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12

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T10137	4-Bromo A23187 4-Bromo A23187	Others	Others
	4-Bromo A23187 is a halogenated analog of the calcium ionophore A-23187. 4-Bromo A23187 is a calcium modulator and induces apoptosis in different cells.
T22946	LY255283 LY 255283	Leukotriene Receptor	GPCR/G Protein
	LY255283 是白三烯 B4 (LTB4) 受体的特异性拮抗剂，抑制人外周血多形核白细胞和由钙离子载体 A23187 激活的单核细胞中 LTB(4) 的产生。
T37650	5(S),15(S)-DiHETE
	5(S),15(S)-DiHETE is synthesized by 15-LO from 5(S)-HETE. It potentiates the degranulation of human PMNL in response to PAF, but not fMLP, calcium ionophore A23187, or LTB4. 5(S),15(S)-DiHETE is chemotactic for eosinophils with an ED50 value of 0.3 μM.
T37556	CAY10502
	Phospholipase A2 (PLA2) catalyzes the hydrolysis of phospholipids at the sn-2 position leading to the production of lysophospholipids and free fatty acids. Calcium-dependent cytosolic PLA2 (cPLA2α) is a 85 kDa enzyme that plays a key role in the arachidonic cascade and the inflammatory response associated with this metabolic pathway. CAY10502 is a potent inhibitor of calcium-dependent cytosolic PLA2α (cPLA2α) with an IC50 value of 4.3 nM for the purified enzyme from human platelets. It inhibits ...
T38350	TAS 205
	TAS 205 is an inhibitor of hematopoietic prostaglandin D synthase (H-PGDS; IC50= 55.8 nM).1It is selective for H-PGDS over lipocalin-type PGDS (L-PGDS) at 100 μM, as well as over enzyme and receptor panels at 10 μM. TAS 205 inhibits production of prostaglandin D2induced by A23187 in KU812 human and RBL-2H3 rat basophils with IC50values of 78.3 and 181.3 nM, respectively. It inhibits ovalbumin-induced nasal lavage fluid eosinophil infiltration and late-phase nasal obstruction in an ovalbumin-sens...
T35541	Lipoxygenin
	Lipoxygenin is an inhibitor of 5-lipoxygenase (5-LO) with an IC50value of 5 μM for inhibition of 5-LO product synthesis in isolated human granulocytes stimulated with the cation ionophore A23187 .1It inhibits hedgehog-dependent signaling in Shh-LIGHT2 cells and TGF-β-, activin A-, bone morphogenic protein (BMP)-, or Wnt-dependent signaling in HEK293T cells (IC50s = 9.3, 3.2, 8.2, 9.6, and 3.7 μM, respectively, in luciferase reporter assays). Lipoxygenin (5 and 10 μM) increases levels of troponin...
T37331	Pyrrophenone
	The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid (AA) from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins (PGs) and leukotrienes (LTs). Pyrrophenone inhibits cPLA2α with an IC50 of 4.2 nM in enzyme assays and potently blocks the release of AA and the production of PGE2 and LTC4 in cells (IC50 = 24, 25, and 14 nM, respectively). Its action is reversible and selective, as py...
T37284	1-Stearoyl-2-15(S)-HETE-sn-glycero-3-PE
	1-Stearoyl-2-15(S)-HETE-sn-glycero-3-PE is a phospholipid that contains stearic acid at the sn-1 position and 15(S)-HETE at the sn-2 position. It is formed in human peripheral monocytes activated by the calcium ionophore A23187 by direct oxidation of 1-stearoyl-2-arachidonoyl-sn-glycero-3-PE by 15-LO. Phosphoethanolamine (PE) HETEs (PE-HETEs), including 1-stearoyl-2-15(S)-HETE-sn-glycero-3-PE, are the main source of esterified HETE in ionophore-activated monocytes.
T71870	CP21
	CP21 is an iron chelator that binds to iron in a 3:1 (ligand:iron) ratio. It is active against P. falciparum when used at concentrations of 10 and 100 µM. CP21 inhibits production of prostaglandin I2 induced by epinephrine, arachidonic acid, or A23187 in isolated rat aortic rings with IC50 values of 1.3, 1.3, and 1.4 mM, respectively. It inhibits glutamate-induced oxytosis, as well as decreases iodoacetic acid-induced cytotoxicity in an in vitro model of ischemia, in HT22 mouse hippocampal cells...
T71303	Flufenamic Acid-d4
	Flufenamic acid-d4 is intended for use as an internal standard for the quantification of flufenamic acid by GC- or LC-MS. Flufenamic acid is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC50s = 3 and 9.3 µM for human COX-1 and COX-2, respectively). Flufenamic acid inhibits TNF-α-induced increases in COX-2 levels and NF-κB activation in HT-29 colon cancer cells in a concentration-dependent manner. It inhibits calcium influx induced by fMLP or A23187 in human polymorphonuclear...
T83773	Prostaglandin E2 Inhibitor 3 PGE2 Inhibitor 3
	Prostaglandin E2抑制剂3是一种microsomal prostaglandin E合酶-1 (mPGES-1; IC50 = 0.2 µM)的抑制剂，相较于COX-1、COX-2、5-lipoxygenase (5-LO)和soluble epoxide hydrolase (sEH)，在10 µM的无细胞试验中表现出对mPGES-1的选择性。在10 µM和1 µM的浓度下，该抑制剂能抑制A549细胞中IL-1β诱导的PGE2生成以及在J774A.1巨噬细胞中，LPS诱导的IL-6和PGE2生成。同时，它还能抑制由钙离子载体A23187单独或结合花生四烯酸和A23187诱导的5-LO产物形成，包括白三烯B4 (LTB4) 和5-H(p)ETE（IC50s分别为4.9和5.2 µM）。在体内，10 mg/kg剂量的Prostaglandin E2抑制剂3能防止在zymosan诱导的小鼠腹膜炎模型中白细胞渗入腹腔液中。
T36618	Rupatadine
	Rupatadine (UR-12592) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 uM(rabbit platelet membranes/guinea pig cerebellum membranes).IC50 value:Target: PAF/H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 +/- 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 +/- 0.08) and in hu...

