| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
NBI-27914 targets the corticotropin-releasing factor 1 (CRF1) receptor, a G protein-coupled receptor that mediates the effects of corticotropin-releasing factor (CRF). CRF1 receptors are involved in the stress response, anxiety, depression, and seizure susceptibility. NBI-27914 is a selective, non-peptide antagonist at CRF1 receptors with no activity at CRF2 receptors.
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| ln Vitro |
NBI-27914 is a potent CRF1 receptor antagonist with a Ki of 1.7 nM. It shows high selectivity for CRF1 over CRF2 receptors. The compound blocks behavioral seizures in vivo, confirming its functional activity as a CRF1 receptor antagonist.
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| ln Vivo |
Both 4 and 24 hours after indomethacin treatment, NBI 27914 (3~30 mg/kg; intraperitoneal injection) hydrochloride reduces referred abdominal discomfort at the highest dose studied [1]. NBI 27914 (1~10 mg/kg; ip) hydrochloride reduces Freund's full adjuvant-induced mechanical hyperalgesia in a dose-dependent manner. The hydrochloride drug NBI 27914 (10 mg/kg) reverses thermal hyperalgesia. With minimal effective doses of 5 and 10 mg/kg, respectively, NBI 27914 hydrochloride can lessen mechanical hyperalgesia and tactile allodynia brought on by spinal nerve ligation [1]. In synchronized electroencephalograms recorded from the amygdala, higher dosages of NBI 27914 hydrochloride inhibit behavioral seizures and prevent epileptic discharges [2].
NBI-27914 blocks behavioral seizures in vivo. In animal models of epilepsy or seizure susceptibility, NBI-27914 reduces seizure frequency or severity. The compound has also been used to study the role of the CRF system in stress-induced behaviors and anxiety. |
| Enzyme Assay |
CRF1 receptor binding affinity is assessed using radioligand binding assays with membrane preparations from cells expressing human CRF1 receptors. Competitive binding experiments are performed using [¹²⁵I]-sauvagine or [³H]-CRF as radioligands. NBI-27914 is incubated at various concentrations, and Ki values are calculated from displacement curves. Selectivity against CRF2 receptors is confirmed using appropriate assays.
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| Cell Assay |
CRF1 receptor antagonism is assessed in functional assays such as CRF-stimulated cAMP accumulation (CRF1 is coupled to Gs and stimulates adenylyl cyclase). Cells expressing human CRF1 are treated with CRF in the presence or absence of NBI-27914. The compound's ability to block CRF-induced cAMP accumulation is measured, and IC50 or Kb values are calculated.
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| Animal Protocol |
Animal/Disease Models: Male CD-1 mice (20~25 g) [1]
Doses: 3~30 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: At the highest tested dose, the abdominal pain caused was diminished at 4 hrs (hrs (hours)) and 24 Are effective after hrs (hrs (hours)) - indomethacin dose. NBI-27914 is administered to animals in models of stress, anxiety, depression, or epilepsy. In seizure models, the compound is typically administered intraperitoneally or orally prior to seizure induction. Seizure frequency, latency, and severity are monitored. In stress models, behavioral endpoints such as anxiety-like behavior (e.g., elevated plus maze, open field test) are assessed. |
| ADME/Pharmacokinetics |
NBI-27914 HCl has a molecular weight of 470.65 and molecular formula C18H21Cl5N4. The IUPAC name is 5-chloro-4-N-(cyclopropylmethyl)-2-methyl-4-N-propyl-6-N-(2,4,6-trichlorophenyl)pyrimidine-4,6-diamine;hydrochloride. Purity is typically >99%. The compound is soluble in ethanol and DMSO. NBI-27914 is a selective CRF1 receptor antagonist and is used as a research tool in neuroscience and psychiatry.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of NBI-27914 have not been extensively reported. The compound has been used in animal studies at various doses without significant adverse effects reported. As a CRF1 receptor antagonist, mechanism-based toxicities may include effects on the hypothalamic-pituitary-adrenal (HPA) axis and stress responses. Standard safety precautions should be followed when handling the compound.
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| References |
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| Additional Infomation |
NBI-27914 HCl (CAS#: 1215766-76-9) is a selective, non-peptide CRF1 receptor antagonist with a Ki of 1.7 nM. It has no activity at CRF2 receptors. The compound blocks behavioral seizures in vivo and is a valuable research tool for studying the CRF system in stress, anxiety, depression, and epilepsy. It is intended for research use only.
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| Molecular Formula |
C18H21CL5N4
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| Molecular Weight |
470.65113902092
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| Exact Mass |
468.02
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| CAS # |
1215766-76-9
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| Related CAS # |
NBI-27914;184241-44-9
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| PubChem CID |
45073446
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
27
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| Complexity |
441
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCN(CC1CC1)C2=NC(=NC(=C2Cl)NC3=C(C=C(C=C3Cl)Cl)Cl)C.Cl
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| InChi Key |
CPMGENCTAWBLNW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H20Cl4N4.ClH/c1-3-6-26(9-11-4-5-11)18-15(22)17(23-10(2)24-18)25-16-13(20)7-12(19)8-14(16)21;/h7-8,11H,3-6,9H2,1-2H3,(H,23,24,25);1H
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| Chemical Name |
5-chloro-4-N-(cyclopropylmethyl)-2-methyl-4-N-propyl-6-N-(2,4,6-trichlorophenyl)pyrimidine-4,6-diamine;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1247 mL | 10.6236 mL | 21.2472 mL | |
| 5 mM | 0.4249 mL | 2.1247 mL | 4.2494 mL | |
| 10 mM | 0.2125 mL | 1.0624 mL | 2.1247 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.
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.
(2) Be sure to add the solvent(s) in order.
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