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MedKoo CAT#: 319816

CAS#: 885220-61-1

Description: 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

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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
100.0mg USD 1750.0 2 Weeks
200.0mg USD 2150.0 2 Weeks
500.0mg USD 2950.0 2 Weeks
1.0g USD 4250.0 2 Weeks
2.0g USD 6950.0 2 Weeks
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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

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

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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.

Verucerfont

100.0mg / USD 1750.0


Additional Information

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.