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Merck
CN

SML3114

R121919

≥98% (HPLC)

Synonym(s):

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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About This Item

Empirical Formula (Hill Notation):
C22H32N6
CAS Number:
195055-03-9
Molecular Weight:
380.53
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD05260874

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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

100

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.

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000132006
0000132007
0000129078

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