Description
BBS-4 is a potent and selective inducible nitric oxide synthase (NOS2) dimerization inhibitor, with an IC50 of 0.49 nM. BBS-4 can protect mice from the cardiovascular dysfunction of sepsis.
Product information
CAS Number: 402934-09-2
Molecular Weight: 420.46
Formula: C22H24N6O3
Chemical Name: (2R)-N-[2-(2H-1,3-benzodioxol-5-yl)ethyl]-1-[2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl]pyrrolidine-2-carboxamide
Smiles: CC1=CC(=NC(=N1)N1C=NC=C1)N1CCC[C@@H]1C(=O)NCCC1=CC2OCOC=2C=C1
InChiKey: LBCGUKCXRVUULK-QGZVFWFLSA-N
InChi: InChI=1S/C22H24N6O3/c1-15-11-20(26-22(25-15)27-10-8-23-13-27)28-9-2-3-17(28)21(29)24-7-6-16-4-5-18-19(12-16)31-14-30-18/h4-5,8,10-13,17H,2-3,6-7,9,14H2,1H3,(H,24,29)/t17-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
BBS-4 exhibits ∼300–2000-fold selective for inhibiting iNOS dimerization in cells versus CYP-3A4 (∼150 nM in a microsomal benzyloxyresorufin assay; ∼1 μM in a cell-based testosterone hydroxylase assay).
In Vivo:
BBS-4 (10 mg/kg; i.p.; 1 h after endotoxin administration) prevents endotoxin-induced hypotension in mice. BBS-4 (30 mg/kg; i.p.; 1 h after endotoxin administration) prevents endotoxin-induced myocardial dysfunction in mice. BBS-4 (10 mg/kg; i.p.; 1 and 8 h after endotoxin administration) prevents endotoxin-induced impairment of murine hypoxic pulmonary vasoconstriction (HPV). BBS-4 (10 mg/kg; i.p.; 1 and 8 h after endotoxin administration) does not affect the endotoxin-induced increase in pulmonary NOS2 gene expression, but it (30 mg/kg) prevents cardiac and pulmonary NOS2 protein dimerization and increases plasma nitrate and nitrite (NOx) concentration in mice. BBS-2 (30 mg/kg; s.c. twice daily for 10 d) does not affect agonist-stimulated NOS3-dependent aortic relaxation ex vivo. BBS-4 (10-30 mg/kg; i.p.) does not improve mortality rate in endotoxemic mice.
Products are for research use only. Not for human use.
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