| Identification | Back Directory | [Name]
4,4′-[1,3-Phenylenebis(oxy-4,1-phenyleneimino)]bis[4-oxo-2-Butenoic acid | [CAS]
139262-76-3 | [Synonyms]
H2L5186303
H2L5186303 >=98% (HPLC)
4,4′-[1,3-Phenylenebis(oxy-4,1-phenyleneimino)]bis[4-oxo-2-Butenoic acid
(Z,Z)-4,4'-[1,3-Phenylenebis(oxy-4,1-phenyleneimino)]bis[4-oxo-2-butenoic acid
(2Z,2′Z)-4,4′-[1,3-Phenylenebis(oxy-4,1-phenyleneimino)]bis[4-oxo-2-butenoic acid
2-Butenoic acid, 4,4'-[1,3-phenylenebis(oxy-4,1-phenyleneimino)]bis[4-oxo-, (Z,Z)- (9CI) | [Molecular Formula]
C26H20N2O8 | [MOL File]
139262-76-3.mol | [Molecular Weight]
488.45 |
| Chemical Properties | Back Directory | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble25mg/mL, clear | [form ]
powder | [color ]
white to beige | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| Hazard Information | Back Directory | [Description]
H2L5186303 (139262-76-3) is a potent and selective lysophosphatidic acid 2 (LPA2) receptor antagonist.? IC50?= 8.9 nM, 1230 nM and 27.35 μM for LPA2, LPA3, and LPA1 respectively.1,2 | [Uses]
H2L5186303 is an antidepressant acting on the LPA1 (lysophosphatidic acid receptor 1) and induce insulin-like growth factor-I receptor transactivation as well as causing enhanced cell proliferation. | [Biochem/physiol Actions]
H2L5186303 is specific antagonist of the lysophosphatidic acid receptor LPA2 (Ki = 7.2 nM). The compound H2L5186303 displays 40- to 1800-fold selectivity over other LPA receptors. | [in vivo]
H2L5186303 (0-50 mg/kg, given by intraperitoneal injection, single dose) suppresses the levels of eosinophils and lymphocytes in OVA-sensitized mice, and has the trachea inflammation inhibitory effect[2].
H2L5186303 (10 mg/kg, given by intraperitoneal injection, three times every other day, 6 days) inhibits cell proliferation in Lpar5f/f Villin-Cre mice intestinal crypts and promotes apoptosis[3]. | Animal Model: | Ovalbumin-Induced allergic asthma in BALB/c mice[2] | | Dosage: | 1 mg/kg, single dose; 0, 6.25, 12.5, 25, 50 mg/mL, single dose | | Administration: | Intraperitoneal injection (i.p.) | | Result: | Showed strong inhibitory effects, reducing airway hyper-responsiveness, levels of inflammatory cytokines, mucus production, and the number of eosinophils before sensitization and toxin exposure in OVA.
Lowered AHR and inflammation scores.
Suppressed mRNA levels of IL-4, IL-13, and IFN-γ, but did not inhibit IgE levels. |
| Animal Model: | Lpar5f/f Villin-Cre mice[3] | | Dosage: | 10 mg/kg, every other day for three times, 6 days | | Administration: | Intraperitoneal injection (i.p.) | | Result: | Reduced the number of proliferating cells in the intestinal crypts of mice and increased cell apoptosis. |
| [IC 50]
LPA2 Receptor: 9 nM (IC50) | [storage]
Store at -20°C | [References]
1) Fells?et al. (2008)?Identification of non-lipid LPA3 antagonists by virtual screening; Bioorg. Med. Chem.?16?6207
2) Fells?et al. (2009)?Structure-based drug design identifies novel LPA3 antagonists; Bioorg. Med. Chem. 17?7457 |
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Sigma-Aldrich
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https://www.sigmaaldrich.cn |
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BOC Sciences
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https://www.bocsci.com |
| Company Name: |
Energy Chemical
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021-58432009 400-005-6266 |
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http://www.energy-chemical.com |
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