| Identification | Back Directory | [Name]
2-(P-AMYLCINNAMOYL)AMINO-4-CHLOROBENZOIC ACID | [CAS]
99754-06-0 | [Synonyms]
ONO-RS-082
2-(4-amylcinnamoyl)amino-4-chlorobenzoic acid
2-(P-AMYLCINNAMOYL)AMINO-4-CHLOROBENZOIC ACID
(E)-4-chloro-2-(3-(4-pentylphenyl)acrylamido)benzoic acid
4-chloro-2-[3-(4-pentylphenyl)prop-2-enoylamino]benzoic acid
2-[[(E)-4-Pentylcinnamoyl]amino]-4-chlorobenzoic acid sodium salt
4-chloro-2-[[(E)-3-(4-pentylphenyl)prop-2-enoyl]amino]benzoic acid
(E)-4-chloro-2-(3-(4-pentylphenyl)acrylamido)benzoic acid(WXC06363)
4-Chloro-2-[[1-oxo-3-(4-pentylphenyl)-2-propen-1-yl]amino]-benzoic acid
Benzoic acid, 4-chloro-2-[[(2E)-1-oxo-3-(4-pentylphenyl)-2-propen-1-yl]amino]- | [Molecular Formula]
C21H22ClNO3 | [MDL Number]
MFCD00210755 | [MOL File]
99754-06-0.mol | [Molecular Weight]
371.86 |
| Chemical Properties | Back Directory | [Melting point ]
175-177℃ | [storage temp. ]
room temp | [solubility ]
DMSO: ≥20mg/mL | [form ]
powder | [color ]
white | [Sensitive ]
Light Sensitive | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. | [InChI]
1S/C21H22ClNO3/c1-2-3-4-5-15-6-8-16(9-7-15)10-13-20(24)23-19-14-17(22)11-12-18(19)21(25)26/h6-14H,2-5H2,1H3,(H,23,24)(H,25,26)/b13-10+ | [InChIKey]
MDVFITMPFHDRBZ-JLHYYAGUSA-N | [SMILES]
Clc1cc(c(cc1)C(=O)O)NC(=O)\C=C\c2ccc(cc2)CCCCC |
| Safety Data | Back Directory | [Hazard Codes ]
N | [Risk Statements ]
50 | [Safety Statements ]
61 | [RIDADR ]
UN 3077 9 / PGIII | [WGK Germany ]
2 | [HazardClass ]
9 | [Storage Class]
11 - Combustible Solids | [Hazard Classifications]
Aquatic Acute 1
Aquatic Chronic 1 |
| Hazard Information | Back Directory | [Description]
ONO-RS-082 (99754-06-0) is a reversible inhibitor of Ca2+-independent phospholipase A2?(PLA2), IC50=7 μM for guinea pig lung PLA2.1?Inhibits epinephrine-induced thromboxane production in platelets.1?Inhibition of PLA2?by ONO-RS-032 disrupts endosome tubule formation and maintenance of the Golgi complex.2-4?Prevents Xenopus oocyte maturation at stage V.5 | [Uses]
ONO-RS-082 is a potent PLA2 and epinephrine inhibitor.ONO-RS-082 is a phospholipase inhibitor. | [in vitro]
previous study found that human platelets stimulated by epinephrine led to enhanced turnover of phosphatidylinositol 4,5-bisphosphate, accumulated inositol trisphosphate, diacylglycerol, and phosphatidic acid, indicating stimulation of phospholipase c. it was shown that these responses could be completely blocked by inhibitors of alpha 2-adrenergic receptors including ono-rs-082 or removal of fibrinogen. in addition, epinephrine could evoked an increased turnover of ester-linked arachidonic acid in aspirin treated platelets that was inhibited by ono-rs-082 or the absence of fibrinogen. moreover, it was found that ono-rs-082 at 3.5 μm was able to inhibit epinephrine-stimulated thromboxane production in human platelets. ono-rs-082 could also disrupt endosome tubule formation and maintenance of the golgi complex [1]. | [in vivo]
In vivo long-term activation of KCNK3 by ONO-RS-082 (50 mg/kg/day; preventive treatment, day 0 to day 21) reduces the development of PH in the MCT-PH model[4].
In contrast, in vivo short-term KCNK3 activation by ONO-RS-082 (curative treatment) fails to reduce PH symptoms, which is attributed to the complete loss of KCNK3 expression in MCT-PH rats at days 14 to 21[4]. | Animal Model: | MCT- pulmonary hypertension (PH) rat model[4] | | Dosage: | 50 mg/kg/day | | Administration: | | | Result: | Reduced the development of PH in the MCT-PH model for long-term.
|
| [storage]
Store at -20°C | [References]
1) Banga?et al.?(1986),?Activation of phospholipases A and C in human platelets exposed to epinephrine: role of glycoproteins IIb/IIIa and dual role of epinephrine; Proc. Natl. Acad. Sci. USA?83?9197
2) De Figueiredo?et al. (2001),?Inhibition of transferrin recycling and endosome tubulation by phospholipase A2 antagonists; J. Biol. Chem.?276?47361
3) Schmidt?et al. (2010),?A role for phospholipase A2 activity in membrane tubule formation and TGN trafficking; Traffic?11?1530
4) Bechler and Brown (2014),?Gβ1γ2 activates phospholipase A2-dependent Golgi membrane tubule formation; Front. Cell. Dev. Biol.?28?0004
5) Islam?et al.?(2005),?The distinct stage-specific effects of 2-(p-amylcinnamoyl)amino-4-chlorobenzoic acid on the activation of MAP kinase and Cdc2 kinase in Xenopus oocyte maturation; Cell Signal.?17?507 |
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Wuxi AppTec
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022-59987777 13552403979 |
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www.labnetwork.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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