E2508

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 561361

CAS#: 685886-34-4

Description: E2508 is a selective corticotropin-releasing factor 1 receptor antagonist. E2508 has the potential to be an effective therapy for the treatment of irritable bowel syndrome with a lower risk of adverse events such as constipation compared with the current clinically used 5-HT3 receptor antagonist.


Price and Availability

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E2508 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 561361
Name: E2508
CAS#: 685886-34-4
Chemical Formula: C36H47N3O7S
Exact Mass: 665.3135
Molecular Weight: 665.85
Elemental Analysis: Chemical Formula: C36H47N3O7S Exact Mass: 665.3135 Molecular Weight: 665.8460 Elemental Analysis: C, 64.94; H, 7.12; N, 6.31; O, 16.82; S, 4.81


Synonym: E2508; E-2508; E 2508;

IUPAC/Chemical Name: N-(Cyclopropylmethyl)-7-[2,6-dimethoxy-4-(methoxymethyl)phenyl]-2-ethyl-N-(oxan-4-ylmethyl)pyrazolo[1,5-a]pyridin-3-amine Tosylate

InChi Key: NOWKXPVUFWKFHF-UHFFFAOYSA-N

InChi Code: InChI=1S/C29H39N3O4.C7H8O3S/c1-5-23-29(31(17-20-9-10-20)18-21-11-13-36-14-12-21)25-8-6-7-24(32(25)30-23)28-26(34-3)15-22(19-33-2)16-27(28)35-4;1-6-2-4-7(5-3-6)11(8,9)10/h6-8,15-16,20-21H,5,9-14,17-19H2,1-4H3;2-5H,1H3,(H,8,9,10)

SMILES Code: CCC1=NN2C(C3=C(OC)C=C(COC)C=C3OC)=CC=CC2=C1N(CC4CC4)CC5CCOCC5.OS(=O)(C6=CC=C(C)C=C6)=O


Technical Data

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

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).

Harmonized System Code:
293490


References

1: Chen X, Cao X, Sun X, Lei R, Chen P, Zhao Y, Jiang Y, Yin J, Chen R, Ye D, Wang Q, Liu Z, Liu S, Cheng C, Mao J, Hou Y, Wang M, Siebenlist U, Eugene Chin Y, Wang Y, Cao L, Hu G, Zhang X. Bcl-3 regulates TGFβ signaling by stabilizing Smad3 during breast cancer pulmonary metastasis. Cell Death Dis. 2016 Dec 1;7(12):e2508. doi: 10.1038/cddis.2016.405. PubMed PMID: 27906182; PubMed Central PMCID: PMC5261001.

2: Taguchi R, Shikata K, Furuya Y, Hirakawa T, Ino M, Shin K, Shibata H. Selective corticotropin-releasing factor 1 receptor antagonist E2508 reduces restraint stress-induced defecation and visceral pain in rat models. Psychoneuroendocrinology. 2017 Jan;75:110-115. doi: 10.1016/j.psyneuen.2016.10.025. Epub 2016 Oct 29. PubMed PMID: 27810704.

3: Santos-Lozada AR. Self-rated mental health and race/ethnicity in the United States: support for the epidemiological paradox. PeerJ. 2016 Sep 22;4:e2508. doi: 10.7717/peerj.2508. eCollection 2016. PubMed PMID: 27688982; PubMed Central PMCID: PMC5036069.

4: Taguchi R, Shikata K, Furuya Y, Ino M, Shin K, Shibata H. Selective corticotropin-releasing factor 1 receptor antagonist E2508 has potent antidepressant-like and anxiolytic-like properties in rodent models. Behav Brain Res. 2016 Oct 1;312:138-47. doi: 10.1016/j.bbr.2016.06.017. Epub 2016 Jun 11. PubMed PMID: 27297028.

5: Masuoka H, Miyauchi A, Higashiyama T, Yabuta T, Kihara M, Miya A. Right-sided aortic arch and aberrant left subclavian artery with or without a left nonrecurrent inferior laryngeal nerve. Head Neck. 2016 Oct;38(10):E2508-11. doi: 10.1002/hed.24492. Epub 2016 Apr 30. PubMed PMID: 27131222; PubMed Central PMCID: PMC5074330.

6: Shah-Kulkarni S, Ha M, Kim BM, Kim E, Hong YC, Park H, Kim Y, Kim BN, Chang N, Oh SY, Kim YJ, Lee B, Ha EH. Neurodevelopment in Early Childhood Affected by Prenatal Lead Exposure and Iron Intake. Medicine (Baltimore). 2016 Jan;95(4):e2508. doi: 10.1097/MD.0000000000002508. Erratum in: Medicine (Baltimore). 2016 Mar;95(10):e077f. Kimʼs, Young Ju [Corrected to Kim, Young Ju]. PubMed PMID: 26825887; PubMed Central PMCID: PMC5291557.

7: Eigege A, Kal A, Miri E, Sallau A, Umaru J, Mafuyai H, Chuwang YS, Danjuma G, Danboyi J, Adelamo SE, Mancha BS, Okoeguale B, Patterson AE, Rakers L, Richards FO. Long-lasting insecticidal nets are synergistic with mass drug administration for interruption of lymphatic filariasis transmission in Nigeria. PLoS Negl Trop Dis. 2013 Oct 31;7(10):e2508. doi: 10.1371/journal.pntd.0002508. eCollection 2013. PubMed PMID: 24205421; PubMed Central PMCID: PMC3814337.

8: Meesat R, Belmouaddine H, Allard JF, Tanguay-Renaud C, Lemay R, Brastaviceanu T, Tremblay L, Paquette B, Wagner JR, Jay-Gerin JP, Lepage M, Huels MA, Houde D. Cancer radiotherapy based on femtosecond IR laser-beam filamentation yielding ultra-high dose rates and zero entrance dose. Proc Natl Acad Sci U S A. 2012 Sep 18;109(38):E2508-13. Epub 2012 Aug 27. PubMed PMID: 22927378; PubMed Central PMCID: PMC3458390.

9: Takahashi Y, Hibi S, Hoshino Y, Kikuchi K, Shin K, Murata-Tai K, Fujisawa M, Ino M, Shibata H, Yonaga M. Synthesis and structure-activity relationships of pyrazolo[1,5-a]pyridine derivatives: potent and orally active antagonists of corticotropin-releasing factor 1 receptor. J Med Chem. 2012 Jun 14;55(11):5255-69. doi: 10.1021/jm300259r. Epub 2012 May 31. PubMed PMID: 22587443.

10: García Rada A. Primary care in Spain is underfunded and unattractive, says report. BMJ. 2012 Apr 3;344:e2508. doi: 10.1136/bmj.e2508. PubMed PMID: 22491486.

11: Abraham JM, Cheng Y, Hamilton JP, Paun B, Jin Z, Agarwal R, Kan T, David S, Olaru A, Yang J, Ito T, Selaru FM, Mori Y, Meltzer SJ. Generation of small 32P-labeled peptides as a potential approach to colorectal cancer therapy. PLoS One. 2008 Jun 25;3(6):e2508. doi: 10.1371/journal.pone.0002508. PubMed PMID: 18575578; PubMed Central PMCID: PMC2423481.