WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H319810
CAS#: 786701-13-1
Description: Emicerfont, also known as GW876008, is a CRF-1 antagonist. Emicerfont blocks the CRH-1 receptor, and so reduces ACTH release. It has been investigated for the treatment of irritable bowel syndrome and alcoholism, and while it was not effective enough to be adopted for medical use in these applications, it continues to be used for research, as the role of the CRH-ACTH system in IBS remains poorly understood.
Hodoodo Cat#: H319810
Name: Emicerfont
CAS#: 786701-13-1
Chemical Formula: C22H24N6O2
Exact Mass: 404.20
Molecular Weight: 404.474
Elemental Analysis: C, 65.33; H, 5.98; N, 20.78; O, 7.91
Synonym: GW876008; GW 876008; GW-876008; GW 876008X; GW-876008X; GW876008X; GW-876,008; Emicerfont.
IUPAC/Chemical Name: 1-(1-(1-(4-methoxy-2-methylphenyl)-6-methyl-2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyrazol-3-yl)imidazolidin-2-one
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)
SMILES Code: O=C1NCCN1C2=NN(C3=C4C(N(C5=CC=C(OC)C=C5C)CC4)=NC(C)=C3)C=C2
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info: Corticotropin releasing factor (CRF), also known as Corticotropin releasing hormone, is an endogenous peptide hormone which is released in response to various triggers such as chronic stress, and activates the two corticotropin-releasing hormone receptors CRH-1 and CRH-2. This then triggers the release of corticotropin (ACTH), another hormone which is involved in the physiological response to stress.
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The following data is based on the product molecular weight 404.47 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
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| In vivo protocol: |
1: Labus JS, Hubbard CS, Bueller J, Ebrat B, Tillisch K, Chen M, Stains J, Dukes
GE, Kelleher DL, Naliboff BD, Fanselow M, Mayer EA. Impaired emotional learning
and involvement of the corticotropin-releasing factor signaling system in
patients with irritable bowel syndrome. Gastroenterology. 2013
Dec;145(6):1253-61.e1-3. doi: 10.1053/j.gastro.2013.08.016. Epub 2013 Aug 14.
Review. PubMed PMID: 23954313; PubMed Central PMCID: PMC4069031.
2: Zorrilla EP, Heilig M, de Wit H, Shaham Y. Behavioral, biological, and
chemical perspectives on targeting CRF(1) receptor antagonists to treat
alcoholism. Drug Alcohol Depend. 2013 Mar 1;128(3):175-86. doi:
10.1016/j.drugalcdep.2012.12.017. Epub 2013 Jan 5. Review. PubMed PMID: 23294766;
PubMed Central PMCID: PMC3596012.
3: Hubbard CS, Labus JS, Bueller J, Stains J, Suyenobu B, Dukes GE, Kelleher DL,
Tillisch K, Naliboff BD, Mayer EA. Corticotropin-releasing factor receptor 1
antagonist alters regional activation and effective connectivity in an
emotional-arousal circuit during expectation of abdominal pain. J Neurosci. 2011
Aug 31;31(35):12491-500. doi: 10.1523/JNEUROSCI.1860-11.2011. PubMed PMID:
21880911; PubMed Central PMCID: PMC3399687.
4: Provera S, Rovatti L, Turco L, Mozzo S, Spezzaferri A, Bacchi S, Ribecai A,
Guelfi S, Mingardi A, Marchioro C, Papini D. A multi-technique approach using
LC-NMR, LC-MS, semi-preparative HPLC, HR-NMR and HR-MS for the isolation and
characterization of low-level unknown impurities in GW876008, a novel
corticotropin-release factor 1 antagonist. J Pharm Biomed Anal. 2010 Nov
2;53(3):517-25. doi: 10.1016/j.jpba.2010.06.012. Epub 2010 Jun 22. PubMed PMID:
20619567.
