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

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: CCCN(CCC)C1=CC(C)=NC2=C(C(C)=NN12)C3=CN=C(C=C3C)N(C)C
• 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
• InChI key: ANNRUWYFVIGKHA-UHFFFAOYSA-N

Description

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.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable