GLPBio

CAY10650

Catalog No.: GC18305Purity:>98.00%
COASDSData Sheet
CAY10650 هو مثبط قوي للغاية لفوسفوليباز A2α (cPLA2α) مع قيمة IC50 تبلغ 12 نانومتر

المنتجات مخصصة للاستخدام البحثي فقط، وليست للاستخدام البشري. نحن لا نبيع للمرضى.

CAY10650
Cas No.: 1233706-88-1
10mM (in 1mL DMSO)In Stock
$131.00
1
1mgIn Stock
$35.00
1
5mgIn Stock
$126.00
1
10mgIn Stock
$164.00
1
25mgIn Stock
$287.00
1
50mgIn Stock
$388.00
1
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com

المراجع (Citations)

لا تتوفر حاليًا مراجع لهذا المنتج. فيما يلي مجموعة مختارة من المنشورات التي تستشهد بمنتجات GlpBio.
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    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    Cell
    183(7):1867-1883 (2020)
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الوصف (Description)

CAY10650 is a highly potent cytosolic phospholipase A2α (cPLA2α) inhibitor with an IC50 value of 12nM[1]. cPLA2α is a crucial enzyme involved in the hydrolysis of phospholipids to release arachidonic acid and is essential for mediating inflammatory responses and cellular signaling pathways[2][3]. CAY10650 is typically used for studying inflammation and cellular signaling pathways related to phospholipase A2[4][5].

In vitro, CAY10650 (12nM; 30min) inhibit the phosphorylation of cPLA2α, and reduced lipid body formation and PGE2 secretion in human neutrophils stimulated with Cr-LAAO[1].

In vivo, CAY10650 (50μg in 5μl eye-drop) attenuated corneal inflammation and decreased neutrophil infiltration when applied topically three times daily for 6 days and then daily from days 7 to 15 post-infection in Chinese hamsters infected with Acanthamoeba castellanii in the eyes[6]. CAY10650 (20μg/ear/day) reduced ear thickness, epidermal thickness, and inflammatory infiltrates in an IMQ-induced psoriasis mouse model when applied topically for 5 days[7].

References:
[1] Paloschi MV, Lopes JA, Boeno CN, et al. Cytosolic phospholipase A2-α participates in lipid body formation and PGE2 release in human neutrophils stimulated with an L-amino acid oxidase from Calloselasma rhodostoma venom. Sci Rep. 2020;10(1):10976.
[2] Murakami M, Kudo I. Phospholipase A2. J Biochem. 2002;131(3):285-292.
[3] Yang D, Ji HF, Zhang XM, et al. Protective effect of cytosolic phospholipase A2 inhibition against inflammation and degeneration by promoting regulatory T cells in rats with experimental autoimmune encephalomyelitis. Mediators Inflamm. 2014;2014:890139.
[4] Lin CY, Xu WB, Li BZ, Shu MA, Zhang YM. Identification and functional analysis of cytosolic phospholipase A2 (cPLA2) from the red swamp crayfish Procambarus clarkii: The first evidence of cPLA2 involved in immunity in invertebrates. Fish Shellfish Immunol. 2023;140:108944.
[5] Wu CZ, Li X, Hong L, et al. NOX4/Src regulates ANP secretion through activating ERK1/2 and Akt/GATA4 signaling in beating rat hypoxic atria. Korean J Physiol Pharmacol. 2021;25(2):159-166.
[6] Tripathi T, Abdi M, Alizadeh H. Role of phospholipase A₂ (PLA₂) inhibitors in attenuating apoptosis of the corneal epithelial cells and mitigation of Acanthamoeba keratitis. Exp Eye Res. 2013;113:182-191.
[7] Shao S, Chen J, Swindell WR, et al. Phospholipase A2 enzymes represent a shared pathogenic pathway in psoriasis and pityriasis rubra pilaris. JCI Insight. 2021;6(20):e151911.

البروتوكول (Protocol)

Cell experiment [1]:

Cell lines

human neutrophils

Preparation Method

Neutrophils isolated according to item above from 3 different donors, were suspended in a RPMI assay medium [RPMI-1640 medium supplemented with 100mg/mL of gentamicin, 2mM of l-glutamine and 2% of fetal bovine serum (FBS)]. 1×107 isolated human neutrophils were plated and pre-treated with CAY10650 (cPLA2-α inhibitor, 12nM for 30min) or the same vehicle used to dissolve the inhibitors in RPMI (control). Then, they were incubated with RPMI (negative control), LPS (1µg/mL; positive control) or Cr-LAAO (50µg/mL) at 37°C, in a humidified atmosphere (5% CO2) for 1h. Lipid bodies were quantified with Oil Red O staining. PGE2 concentrations in the supernatant were determined by a specific enzymatic immunoassay (EIA). Proteins were extracted for western blot analysis.

