| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg | |||
| 10mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Emicerfont targets the corticotropin-releasing factor type 1 receptor (CRF1). It acts as an antagonist with an IC50 of 66 nM. By inhibiting CRF1 receptor activation, it reduces CRF-mediated activation of the hypothalamic-pituitary-adrenal (HPA) axis and decreases cortisol release and stress-induced symptoms.
|
|---|---|
| ln Vitro |
Emicerfont has an IC50 of 66 nM and functions as a corticotropin-releasing factor type 1 (CRF1) receptor antagonist[1].
In vitro, Emicerfont is a CRF1 receptor antagonist with an IC50 of 66 nM. It blocks CRF-mediated signaling at the receptor level, preventing downstream activation of the HPA axis. The compound's activity has been characterized in receptor binding and functional assays. |
| ln Vivo |
Emicerfont decreased defensive postures in marmosets and icv CRF-induced forepaw stepping in gerbils at a dosage of 10 mg/kg. At a dose of 30 mg/kg, emicerfont also lessens ultrasonic vocalizations in rat pups [1].
In vivo, Emicerfont (10 mg/kg) decreases intracerebroventricular CRF-induced gerbil forepaw treading and marmoset defensive postures. At 30 mg/kg, it reduces rat pup ultrasonic vocalization, an index of anxiety-like behavior. These effects demonstrate the compound's ability to block CRF-mediated stress responses in vivo. |
| Enzyme Assay |
For receptor binding assays, membranes from cells expressing human recombinant CRF1 receptors are incubated with radiolabeled CRF or a selective CRF1 ligand and varying concentrations of Emicerfont. Non-specific binding is determined using excess unlabeled competitor. Bound radioactivity is measured to calculate Ki or IC50 values.
|
| Cell Assay |
Cellular assays utilize cell lines expressing CRF1 receptors. Cells are pre-incubated with Emicerfont and then stimulated with CRF. Downstream signaling, such as cAMP accumulation or calcium mobilization, is measured using luminescent or fluorescent assays. Inhibition of CRF-stimulated signaling is used to determine antagonist potency.
|
| Animal Protocol |
In vivo studies are conducted in gerbils, marmosets, and rats. Emicerfont is administered orally or intraperitoneally. In gerbils, CRF-induced forepaw treading is assessed after intracerebroventricular CRF administration. In marmosets, defensive postures are scored. In rat pups, ultrasonic vocalizations are recorded as a measure of anxiety-like behavior.
|
| ADME/Pharmacokinetics |
Emicerfont (molecular weight 404.46) is a small-molecule CRF1 antagonist with good oral bioavailability. The compound has been advanced into Phase II clinical trials, indicating acceptable pharmacokinetic properties. It is typically formulated for oral administration.
|
| Toxicity/Toxicokinetics |
Preclinical and clinical toxicology studies have evaluated Emicerfont in animals and humans. As a CRF1 antagonist, the compound is expected to modulate stress responses and HPA axis function. Clinical trials have assessed its safety and tolerability in patients with anxiety disorders and IBS. The compound has shown a manageable safety profile.
|
| References | |
| Additional Infomation |
Emicerfont is an aromatic amine and tertiary amine compound. Emicerfont has been used in trials investigating the diagnosis and treatment of social anxiety disorder and irritable bowel syndrome (IBS).
Emicerfont (GW876008) is a CRF1 receptor antagonist that reached Phase II clinical trials for social anxiety disorder and irritable bowel syndrome. Its mechanism involves blocking CRF1 receptors, thereby reducing CRF-mediated activation of the HPA axis and stress-induced symptoms. By attenuating the stress response, the compound aims to reduce anxiety and improve gastrointestinal symptoms in stress-sensitive conditions. |
| Molecular Formula |
C22H24N6O2
|
|---|---|
| Molecular Weight |
404.46496
|
| Exact Mass |
404.196
|
| CAS # |
786701-13-1
|
| PubChem CID |
11223423
|
| Appearance |
Light yellow to brown solid powder
|
| LogP |
2.886
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
30
|
| Complexity |
635
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
JFHJGXQFESYQGY-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H24N6O2/c1-14-12-16(30-3)4-5-18(14)26-9-6-17-19(13-15(2)24-21(17)26)28-10-7-20(25-28)27-11-8-23-22(27)29/h4-5,7,10,12-13H,6,8-9,11H2,1-3H3,(H,23,29)
|
| Chemical Name |
1-[1-[1-(4-methoxy-2-methylphenyl)-6-methyl-2,3-dihydropyrrolo[2,3-b]pyridin-4-yl]pyrazol-3-yl]imidazolidin-2-one
|
| Synonyms |
GW-876008; GW 876008; GW876008
|
| 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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DCM :≥ 16.67 mg/mL (~41.22 mM)
|
|---|---|
| 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 | 2.4724 mL | 12.3619 mL | 24.7237 mL | |
| 5 mM | 0.4945 mL | 2.4724 mL | 4.9447 mL | |
| 10 mM | 0.2472 mL | 1.2362 mL | 2.4724 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA