R 121919 | CAS#195055-66-4 | Antagonist

MedKoo Cat#: 584725 | Name: R 121919 hydrochloride

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Description:

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

R 121919 hydrochloride is a high affinity CRF1 antagonist and is orally bioavailable.

Chemical Structure

R 121919 hydrochloride

CAS#195055-66-4

Theoretical Analysis

MedKoo Cat#: 584725

Name: R 121919 hydrochloride

CAS#: 195055-66-4

Chemical Formula: C22H33ClN6

Exact Mass: 0.0000

Molecular Weight: 417.00

Elemental Analysis: C, 63.37; H, 7.98; Cl, 8.50; N, 20.15

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 450.00	2 weeks
50mg	USD 1,000.00	2 weeks

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Synonym

R 121919 hydrochloride; R121919 hydrochloride; R-121919 hydrochloride; R-121919; R 121919; R121919

IUPAC/Chemical Name

3-[6-(Dimethylamino)-4-methyl-3-pyridinyl]-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine hydrochloride

InChi Key

LGDDPMVPDGTXMV-UHFFFAOYSA-N

InChi Code

InChI=1S/C22H32N6.ClH/c1-8-10-27(11-9-2)20-13-16(4)24-22-21(17(5)25-28(20)22)18-14-23-19(26(6)7)12-15(18)3;/h12-14H,8-11H2,1-7H3;1H

SMILES Code

CCCN(CCC)C1=CC(C)=NC2=C(C3=C(C)C=C(N(C)C)N=C3)C(C)=NN12.[H]Cl

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

>3 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

2934.99.03.00

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

R 121919 hydrochloride reduces stress-induced elevations of plasma ACTH. It is an anxiolytic and antidepressant in vivo.

In vitro activity:

R121919 exhibited inhibitory effects on Chikungunya virus infection. Reference: Biochem Biophys Res Commun. 2022 Dec 31;637:181-188. https://pubmed.ncbi.nlm.nih.gov/36403481/

In vivo activity:

This study compared the potential antidepressant-like effects of four CRF antagonists, one being R121919, 60 min prior to the forced swim test and the corresponding effect on swim-induced HPA activation. They found that R121919 did not produce antidepressant-like effects in the forced swim test. Reference: Psychopharmacology (Berl). 2005 Jul;180(2):215-23. https://pubmed.ncbi.nlm.nih.gov/15450359/

	Solvent	mg/mL	mM
Solubility
	Ethanol	41.7	100.00
	DMSO	4.2	10.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 417.00 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:

1. Watanabe Y, Suzuki Y, Emi A, Murakawa T, Hishiki T, Kato F, Sakaguchi S, Wu H, Yano T, Lim CK, Takasaki T, Nakano T. Identification of the corticotropin-releasing factor receptor 1 antagonists as inhibitors of Chikungunya virus replication using a Gaussia luciferase-expressing subgenomic replicon. Biochem Biophys Res Commun. 2022 Dec 31;637:181-188. doi: 10.1016/j.bbrc.2022.11.013. Epub 2022 Nov 9. PMID: 36403481. 2. Jutkiewicz EM, Wood SK, Houshyar H, Hsin LW, Rice KC, Woods JH. The effects of CRF antagonists, antalarmin, CP154,526, LWH234, and R121919, in the forced swim test and on swim-induced increases in adrenocorticotropin in rats. Psychopharmacology (Berl). 2005 Jul;180(2):215-23. doi: 10.1007/s00213-005-2164-z. Epub 2005 Feb 5. PMID: 15696320; PMCID: PMC1315297. 3. Hu P, Liu J, Maita I, Kwok C, Gu E, Gergues MM, Kelada F, Phan M, Zhou JN, Swaab DF, Pang ZP, Lucassen PJ, Roepke TA, Samuels BA. Chronic Stress Induces Maladaptive Behaviors by Activating Corticotropin-Releasing Hormone Signaling in the Mouse Oval Bed Nucleus of the Stria Terminalis. J Neurosci. 2020 Mar 18;40(12):2519-2537. doi: 10.1523/JNEUROSCI.2410-19.2020. Epub 2020 Feb 13. PMID: 32054675; PMCID: PMC7083537.

