SB-772077B (hydrochloride)

SB-772077B is a Rho-associated kinase (ROCK) inhibitor (IC50s = 5.6 and 6 nM for ROCK1 and ROCK2, respectively). It is selective for ROCK1 and ROCK2 over Akt1, Akt2, and Akt3 (IC50s = 324, 1,950, and 1,290 nM, respectively), as well as Cdk2, GSK3alpha, IKKbeta, JNK3, and Plk (IC50s = >7,000 nM for all), but also inhibits RSK1 and MSK1 (IC50s = 35 and 14 nM, respectively). SB-772077B inhibits LPS-induced TNF-alpha and IL-6 production in THP-1 cells in a concentration-dependent manner. It induces relaxation of pre-contracted isolated rat aortic rings (IC50 = 39 nM). It reduces blood pressure in spontaneously hypertensive rats in a dose-dependent manner and in DOCA-salt hypertensive rats when administered at a dose of 1 mg/kg. SB-772077B (30, 100, and 300 µg/kg, i.v.) reduces pulmonary and systemic arterial pressure and increases cardiac output in normotensive rats and rats with monocrotaline-induced pulmonary hypertension.Formal Name: [2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-7-yl][(3S)-3-amino-1-pyrrolidinyl]-methanone, dihydrochloride. CAS Number: 607373-46-6. Molecular Formula: C15H18N8O2 . 2HCl. Formula Weight: 415.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 100 mM, Water: 100 mM. SMILES: O=C(N1CC[C@H](N)C1)C2=C3C(N=C(C4=NON=C4N)N3CC)=CN=C2.Cl.Cl. InChi Code: InChI=1S/C15H18N8O2.2ClH/c1-2-23-12-9(15(24)22-4-3-8(16)7-22)5-18-6-10(12)19-14(23)11-13(17)21-25-20-11,,/h5-6,8H,2-4,7,16H2,1H3,(H2,17,21),2*1H/t8-,,/m0../s1. InChi Key: HSROPTGRSYJPJY-JZGIKJSDSA-N.