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

R 121919 hydrochloride
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 584725

CAS#: 195055-66-4

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

Chemical Structure

R 121919 hydrochloride

CAS# 195055-66-4

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 584725
Name: R 121919 hydrochloride
CAS#: 195055-66-4
Chemical Formula: C22H33ClN6
Exact Mass: 0.00
Molecular Weight: 417.000
Elemental Analysis: C, 63.37; H, 7.98; Cl, 8.50; N, 20.15

Price and Availability

Size	Price	Availability
10mg	USD 320	2 weeks
50mg	USD 880	2 weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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:

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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/

Solubility Data

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

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:	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.
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.

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Chen and Grigoriadis (2005) NBI 30775 (R121919), an orally active antagonist of the corticotropin-releasing factor (CRF) type-1 receptor for the treatment of anxiety and depression. Drug Dev.Res. 65 216

Jutkiewicz et al (2005) 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). 180 215 PMID: 15696320

Gutman et al (2003) The corticotropin-releasing factor1 receptor antagonist R121919 attenuates the behavioral and endocrine responses to stress. J.Pharmacol.Exp.Ther. 304 874 PMID: 12538845

Heinrichs et al (2002) Brain penetrance, receptor occupancy and antistress in vivo efficacy of a small molecule corticotropin releasing factor type I receptor selective antagonist. Neuropsychopharmacology 27 194 PMID: 12093593

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