In vitro protocol:

In vivo protocol:

1. Jutkiewicz EM, Wood SK, Houshyar H, Hsin LW, Rice KC, Woods JH. The effects of CRF antagonists, antalarmin, CP154,526, LWH234, and R121919, in the forced swim test and on swim-induced increases in adrenocorticotropin in rats. Psychopharmacology (Berl). 2005 Jul;180(2):215-23. doi: 10.1007/s00213-005-2164-z. Epub 2005 Feb 5. PMID: 15696320; PMCID: PMC1315297. 2. Hu P, Liu J, Maita I, Kwok C, Gu E, Gergues MM, Kelada F, Phan M, Zhou JN, Swaab DF, Pang ZP, Lucassen PJ, Roepke TA, Samuels BA. Chronic Stress Induces Maladaptive Behaviors by Activating Corticotropin-Releasing Hormone Signaling in the Mouse Oval Bed Nucleus of the Stria Terminalis. J Neurosci. 2020 Mar 18;40(12):2519-2537. doi: 10.1523/JNEUROSCI.2410-19.2020. Epub 2020 Feb 13. PMID: 32054675; PMCID: PMC7083537.

1: Agoglia AE, Zhu M, Quadir SG, Bluitt MN, Douglass E, Hanback T, Tella J, Ying R, Hodge CW, Herman MA. Sex-specific plasticity in CRF regulation of inhibitory control in central amygdala CRF1 neurons after chronic voluntary alcohol drinking. Addict Biol. 2022 Jan;27(1):e13067. doi: 10.1111/adb.13067. Epub 2021 Jun 2. PMID: 34075665; PMCID: PMC8636550. 2: Short AK, Maras PM, Pham AL, Ivy AS, Baram TZ. Blocking CRH receptors in adults mitigates age-related memory impairments provoked by early-life adversity. Neuropsychopharmacology. 2020 Feb;45(3):515-523. doi: 10.1038/s41386-019-0562-x. Epub 2019 Nov 7. PMID: 31698409; PMCID: PMC6969076. 3: Dong H, Keegan JM, Hong E, Gallardo C, Montalvo-Ortiz J, Wang B, Rice KC, Csernansky J. Corticotrophin releasing factor receptor 1 antagonists prevent chronic stress-induced behavioral changes and synapse loss in aged rats. Psychoneuroendocrinology. 2018 Apr;90:92-101. doi: 10.1016/j.psyneuen.2018.02.013. Epub 2018 Feb 19. PMID: 29477954; PMCID: PMC5864558. 4: Kimbrough A, de Guglielmo G, Kononoff J, Kallupi M, Zorrilla EP, George O. CRF1 Receptor-Dependent Increases in Irritability-Like Behavior During Abstinence from Chronic Intermittent Ethanol Vapor Exposure. Alcohol Clin Exp Res. 2017 Nov;41(11):1886-1895. doi: 10.1111/acer.13484. Epub 2017 Sep 22. PMID: 28833238; PMCID: PMC5659873. 5: Zhang C, Rissman RA. Corticotropin-releasing factor receptor-1 modulates biomarkers of DNA oxidation in Alzheimer's disease mice. PLoS One. 2017 Jul 27;12(7):e0181367. doi: 10.1371/journal.pone.0181367. PMID: 28750017; PMCID: PMC5531470. 6: Hollis F, Sevelinges Y, Grosse J, Zanoletti O, Sandi C. Involvement of CRFR1 in the Basolateral Amygdala in the Immediate Fear Extinction Deficit. eNeuro. 2016 Nov 2;3(5):ENEURO.0084-16.2016. doi: 10.1523/ENEURO.0084-16.2016. PMID: 27844053; PMCID: PMC5093152. 7: Schreiber AL, Lu YL, Baynes BB, Richardson HN, Gilpin NW. Corticotropin- releasing factor in ventromedial prefrontal cortex mediates avoidance of a traumatic stress-paired context. Neuropharmacology. 2017 Feb;113(Pt A):323-330. doi: 10.1016/j.neuropharm.2016.05.008. Epub 2016 May 24. PMID: 27235163; PMCID: PMC5122468. 8: 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. PMID: 27297028. 9: Itoga CA, Roltsch Hellard EA, Whitaker AM, Lu YL, Schreiber AL, Baynes BB, Baiamonte BA, Richardson HN, Gilpin NW. Traumatic Stress Promotes Hyperalgesia via Corticotropin-Releasing Factor-1 Receptor (CRFR1) Signaling in Central Amygdala. Neuropsychopharmacology. 2016 Sep;41(10):2463-72. doi: 10.1038/npp.2016.44. Epub 2016 Mar 25. PMID: 27013358; PMCID: PMC4987844. 10: Zhang C, Kuo CC, Moghadam SH, Monte L, Campbell SN, Rice KC, Sawchenko PE, Masliah E, Rissman RA. Corticotropin-releasing factor receptor-1 antagonism mitigates beta amyloid pathology and cognitive and synaptic deficits in a mouse model of Alzheimer's disease. Alzheimers Dement. 