R-121,919
- CAS No.
- 195055-03-9
- Chemical Name:
- R-121,919
- Synonyms
- R-121,919;NBI 30775;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
- Molecular Weight:
- 380.53
- MDL Number:
- MFCD05260874
- MOL File:
- 195055-03-9.mol
- MSDS File:
- SDS
| 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 |
| FDA UNII | G82N555U1N |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
R-121,919 price More Price(18)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| TRC | D461680 | 3-[6-(Dimethylamino)-4-methyl-3-pyridinyl]-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine | 195055-03-9 | 10mg | $1260 | 2021-12-16 | Buy |
| ChemScene | CS-6231 | R121919 99.84% | 195055-03-9 | 50mg | $1440 | 2021-12-16 | Buy |
| Matrix Scientific | 093471 | 3-(6-(Dimethylamino)-4-methylpyridin-3-yl)-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine 95+% | 195055-03-9 | 250mg | $3780 | 2021-12-16 | Buy |
| AK Scientific | 0092AB | 3-(6-(Dimethylamino)-4-methylpyridin-3-yl)-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine | 195055-03-9 | 250mg | $5153 | 2021-12-16 | Buy |
| American Custom Chemicals Corporation | API0009338 | R-121919 95.00% | 195055-03-9 | 1G | $7304.85 | 2021-12-16 | Buy |
R-121,919 Chemical Properties,Uses,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
R-121,919 Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Alchem Pharmtech,Inc. | 8485655694 | sales@alchempharmtech.com | United States | 63687 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32222 | 58 |
| Zibo Hangyu Biotechnology Development Co., Ltd | +86-0533-2185556 +8615965530500 | nickzhang@hangyubiotech.com | China | 10983 | 58 |
| Shenyang Zhongshen Zekang Biomedical Technology Research Co., Ltd | +86-18341751992 +86-15382112998 | 757984502@qq.com | China | 892 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 52924 | 58 | |
| Suzhou ARTK Medchem Co., Ltd. | +86-512-68323658 +86-18168183658 | sales1@artkmedchem.com | China | 39003 | 58 |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131957 | 58 |
| J & K SCIENTIFIC LTD. | 18210857532 | jkinfo@jkchemical.com | China | 96815 | 76 |
| AdooQ Bioscience CHINA | 025-58849295 18951903616; | info@adooq.cn | China | 2990 | 60 |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9803 | 58 |