MedKoo Cat#: 319816 | Name: Verucerfont
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Description:

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

Verucerfont, also known as GSK561679 and NBI77860, is a CRF-1 antagonist. Verucerfont blocks the CRH-1 receptor, and so reduces ACTH release following chronic stress. It is under investigation as a potential treatment for alcoholism, as chronic stress is often a factor in both development of alcoholism and relapse in recovering alcoholics. It has shown promising results in animal studies but has not been tested in humans.

Chemical Structure

Verucerfont
Verucerfont
CAS#885220-61-1

Theoretical Analysis

MedKoo Cat#: 319816

Name: Verucerfont

CAS#: 885220-61-1

Chemical Formula: C22H26N6O2

Exact Mass: 406.2117

Molecular Weight: 406.49

Elemental Analysis: C, 65.01; H, 6.45; N, 20.68; O, 7.87

Price and Availability

Size Price Availability Quantity
100mg USD 1,750.00 2 Weeks
200mg USD 2,150.00 2 Weeks
500mg USD 2,950.00 2 Weeks
1g USD 4,250.00 2 Weeks
2g USD 6,950.00 2 Weeks
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Related CAS #
No Data
Synonym
GSK561679; GSK-561679; GSK 561679; SK-561,679; GSK561679A; NBI77860; NBI-77860; NBI 77860; Verucerfont.
IUPAC/Chemical Name
(S)-3-(4-methoxy-2-methylphenyl)-2,5-dimethyl-N-(1-(3-methyl-1,2,4-oxadiazol-5-yl)propyl)pyrazolo[1,5-a]pyrimidin-7-amine
InChi Key
VKHVAUKFLBBZFJ-SFHVURJKSA-N
InChi Code
InChI=1S/C22H26N6O2/c1-7-18(22-24-15(5)27-30-22)25-19-11-13(3)23-21-20(14(4)26-28(19)21)17-9-8-16(29-6)10-12(17)2/h8-11,18,25H,7H2,1-6H3/t18-/m0/s1
SMILES Code
CC[C@H](NC1=CC(C)=NC2=C(C3=CC=C(OC)C=C3C)C(C)=NN12)C4=NC(C)=NO4
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.

Preparing Stock Solutions

The following data is based on the product molecular weight 406.49 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.

Recalculate based on batch purity %
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: Turcu AF, Spencer-Segal JL, Farber RH, Luo R, Grigoriadis DE, Ramm CA, Madrigal D, Muth T, O'Brien CF, Auchus RJ. Single-Dose Study of a Corticotropin-Releasing Factor Receptor-1 Antagonist in Women with 21-Hydroxylase Deficiency. J Clin Endocrinol Metab. 2016 Jan 11:jc20153574. [Epub ahead of print] PubMed PMID: 26751191. 2: Grillon C, Hale E, Lieberman L, Davis A, Pine DS, Ernst M. The CRH1 antagonist GSK561679 increases human fear but not anxiety as assessed by startle. Neuropsychopharmacology. 2015 Mar 13;40(5):1064-71. doi: 10.1038/npp.2014.316. PubMed PMID: 25430779; PubMed Central PMCID: PMC4367474. 3: Dunlop BW, Rothbaum BO, Binder EB, Duncan E, Harvey PD, Jovanovic T, Kelley ME, Kinkead B, Kutner M, Iosifescu DV, Mathew SJ, Neylan TC, Kilts CD, Nemeroff CB, Mayberg HS. Evaluation of a corticotropin releasing hormone type 1 receptor antagonist in women with posttraumatic stress disorder: study protocol for a randomized controlled trial. Trials. 2014 Jun 21;15:240. doi: 10.1186/1745-6215-15-240. PubMed PMID: 24950747; PubMed Central PMCID: PMC4082482. 4: 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. 5: Tellew JE, Lanier M, Moorjani M, Lin E, Luo Z, Slee DH, Zhang X, Hoare SR, Grigoriadis DE, St Denis Y, Di Fabio R, Di Modugno E, Saunders J, Williams JP. Discovery of NBI-77860/GSK561679, a potent corticotropin-releasing factor (CRF1) receptor antagonist with improved pharmacokinetic properties. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7259-64. doi: 10.1016/j.bmcl.2010.10.095. Epub 2010 Oct 25. PubMed PMID: 21074436.