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31

抑制剂 & 化合物

12

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T15666	KP136 AL136	Others	Others
	KP136 is an orally effective antiallergic compound (IC50: 76.1 μg/mL for histamine release and 63 ug/mL for degranulation).
T29221	(R)-ZINC-3573 ZINC 3573	Others	Others
	(R)-ZINC-3573是一种有效且高选择性的MRGPRX2探针。(R)-ZINC-3573激活人肥大细胞系中的内源性MRGPRX2，诱导细胞脱粒和钙释放。
T2238	Cariporide 卡立泊来德,HOE-642	Sodium Channel	Membrane transporter/Ion channel
	Cariporide (HOE-642) 是一种选择性的Na+/H+交换抑制剂。
TP1909L1	CALP2 acetate(261969-04-4 free base)	CaMK; PDE	Metabolism; Neuroscience
	CALP2 acetate 是一种钙调蛋白拮抗剂，对与 CaM EF-hand/Ca2+-结合位点具有高亲和力，Kd 为 7.9 µM。它有效抑制粘附和脱粒。它也是肺泡巨噬细胞的强激活剂。它抑制 CaM 依赖性磷酸二酯酶活性并增加细胞内 Ca2+ 浓度。
TP1956L	PKC ζ pseudosubstrate acetate PKC ζ pseudosubstrate acetate (799764-07-1 free base)	PKC	Chromatin/Epigenetic; Cytoskeletal Signaling
	PKC ζ pseudosubstrate acetate 是蛋白激酶 C (PKC) ζ 的抑制剂；附着于细胞通透性触角足结构域载体肽。由 PKC ζ 假底物结构域的氨基酸 113-129 组成，通过二硫键连接到触角足结构域载体肽。 Antennapedia 肽在 4 或 37°C 时被完整细胞积极吸收，确保快速有效地吸收抑制肽。一旦进入细胞，二硫键在细胞质中被还原，导致抑制肽的释放。通过 PKC ζ 非依赖性途径诱导肥大细胞脱粒。
T63394	MrgprX2 antagonist-6
	MrgprX2 antagonist-6 是一种高效抗过敏剂，对肥大细胞脱颗粒具有抑制作用。
T0260L	Meclofenamate sodium hydrate INF 4668,CI583,CI-583,INF-4668,CI 583,INF4668
	Meclofenamate sodium is a potent non-steroidal anti-inflammatory agent, which can specifically inhibit chemokine-induced human polymorphonuclear leukocyte function: chemotaxis, degranulation, and superoxide anion free radical production.
T71472	LN6023
	LN6023 is a ACKR3/CXCR7 Superagonist for Platelet Degranulation Modulation. LN6023 effectively reduced P-selectin expression by up to 97%, suggesting to be a potential candidate for the treatment of platelet-mediated thrombosis.
T38087	20-hydroxy Leukotriene B4 20-hydroxy Leukotriene B4
	20-hydroxy LTB4 is a metabolite of LTB4 in human neutrophils. In human leukocytes, LTB4 is inactivated by the enzyme LTB4 20-hydroxylase. 20-hydroxy LTB4 is not only much less active (~5%) compared to LTB4 in causing degranulation of PMNL, but actually inhibits LTB4-induced degranulation of human neutrophils (Ki = 13.3 nM). However, 20-hydroxy LTB4 is as active as LTB4 in contracting parenchymal strips from guinea pig lung. 20-hydroxy LTB4 retains considerable ligand binding affinity at the BLT2...
TP1946	QWF
	Tripeptide substance P (SP) antagonist (IC50 = 90 μM). Also inhibits binding of SP to Mas-related GPCR (MRGPR) X2. Inhibits SP-induced IgE-independent degranulation of mast cells in vitro. Inhibits compound 48/80-induced MRGPRX2 activation and scratching
T72016	ST101036
	MC activators have recently been described as safe and effective vaccine adjuvants. ST101036 exhibited high degranulation potency in both human and mouse MCs.
T63298	B10-S
	B10-S 是有效的抗过敏剂，对 P 物质诱导的 LAD2 脱颗粒具有抑制作用。
T41103	Compound 48/80 Poly-p-methoxyphenethylmethylamine
	Compound 48/80, also known as Poly-p-methoxyphenethylmethylamine, is a commonly utilized mast cell activator in animal and tissue models. This compound exerts its effect by stimulating trimeric G-proteins at the mast cell membrane, triggering degranulation through both phospholipase C and D pathways.
T63766	MrgprX2 antagonist-7
	MrgprX2 antagonist-7 是一种抗过敏剂，具有明显的抗过敏效果，能够抑制肥大细胞脱颗粒。
T81515	Peptide 12d
	Peptide 12d为源自大胡蜂毒液的抗菌肽。其抗微生物作用是通过诱导肥大细胞脱颗粒来实现的。
T38127	pNPS-DHA
	pNPS-DHA is an arylamide derivative of docosahexaenoyl ethanolamide that has anti-allergic activity.1It inhibits degranulation of RBL-2H3 mast cells (IC50= 15 μM).pNPS-DHA (1,000 mg/kg) inhibits IgE-dependent passive cutaneous anaphylaxis (PCA) in mice. 1.Kim, I.-H., Kanayama, Y., Nishiwaki, H., et al.Structure-activity relationships of fish oil derivatives with anti-allergic activity in vitro and in vivoJ. Med. Chem.62(21)9576-9592(2019)
T37618	Leukotriene B4 dimethyl amide Leukotriene B4 dimethyl amide
	LTB4 dimethyl amide is a moderate inhibitor of LTB4-induced degranulation of human neutrophils (Ki = 130 nM) and lysozyme release from rat PMNL. LTB4 dimethyl amide appears to be an antagonist of the LTB4 receptor on guinea pig lung membranes.
T77034	Inbakicept N-803
	Inbakicept (ALT-803) 是一种 IL-15超激动剂，由 IL-15突变体和 IL-15Rα-Fc 融合体组成。Inbakicept 可放大抗 CD20单抗介导的 NK 细胞反应和抗体依赖性细胞毒性 (ADCC)。INbakicept 也增加 NK 细胞的脱粒或 IFNγ 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.
T73793	20-Carboxy-Leukotriene B4
