245329-99-1
Chemical Structure
CI-1018
- CAS No.: 245329-99-1
- Formula:C24H20N4O2
- Molecular Weight:396.45
IUPAC Name: N-(9-methyl-4-oxo-1-phenyl-3,4,6,7-tetrahydro-[1,4]diazepino[6,7,1-hi]indol-3-yl)isonicotinamide
InChIKey: KYFWUBJMTHVBIF-UHFFFAOYSA-N
SMILES: O=C(NC1N=C(C=2C=CC=CC2)C=3C=C(C=C4C3N(C1=O)CC4)C)C=5C=CN=CC5
Biological Activity: CI-1018 is an orally active selective PDE-4 inhibitor, with IC50 values of 1.1 μM, 35.8 μM, and 73.4 μM against hPDE-4, canine PDE-4, and guinea pig PDE-4, respectively. CI-1018 induces iNOS expression and Apoptosis. CI-1018 induces vascular injury, medial necrosis, hemorrhage, edema, thymic atrophy, ketonuria, and weight loss. CI-1018 can be used in research related to asthma, vasculitis, and mesenteric vasculitis/arteriopathy[1][2][3][4].
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CI-1018 | CI-1018 is an orally active selective PDE-4 inhibitor, with IC50 values of 1.1 μM, 35.8 μM, and 73.4 μM against hPDE-4, canine PDE-4, and guinea pig PDE-4, respectively. CI-1018 induces iNOS expression and Apoptosis. CI-1018 induces vascular injury, medial necrosis, hemorrhage, edema, thymic atrophy, ketonuria, and weight loss. CI-1018 can be used in research related to asthma, vasculitis, and mesenteric vasculitis/arteriopathy. | |||||||||||||||||||||
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References
- [1]. Slim RM, et al. Effect of dexamethasone on the metabonomics profile associated with phosphodiesterase inhibitor-induced vascular lesions in rats. Toxicology and applied pharmacology. 2002 Sep 01;183(2):108-9. [Content Brief]
- [2]. Robertson DG, et al. Metabonomic assessment of vasculitis in rats. Cardiovascular toxicology. 2001;1(1):7-19. [Content Brief]
- [3]. Burnouf C, et al. Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors. Journal of medicinal chemistry. 2000 Dec 14;43(25):4850-67. [Content Brief]
- [4]. Slim RM, et al. Apoptosis and nitrative stress associated with phosphodiesterase inhibitor-induced mesenteric vasculitis in rats. Toxicologic pathology. 2003;31(6):638-45. [Content Brief]
