A ROCK1 and ROCK2 inhibitor
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SB-772077B (hydrochloride)

Item No. 30975

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMSO: 100 mMWater: 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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    SB-772077B is a Rho-associated kinase (ROCK) inhibitor (IC50s = 5.6 and 6 nM for ROCK1 and ROCK2, respectively).1 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, GSK3α, IKKβ, 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-α 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.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Doe, C., Bentley, R., Behm, D.J., et al. Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. J. Pharmacol. Exp. Ther. 320(1), 89-98 (2007).

    2. Dhaliwal, J.S., Badejo, A.M., Jr., Casey, D.B., et al. Analysis of pulmonary vasodilator responses to SB-772077-B [4-(7-((3-amino-1-pyrrolidinyl)carbonyl)-1-ethyl-1H-imidazo(4,5-c)pyridin-2-yl)-1,2,5-oxadiazol-3-amine], a novel aminofurazan-based Rho kinase inhibitor. J. Pharmacol. Exp. Ther. 330(1), 334-341 (2009).