SML3114
R121919
≥98% (HPLC)
别名:
3-[6-(Dimethylamino)-4-methyl-3-pyridinyl]-2,5-dimethyl-N,N-dipropylpyrazolo[1,5-a]pyrimidin-7-amine, NBI 30775, NBI-30775, NBI30775, R 121919, R-121919
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选择尺寸
关于此项目
经验公式（希尔记法）:
C22H32N6
化学文摘社编号:
分子量:
380.53
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
InChI
1S/C22H32N6/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
SMILES string
CCCN(CCC)C1=CC(C)=NC2=C(C(C)=NN12)C3=CN=C(C=C3C)N(C)C
InChI key
ANNRUWYFVIGKHA-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Brain-penetrant and orally available selective CRF1 (CRFR-1, CRHR-1) antagonist with in vivo antistress efficacy.
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 rat 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 rat anxiety models (0.63-20 mg/kg p.o.), R121919 also demonstrates therapeutic efficacy and long-term safety in Alzheimer′s disease (AD) mice (20 mg/kg/day s.c.) in vivo.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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