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Search Results for " spla2 "

19

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T27731	sPLA2 inhibitor 1 KH-064,KH 064,KH064,5-BPP acid
	KH064 is a sPLA2-IIA inhibitor of oral activity.
T12990	sPLA2-X Inhibitor 31	Others	Others
	sPLA2-X Inhibitor 31 is a selective inhibitor of secreted phospholipase A2 type X (sPLA2-X) (IC50s of 26 nM, 310 nM, and 2230 nM for sPLA2-X, sPLA2-IIa, and sPLA2-V, respectively).
T81115	sPLA2-IIA Inhibitor
	sPLA2-IIA Inhibitor 是 FLSYK 的环状五肽类似物，具有环2-Nal-Leu-Ser-2-Nal-Arg (c2) 结构，能够特异性结合 hGIIA（人类 IIA 磷脂酶 A2），有效抑制其酯键水解活性。该化合物作为酯酶超家族的一员，主要作用于甘油磷脂 sn-2 位置的酯键，从而阻断游离脂肪酸和花生四烯酸等物质的释放。
T2044	Varespladib LY315920,伐瑞拉地,伐瑞拉迪	Phospholipase	Metabolism
	Varespladib (LY315920) 是选择性group IIA, secretory phospholipase A2(sPLA2)抑制剂，其IC50=9 nM。它对大鼠，兔，豚鼠和人等各种物种血清的sPLA2活性具有明显的抑制作用，IC50分别为 8.1 nM，5.0 nM，3.2 nM 和 6.2 nM。
T39173	Varespladib sodium LY315920 sodium,伐瑞拉迪钠；伐瑞拉地钠
	Varespladib sodium (LY315920 sodium) is a highly potent and selective inhibitor of group IIA secretory phospholipase A2 (sPLA2), with an IC50 of 9 nM. It demonstrates significant inhibitory activity against sPLA2 in serum samples from multiple species, including rat, rabbit, guinea pig, and human, with IC50 values of 8.1 nM, 5.0 nM, 3.2 nM, and 6.2 nM, respectively.
T22950	LY-311727 LY 311727	Others	Others
	secreted phospholipase A2 (sPLA2) inhibitor
T23547	YM 26734	Others	Others
	Competitive inhibitor of secretory phospholipase A2 (sPLA2)
T30831	Cgp 43182 Cgp-43182,Cgp43182
	CGP 43182 is an effective inhibitor of group IIA secretory phospholipase A2 (Group IIA sPLA2) activity in vitro, which can be used to prevent the synergistic effect of pro-inflammatory genes stimulated by cytokines mediated by NFkappaB.
T25787	Me-Indoxam Methyl indoxam,Methyl-indoxam
	Me-Indoxam is an inhibitor of sPLA2. It has no effect on arachidonic acid release and platelet activating factor synthesis.
T61168	CAY10590
	CAY10590 (GK115) is a compound that functions as an inhibitor of secreted phospholipase A2 (sPLA2). It is commonly employed in research related to chronic inflammatory kidney diseases [1].
T75589	Bitis Cornuta Venom
	Bitis Cornuta Venom (Many-horned Adder Venom) 是从 Bitis Cornuta 提取的蛇毒，含有sPLA2毒素，该毒素具有通过抑制凝血酶原复合物以发挥抗凝活性的能力，并能促使凝血酶原转化为凝血酶，引发凝块形成。
T37785	1-Palmitoyl-2-linoleoyl PE
	Phosphatidylethanolamines are important components of cell membranes and biochemical pathways of fatty acid synthesis. 1-Palmitoyl-2-linoleoyl PE (PLPE) is one of the many phosphatidylethanolamines that may be present in cellular membranes. It has been used in studies involving the biosynthesis of anandamide via the phospholipase A2 (PLA2) and lysoPLD pathways. PLPE can also be used as a specific substrate to assess the activity of sPLA2-IIA in the presence of other phospholipids.
T37580	Arachidonoyl thio-PC
	Arachidonoyl Thio-PC is a substrate for many phospholipase A2s (PLA2s) including sPLA2, cPLA2, and iPLA2. Cleavage of the sn-2 fatty acid by PLA2 results in generation of a free thiol which reacts with chromogenic reagents such as DTNB (Ellman's reagent) and DTP to allow quantitation of PLA2 activity. Isozyme-specific cPLA2 activity can be measured by excluding or inhibiting sPLA2 and iPLA2 activities in the assay.
T37221	GK187
	GK187 is an inhibitor of Group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2), an enzyme involved in basal cell metabolism. It inhibits GVIA iPLA2 by 99.8% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows less than 25% and 32.8% inhibition, respectively.
T37123	1,2-Dioctanoyl PC
	Phosphatidylcholine (PC) species are a common class of phospholipids that comprise the mammalian cell membrane. 1,2-Dioctanoyl PC is a synthetic analog of natural phosphatidylcholine species containing saturated C8:O fatty acids in the sn-1 and sn-2 positions of the glycerol backbone. It exhibits a critical micelle concentration (CMC) value of 0.25 mM at 27°C. 1,2-Dioctanoyl PC serves as an efficient substrate for phospholipase D (PLD) as well as sPLA2 isozymes from bovine pancreas and bee venom...
T37244	Palmitoyl thio-PC
	Thioester analogs of glycerophospholipids, in combination with Ellman's reagent, are convenient colorimetric substrates for the measurement of phospholipase (PL) activity. Palmitoyl thio-PC is a chromogenic PLA2 substrate that contains a palmitoyl thioester at the sn-2 position of the glycerol backbone. Hydrolysis of the thioester by PLA2 yields a free thiol that reacts readily with DTNB (Ellman's reagent) giving a bright yellow product with an absorbance maximum at 412 nm. Palmitoyl thio-PC has...
T10168	5-HT1A modulator 1 5-HT1Amodulator1	Phospholipase; Dopamine Receptor; 5-HT Receptor; Adrenergic Receptor	GPCR/G Protein; Metabolism; Neuroscience
	5-HT1A modulator 1 对 5-HT1A、α1-肾上腺素能受体和 D2 受体具有非常高的亲和力（IC50s = 2 nM、10 nM 和 40 nM）。
T35622	FKGK 18
	FKGK 18 is an inhibitor of group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2). It inhibits GVIA iPLA2 by 99.9% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows 80.8 and 36.8% inhibition, respectively. FKGK 18 inhibits iPLA2β activity in cytosolic extracts from INS-1 cells overexpressing iPLA2β (IC50 = ~50 nM) as well as iPLA2γ activity in mouse heart membrane fractions (IC50s = ~1-3 μM). It inhibits gl...
T22589	Asenapine hydrochloride	Others	Others
	Asenapine is a new atypical antipsychotic developed for the treatment of schizophrenia and acute mania associated with bipolar disorder.

