R-121,919
- Product Name
- R-121,919
- CAS No.
- 195055-03-9
- Chemical Name
- R-121,919
- Synonyms
- NBI 30775;R-121,919;R121919,R-121919;R121919 (NBI-30775);-4-methylpyridin-3-yl);R121919, 10 mM in DMSO;NBI30775;R 121919;R-121919;-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine;3-(6-(Dimethylamino)-4-methylpyridin-3-yl)-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7;3-(6-(Dimethylamino)-4-methylpyridin-3-yl)-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-am
- CBNumber
- CB3464821
- Molecular Formula
- C22H32N6
- Formula Weight
- 380.53
- MOL File
- 195055-03-9.mol
R-121,919 Property
- Density
- 1.11±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 6.2 mg/mL (16.29 mM)
- form
- Solid
- pka
- 6.33±0.10(Predicted)
- color
- White to off-white
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H303May be harmfulif swallowed
H320Causes eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P312Call a POISON CENTER or doctor/physician if you feel unwell.
P337+P313IF eye irritation persists: Get medical advice/attention.
N-Bromosuccinimide Price
- Product number
- SML3114
- Product name
- R121919
- Purity
- ≥98% (HPLC)
- Packaging
- 5 mg
- Price
- $114
- Updated
- 2025/07/31
- Product number
- SML3114
- Product name
- R121919
- Purity
- ≥98% (HPLC)
- Packaging
- 25 mg
- Price
- $481
- Updated
- 2025/07/31
- Product number
- D461680
- Product name
- 3-[6-(Dimethylamino)-4-methyl-3-pyridinyl]-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine
- Packaging
- 10mg
- Price
- $1260
- Updated
- 2021/12/16
- Product number
- CS-6231
- Product name
- R121919
- Purity
- 99.84%
- Packaging
- 1mg
- Price
- $132
- Updated
- 2021/12/16
- Product number
- CS-6231
- Product name
- R121919
- Purity
- 99.84%
- Packaging
- 5mg
- Price
- $264
- Updated
- 2021/12/16
R-121,919 Chemical Properties,Usage,Production
Uses
3-[6-(Dimethylamino)-4-methyl-3-pyridinyl]-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine, is a potent and Orally active Corticotropin-Releasing factor 1 receptor antagonists, which is hown to reduce negative emotional symptoms of acute and protracted alcohol withdrawal, and thus used for the treatment of alcoholism.
Biological Activity
R121919 (NBI 30775) is a brain-penetrant, orally available high-affinity corticotropin-releasing factor/hormone (CRF or CRH) receptor 1 (CRF1, CRF-R1, CRFR-1, CRH-R1, CRHR-1) antagonist (Ki = 3.5 nM against sauvagine for binding hCRFR1-expressing HEK293 cells; IC50 = 20 nM/CRF-stimulated ACTH release from r at anterior pituitary cells & IC50 = 80 nM/CRF-stimulated cAMP production in hCRFR1-expressing HEK293 cells) without affinity toward CRFR2. In addition to its antistress efficacy in various r at anxiety models (0.63-20 mg/kg p.o.), R121919 also demonstrates therapeutic efficacy and long-term safety in Alzheimerμs disease (AD) mice (20 mg/kg/day s.c.) in vivo.
in vivo
R121919 (NBI30775) dose dependently decreases adrenocorticopin hormone and Corticosterone (HY-B1618) responses to restraint stress in rats. Peak plasma adrenocorticopin hormone and corticosterone concentrations at a dose of 10 mg/kg R121919 are 9 and 25%, respectively[1].
R121919 reduces levels of anxiety in mice with a steep dose-response curve[2].
IC 50
CRFR1: 2-5 nM (Ki)
R-121,919 Preparation Products And Raw materials
Raw materials
Preparation Products
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