| Identification | Back Directory | [Name]
4,5-Dihydro-3-phenyl-5-isoxazoleaceticacid | [CAS]
6501-72-0 | [Synonyms]
GIT 27
CS-1488
VGX-127
VGX-1027
VGX-1027, >=98%
VGX-1027(GIT 27)
VGX-1027, 6501-72-0
3-Phenyl-2-isoxazoline-5-acetic acid
2-Isoxazoline-5-acetic acid, 3-phenyl-
GIT27; GIT27; GIT-27; VGX1027; VGX 1027
4,5-Dihydro-3-phenyl-5-isoxazoleaceticacid
5-Isoxazoleacetic acid, 4,5-dihydro-3-phenyl-
2-(3-PHENYL-4,5-DIHYDROISOXAZOL-5-YL)ACETIC ACID
(3-Phenyl-4,5-dihydro-1,2-oxazol-5-yl)acetic acid
(S,R)-3-Phenyl-4,5-dihydro-5-isoxasole acetic acid
2-(3-phenyl-4,5-dihydro-1,2-oxazol-5-yl)acetic acid
VGX 1027 3-Phenyl-2-isoxazoline-5-acetic acid | [Molecular Formula]
C11H11NO3 | [MDL Number]
MFCD08696167 | [MOL File]
6501-72-0.mol | [Molecular Weight]
205 |
| Chemical Properties | Back Directory | [Melting point ]
157-158℃ | [storage temp. ]
Store at +4°C | [solubility ]
Soluble in DMSO (up to 30 mg/ml). | [form ]
solid | [color ]
White | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| Hazard Information | Back Directory | [Description]
VGX-1027 (6501-72-0) is an immunomodulator that inhibits secretion of IL-1β, TNF-α, and IL-10 from murine macrophages stimulated with LPS and spares T cell function.1?Ameliorates the course of acute and chronic immunoinflammatory conditions such as carrageenan-induced pleurisy, LPS-induced lethality, and type II collagen-induced arthritis in mouse models.1?Prevents spontaneous and accelerated forms of autoimmune diabetes in a NOD mouse model.2?Modulates genes involved in LPS-induced Toll-like receptor 4 activation in a mouse Lupus model.3?Displays protective effects in particulate matter-induced acute lung injury by blocking TLR4 signaling.4 | [Uses]
2-(3-Phenyl-4,5-dihydroisoxazol-5-yl)acetic Acid reduces the secretion of IL-1β, TNF-α and IL-10 from purified murine macrophages but not of T cells; and reduces the activation of NF-κB and p38 MAP kinase pathways along with up-regulation of ERK pathways. 2-(3-Phenyl-4,5-dihydroisoxazol-5-yl)acetic Acid inhibits proliferation of enterobacterial antigen-reactive CD4+CD25- T cells in vitro . | [in vivo]
VGX-1027 (10, 20 mg/kg of i.p. for 12 day or 100 mg/kg of p.o. for 11 day) successfully counteractes the development of destructive insulitis and hyperglycemia[1].
VGX-1027 (25?mg/kg; ip; single dose) counteracts the uveitis-inducing effect of LPS in eight-week-old male Lewis rats (180-220?g)[3].
| Animal Model: | Adult male mice, at 6 to 8 weeks of age with 25 to 30 g[1] | | Dosage: | 10, 20 mg/kg for i.p. or 100 mg/kg for p.o. | | Administration: | IP daily for 12 consecutive day or PO daily for 11 consecutive day | | Result: | Successfully counteracted the development of destructive insulitis and hyperglycemia to the mice made diabetic with multiple low doses of Streptozotocin.
|
| [IC 50]
IL-1β; IL-10 | [storage]
Store at +4°C | [References]
1) Stojanovic?et al.?(2007),?In vitro, ex vivo and in vivo immunopharmacological activities of the isooxazoline compound VGX-1027: modulation of cytokine synthesis and prevention of both organ-specific and systemic autoimmune diseases in murine models; Clin. Immunol.,?123?311
2) Stosic-Grujisic?et al.?(2007),?A potent immunomodulatory compound, (S,R)-3-Phenyl-4,5-dihydro-5-isoxazole acetic acid, prevents spontaneous and accelerated forms of autoimmune diabetes in NOD mice and inhibits the immunoinflammatory diabetes induced by multiple low doses of streptozotocin in CBA/H mice; J. Pharmacol. Exp. Ther.,?320?1038
3) Fagone?et al.?(2014),?VGX-1027 modulates genes involved in lipopolysaccharide-induced Toll-like receptor 4 activation and in a murine model of systemic lupus erythematosus; Immunology,?142?594
4) Xu?et al.?(2019),?Protective effects of VGX-1027 in PM2.5-induced airway inflammation and bronchial hyperresponsiveness; Eur. J, Pharmacol.,?842?373 |
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