化合物

sPLA2 inhibitor 1

Cat.No: T27731

Synonym: KH-064,KH 064,KH064,5-BPP acid

sPLA2-X Inhibitor 31

Cat.No: T12990

Target: Others

sPLA2-IIA Inhibitor

Cat.No: T81115

Cat.No: T2044

Synonym: LY315920,伐瑞拉地,伐瑞拉迪

Target: Phospholipase

Varespladib sodium

Cat.No: T39173

Synonym: LY315920 sodium,伐瑞拉迪钠；伐瑞拉地钠

Cat.No: T22950

Synonym: LY 311727

Target: Others

Cat.No: T23547

Target: Others

Cat.No: T30831

Synonym: Cgp-43182,Cgp43182

Cat.No: T25787

Synonym: Methyl indoxam,Methyl-indoxam

Cat.No: T61168

Bitis Cornuta Venom

Cat.No: T75589

1-Palmitoyl-2-linoleoyl PE

Cat.No: T37785

Arachidonoyl thio-PC

Cat.No: T37580

Cat.No: T37221

1,2-Dioctanoyl PC

Cat.No: T37123

Palmitoyl thio-PC

Cat.No: T37244

5-HT1A modulator 1

Cat.No: T10168

Synonym: 5-HT1Amodulator1

Target: Phospholipase, Dopamine Receptor, 5-HT Receptor, Adrenergic Receptor

Cat.No: T35622

Asenapine hydrochloride

Cat.No: T22589

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T13206	Tris(2,4-di-tert-butylphenyl)phosphate	Phospholipase	Metabolism
	Tris(2,4-di-tert-butylphenyl)phosphate 是一种从 Vitex negundoL 中分离的活性化合物，能够通过分子对接抑制了分泌性磷脂酶 A2(sPLA2)，具有抗炎作用。
T2907	Tanshinone I 丹参酮I,Tanshinone A	Phospholipase	Metabolism
	Tanshinone I (Tanshinone A) 是IIA 型人重组sPLA2(IC50=11 μM)和兔重组cPLA2(IC50=82 μM)抑制剂。

天然产物

Tris(2,4-di-tert-butylphenyl)phosphate

Cat.No: T13206

Target: Phospholipase

Cat.No: T2907

Synonym: 丹参酮I,Tanshinone A

Target: Phospholipase

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