2016 May;12(5):527-37. doi: 10.1016/j.jalz.2015.09.007. Epub 2015 Nov 7. PMID: 26555315; PMCID: PMC4860182. 11: Herman MA, Varodayan FP, Oleata CS, Luu G, Kirson D, Heilig M, Ciccocioppo R, Roberto M. Glutamatergic transmission in the central nucleus of the amygdala is selectively altered in Marchigian Sardinian alcohol-preferring rats: Alcohol and CRF effects. Neuropharmacology. 2016 Mar;102:21-31. doi: 10.1016/j.neuropharm.2015.10.027. Epub 2015 Oct 28. PMID: 26519902; PMCID: PMC4698227. 12: Zhang C, Kuo CC, Moghadam SH, Monte L, Rice KC, Rissman RA. Corticotropin- Releasing Factor Receptor-1 Antagonism Reduces Oxidative Damage in an Alzheimer’s Disease Transgenic Mouse Model. J Alzheimers Dis. 2015;45(2):639-50. doi: 10.3233/JAD-141722. PMID: 25649650; PMCID: PMC4486520. 13: Micioni Di Bonaventura MV, Ciccocioppo R, Romano A, Bossert JM, Rice KC, Ubaldi M, St Laurent R, Gaetani S, Massi M, Shaham Y, Cifani C. Role of bed nucleus of the stria terminalis corticotrophin-releasing factor receptors in frustration stress-induced binge-like palatable food consumption in female rats with a history of food restriction. J Neurosci. 2014 Aug 20;34(34):11316-24. doi: 10.1523/JNEUROSCI.1854-14.2014. PMID: 25143612; PMCID: PMC4138341. 14: Dong H, Wang S, Zeng Z, Li F, Montalvo-Ortiz J, Tucker C, Akhtar S, Shi J, Meltzer HY, Rice KC, Csernansky JG. Effects of corticotrophin-releasing factor receptor 1 antagonists on amyloid-β and behavior in Tg2576 mice. Psychopharmacology (Berl). 2014 Dec;231(24):4711-22. doi: 10.1007/s00213-014-3629-8. Epub 2014 May 27. PMID: 24862368; PMCID: PMC4233002. 15: Veenit V, Riccio O, Sandi C. CRHR1 links peripuberty stress with deficits in social and stress-coping behaviors. J Psychiatr Res. 2014 Jun;53:1-7. doi: 10.1016/j.jpsychires.2014.02.015. Epub 2014 Feb 28. PMID: 24630468. 16: Roltsch EA, Baynes BB, Mayeux JP, Whitaker AM, Baiamonte BA, Gilpin NW. Predator odor stress alters corticotropin-releasing factor-1 receptor (CRF1R)-dependent behaviors in rats. Neuropharmacology. 2014 Apr;79:83-9. doi: 10.1016/j.neuropharm.2013.11.005. Epub 2013 Nov 20. PMID: 24269607; PMCID: PMC4144021. 17: Baiamonte BA, Valenza M, Roltsch EA, Whitaker AM, Baynes BB, Sabino V, Gilpin NW. Nicotine dependence produces hyperalgesia: role of corticotropin- releasing factor-1 receptors (CRF1Rs) in the central amygdala (CeA). Neuropharmacology. 2014 Feb;77:217-23. doi: 10.1016/j.neuropharm.2013.09.025. Epub 2013 Oct 6. PMID: 24107576; PMCID: PMC4144034. 18: Iemolo A, Blasio A, St Cyr SA, Jiang F, Rice KC, Sabino V, Cottone P. CRF- CRF1 receptor system in the central and basolateral nuclei of the amygdala differentially mediates excessive eating of palatable food. Neuropsychopharmacology. 2013 Nov;38(12):2456-66. doi: 10.1038/npp.2013.147. Epub 2013 Jun 10. PMID: 23748225; PMCID: PMC3799065. 19: Wood SK, McFadden K, Griffin T, Wolfe JH, Zderic S, Valentino RJ. A corticotropin-releasing factor receptor antagonist improves urodynamic dysfunction produced by social stress or partial bladder outlet obstruction in male rats. Am J Physiol Regul Integr Comp Physiol. 2013 Jun 1;304(11):R940-50. doi: 10.1152/ajpregu.00257.2012. Epub 2013 Apr 3. PMID: 23552576; PMCID: PMC3680758. 20: Sabino V, Kwak J, Rice KC, Cottone P. Pharmacological characterization of the 20% alcohol intermittent access model in Sardinian alcohol-preferring rats: a model of binge-like drinking. Alcohol Clin Exp Res. 2013 Apr;37(4):635-43. doi: 10.1111/acer.12008. Epub 2012 Nov 5. PMID: 23126554; PMCID: PMC3567206.