and HPA axis dysregulation.
5. Anxiolytic-Like Effects: Shown to reduce stress-induced behaviors in rodent models without significant sedative or off-target motor effects at effective doses.
Specifications
Size: Available in 1 mg and 10 mg
CAS Number: 1210627-24-1
Molecular Weight: 438.39
Molecular Formula: C18H21Cl2F3N4
Purity: ≥98%
Solubility: DMSO: ≥10 mg/mL
Storage and Stability
Storage Conditions: Store at -20°C or -80°C, protected from light. For reconstituted solutions, aliquot and store at -20°C or -80°C.
Shelf Life: The product is stable for 12 months from the date of manufacture when stored as directed. Avoid repeated freeze-thaw cycles.
Protocol (For Reference Only)
Important: Protect compound from light and moisture during handling and storage. Prepare stock solutions using anhydrous DMSO.
1. Stock Solution Preparation: Dissolve NBI-27914 hydrochloride in anhydrous DMSO to prepare a concentrated stock solution (e.g., 10-50 mM), aliquot into single-use vials, and store at -20°C or -80°C protected from light.
2. In Vitro Working Solution Preparation: Dilute DMSO stock solution into aqueous buffer or culture medium to achieve final working concentrations typically ranging from 10 nM to 10 µM depending on experimental design and CRF1 expression levels in the cell system.
3. In Vitro Treatment: Pre-incubate cells with NBI-27914 hydrochloride for 15-30 minutes prior to CRF stimulation, then assess downstream signaling by measuring cAMP accumulation, ACTH release, or intracellular calcium flux.
4. In Vivo Administration: For rodent studies, NBI-27914 hydrochloride may be administered via intraperitoneal injection or oral gavage; typical doses range from 1-20 mg/kg dissolved in an appropriate vehicle such as saline or a mixture of saline with low concentrations of solubilizing agents.
5. Behavioral Testing: Following compound administration, conduct behavioral assays such as elevated plus maze, open field test, or defensive withdrawal test to evaluate anxiolytic-like effects and stress-coping behaviors.
Precautions
1. Protect from light and moisture during handling and storage to maintain compound integrity.
2. Use appropriate vehicle controls in all experiments; DMSO concentration should not exceed 0.1% in cell culture to avoid cytotoxicity or off-target effects.
3. For in vivo studies, optimize vehicle formulation to ensure compound solubility and bioavailability while minimizing potential vehicle-related effects on behavior or neuroendocrine parameters.
4. NBI-27914 hydrochloride is a selective CRF1 antagonist; results should be interpreted in the context of CRF1-specific blockade and may not reflect effects mediated by CRF2 or other stress-related signaling pathways.
5. For research use only. Not for use in diagnostic or therapeutic procedures.
FAQ (Simplified)
Q1: What is the recommended starting concentration for in vitro CRF1 antagonism?
A1: Effective concentrations typically range from 100 nM to 1 µM depending on cell type and receptor expression level. Titration experiments starting from 10 nM to 10 µM are recommended to establish the optimal inhibitory concentration for specific assays.
Q2: Can NBI-27914 hydrochloride be used in vivo?
A2: Yes. NBI-27914 hydrochloride has been successfully administered via intraperitoneal injection and oral gavage at doses ranging from 1-20 mg/kg in rodent stress and anxiety models. Vehicle optimization is recommended for best results.
Q3: How should I store stock solutions?
A3: Prepare concentrated stock solutions in anhydrous DMSO, aliquot into single-use volumes to minimize freeze-thaw cycles, and store at -20°C for short-term or -80°C for long-term storage protected from light.
Q4: What is the selectivity profile of NBI-27914 hydrochloride?
A4: NBI-27914 hydrochloride exhibits high selectivity for CRF1 over CRF2, with reported Ki values in the low nanomolar range for CRF1 and negligible binding to CRF2 at concentrations up to 10 µM, making it a valuable tool for dissecting CRF1-specific signaling.
Disclaimer
1. For Research Use Only. Not for use in diagnostic or therapeutic procedures.
2. Due to the variable nature of biological research, optimization of conditions using a small-scale pilot experiment is strongly recommended before processing valuable samples.
3. This warranty is limited to the replacement of the product. The manufacturer assumes no liability for incidental or consequential damages, including loss of samples or data.
4. Wear appropriate protective clothing and gloves when handling this product.
Ordering Information
Catalog Number: IC-0296160
Product Name: NBI-27914 hydrochloride
Size: 1 mg / 10 mg
Price:
1 mg: CNY ¥2100.00 / USD $210.00 / EUR �252.00 / JPY ¥37800.00
10 mg: CNY ¥2875.00 / USD $287.50 / EUR �345.00 / JPY ¥51750.00
2023 Version