Reaction Conditions

12nM; 30min

Applications

CAY10650 inhibit the phosphorylation of cPLA2α, and reduced lipid body formation and PGE2 secretion in human neutrophils stimulated with Cr-LAAO.
Animal experiment [2]:

Animal models

Chinese hamsters

Preparation Method

Chinese hamsters (n=9/group) were infected with Acanthamoeba castellanii-laden contact lenses. cPLA2α inhibitor (CAY10650; 50μg in 5μl) was injected with topical eye-drop under the contact lens of an infected cornea three times a day for 6 days and topically on days 7 to 20 postinfection. As a control infected animals were treated with 50μg/5μl of BSA. Lenses were removed 7 days postinfection, and corneas were scored for clinical severity for the period indicated. Each graph line represents the mean severity of the observed time points. The results shown are representative of three separate experiments. The infections were scored on a scale of 0 to 5 based on the following parameters: corneal infiltration, corneal neovascularization and corneal ulceration. The pathology was recorded as: 0=no pathology, 1=<10% of the cornea involved, 2=10 to 25% involved, 3=25 to 50% involved, 4=50 to 75% involved, and 5=75 to 100% involved. Any animals receiving a score of at least 1.0 for any parameter were scored as infected. Animals were anesthetized and sacrificed 15 days after application of CAY10650. Each animal’s right eye (uninfected and untreated) was used as negative control. As control, uninfected eyes of animals (n=6/group) were treated with CAY10650. Eyes were removed and used for histopathological examination.

Dosage form

50μg in 5μl eye-drop; topically three times daily for 6 days and then daily from days 7 to 15 post-infection

Applications

CAY10650 attenuated corneal inflammation and decreased neutrophil infiltration when applied topically three times daily for 6 days and then daily from days 7 to 15 post-infection in Chinese hamsters infected with Acanthamoeba castellanii in the eyes.

References:
[1] Paloschi MV, Lopes JA, Boeno CN, et al. Cytosolic phospholipase A2-α participates in lipid body formation and PGE2 release in human neutrophils stimulated with an L-amino acid oxidase from Calloselasma rhodostoma venom. Sci Rep. 2020;10(1):10976.
[2] Tripathi T, Abdi M, Alizadeh H. Role of phospholipase A₂ (PLA₂) inhibitors in attenuating apoptosis of the corneal epithelial cells and mitigation of Acanthamoeba keratitis. Exp Eye Res. 2013;113:182-191.

وثائق المنتج (Product Documents)

Purity:>98.00%Appearance:A solid
COASDSData Sheet

الخصائص الكيميائية (Chemical Properties)

رقم CAS
1233706-88-1
الاسم الكيميائي
3-(2-methyl-1-oxopropyl)-1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indole-5-carboxylic acid
SMILES
O=C(CN1C(C=CC(C(O)=O)=C2)=C2C(C(C(C)C)=O)=C1)COC3=CC=C(OC4=CC=CC=C4)C=C3
الصيغة الجزيئية
C28H25NO6
الوزن الجزيئي
471.5
الذوبانية
DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:10): 0.1 mg/ml
التخزين
Store at -20°C
إرشادات عامة
اختر مذيبًا مناسبًا وفقًا لبيانات ذوبانية المنتج. بعد التحضير، قسّم المحلول المخزون إلى أجزاء لتجنب دورات التجميد والذوبان المتكررة.
استخدم المحاليل المخزونة خلال 6 أشهر عند حفظها في -80°C، أو خلال شهر واحد عند حفظها في -20°C.
لتحسين الذوبانية، سخّن الأنبوب إلى 37°C وعرّضه للموجات فوق الصوتية لمدة مناسبة.
شروط الشحن
تُشحن عينات التقييم مع عبوات تبريد. وتُشحن الأحجام الأخرى المتاحة في درجة حرارة الغرفة، أو مع عبوات تبريد عند الطلب.

الحاسبات (Calculators)المولارية / التخفيف / الوزن الجزيئي / تحويل الوحدات / تركيبة داخل الجسم الحي / الذوبانية

g/mol

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