化合物

4-Bromo A23187

Cat.No: T10137

Synonym: 4-Bromo A23187

Target: Others

Cat.No: T22946

Synonym: LY 255283

Target: Leukotriene Receptor

5(S),15(S)-DiHETE

Cat.No: T37650

Cat.No: T37556

Cat.No: T38350

Cat.No: T35541

Cat.No: T37331

1-Stearoyl-2-15(S)-HETE-sn-glycero-3-PE

Cat.No: T37284

Cat.No: T71870

Flufenamic Acid-d4

Cat.No: T71303

Prostaglandin E2 Inhibitor 3

Cat.No: T83773

Synonym: PGE2 Inhibitor 3

Cat.No: T36618

Cat. No.	Product Name	Target	Signaling Pathways
T10662L	Calcimycin Antibiotic A-23187,离子载体(钙镁盐混合物),A-23187	Apoptosis; Antibacterial; Antibiotic; Autophagy; Antifungal	Apoptosis; Autophagy; Microbiology/Virology
	Calcimycin (A-23187) 是抗生素和二价阳离子离子载体。它抑制革兰氏阳性细菌和一些真菌生长，也抑制 ATP 酶的活性并解耦哺乳动物细胞的氧化磷酸化。它通过增加细胞内钙浓度诱导 Ca2+依赖性细胞死亡。
T10662	Calcimycin hemicalcium salt Antibiotic A-23187 hemicalcium salt,A-23187 hemicalcium salt	Others	Others
	Calcimycin (A-23187) hemicalcium salt is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). It induces Ca2+-dependent cell death by increasing intracellular calcium concentration.
TN2169	Saikogenin D 柴胡皂甙元 D,皂苷元 D	IL Receptor; Calcium Channel; Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism
	Saikogenin D possesses a dual effect: an inhibition of A23187-induced PGE2 production without a direct inhibition of cyclooxygenase activity; and an elevation of [Ca2+]i that is attributed to Ca2+ release from intracellular stores. Saikogenin D has immuno
TN1227	25R-Inokosterone	TNF	Apoptosis
	25R-Inokosterone exhibits potent inhibition against TNF-expression levels in A23187 plus phorbol-myrisrate acetate-induced RBL-2H3 cells. 25R-Inokosterone has excellent anti-atopy activity, thus 25R-Inokosterone could be used to a large range of functional anti-atopy cosmetics.
TN1228	25S-Inokosterone	TNF	Apoptosis
	25S-Inokosterone exhibits potent inhibition against TNF-expression levels in A23187 plus phorbol-myrisrate acetate-induced RBL-2H3 cells. 25S-Inokosterone has excellent anti-atopy activity, thus 25S-Inokosterone could be used to a large range of functional anti-atopy cosmetics.

天然产物

Cat.No: T10662L

Synonym: Antibiotic A-23187,离子载体(钙镁盐混合物),A-23187

Target: Apoptosis, Antibacterial, Antibiotic, Autophagy, Antifungal

Calcimycin hemicalcium salt

Cat.No: T10662

Synonym: Antibiotic A-23187 hemicalcium salt,A-23187 hemicalcium salt

Target: Others

Cat.No: TN2169

Synonym: 柴胡皂甙元 D,皂苷元 D

Target: IL Receptor, Calcium Channel, Prostaglandin Receptor

25R-Inokosterone

Cat.No: TN1227

Target: TNF

25S-Inokosterone

Cat.No: TN1228

Target: TNF

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