E2508 | CAS#685886-34-4 | corticotropin-releasing factor 1 receptor antagonist

MedKoo Cat#: 561361 | Name: E2508

Description:

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

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.

Chemical Structure

E2508

CAS#685886-34-4

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

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

No Data

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

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).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 665.85 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

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.