	20-Carboxy-Leukotriene B4 (20-COOH LTB4) 是 Leukotriene B4 (LTB4) 的代谢物。20-Carboxy-Leukotriene B4 以高亲和力与 BLT1 受体结合。20-Carboxy-Leukotriene B4 抑制 LTB4 介导的中性粒细胞反应，迁移、脱粒、白三烯生物合成。
T38227	Quin C1
	Potent and selective FPR2 agonist (EC50 = 15 nM). Induces Ca2+ mobilization in FPR2 but not FPR1-transfected mast cells. Induces neutrophil chemotaxis and degranulation in vitro. Reduces neutrophil and lymphocyte counts in bronchoalveolar lavage fluid in a mouse lung injury model. Anti-inflammatory. Zhou et al (2007) Pharmacological characterization of a novel nonpeptide antagonist for formyl peptide receptor-like 1. Mol.Pharmacol. 72 976 PMID:17652444 \|Corminboeuf et al (2014) FPR2/ALXR agonist...
TP1408	Peptide 401
	Peptide 401 is an antimicrobial peptide (AMP) derived from the venom of bees and wasps. Peptide 401 induces mast cell degranulation, activating histamine release from peritoneal mast cells. Additionally, peptide 401 exhibits some anti-inflammatory activit
T37303	5-OxoETE 5-KETE,5-OxoETE
	5-OxoETE is a polyunsaturated keto acid formed by the oxidation of 5-HETE in human neutrophils by a specific dehydrogenase.[1] It stimulates cytosolic calcium levels in neutrophils with an EC50 value of 2 nM.[2] 5-OxoETE selectively stimulates the migration and degranulation of eosinophils and activates the MAPK pathway in stimulated neutrophils via a specific G protein-coupled receptor.[3],[4],[5],[6]
T70377	BAY 61-3606 HCl
	BAY 61-3606 HCl is a cell-permeable, reversible inhibitor of spleen tyrosine kinase. BAY 61-3606 HCl can inhibit degranulation and block cytokine release from mast cells. Oral administration of BAY 61-3606 to rats was shown to suppress antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema. It can also sensitize MCF-7 breast cancer cells to TNF-related apoptosis-inducing ligand (TRAIL)-mediated apoptosis by inhibiting Cdk9. This compound has been used i...
TP1956	PKC ζ pseudosubstrate
	Inhibitor of protein kinase C (PKC) ζ; attached to cell permeabilisation Antennapedia domain vector peptide. Consists of amino acids 113 - 129 of PKC ζ pseudosubstrate domain linked by a disulphide bridge to the Antennapedia domain vector peptide. The Antennapedia peptide is actively taken up by intact cells, at 4 or 37°C, ensuring rapid and effective uptake of the inhibitor peptide. Once inside the cell, the disulphide bonds are subjected to reduction in the cytoplasm leading to release of the ...
T75790	CALP2 TFA
	CALP2 TFA 是一种钙调蛋白 (CaM) 拮抗剂 (Kd 为 7.9 µM)，以亲和力结合CaMEF-hand/Ca2+结合位点。CALP2 TFA 抑制CaM 依赖性磷酸二酯酶 (phosphodiesterase) 活性并增加细胞内 Ca2+浓度。CALP2 TFA 有效抑制粘附和脱粒。CALP2 TFA 还是肺泡巨噬细胞的强激活剂。
T35669	Neuromedin C (trifluoroacetate salt)
	Neuromedin C is a bombesin-like neuropeptide that stimulates uterine smooth muscle contraction and the release of gastrin , somatostatin, and amylase in rats. Neuromedin C is a truncated form of gastrin-releasing peptide corresponding to the GRP amino acids 18-27. It inhibits GRP and bombesin binding to rat pancreatic membranes (IC50s = 0.4 and 2.2 nM, respectively), which can be reduced by sodium chloride and guanylyl imidodiphosphate . Neuromedin C induces scratching and mast cell degranulatio...
T35695	Oleic Acid-13C
	Oleic acid-13C is intended for use as an internal standard for the quantification of oleic acid by GC- or LC-MS. Oleic acid is a monounsaturated fatty acid and a major component of membrane phospholipids that has been found in human plasma, cell membranes, and adipose tissue.1,2 It contributes approximately 17% of the total fatty acids esterified to phosphatidylcholine, the major phospholipid class in porcine platelets.1 Oleic acid inhibits collagen-stimulated platelet aggregation by approximate...
T36713	Streptochlorin
	Streptochlorin is a bacterial metabolite originally isolated from Streptomyces sp. SF2583 that has diverse biological activities, including antiangiogenic, antiproliferative, and anti-allergic properties. It inhibits TNF-α-induced NF-κB transcriptional activity and decreases proliferation of human umbilical vein endothelial cells (HUVECs) when used at concentrations ranging from 5 to 20 μM. Streptochlorin (12 μg/ml) decreases viability of, as well as induces apoptosis and increases the productio...
T80265	C5a Receptor agonist, mouse, human	Complement System	Immunology/Inflammation
	C5a Receptor agonist, mouse, human 是一种源自血浆蛋白C5a C末端的生物活性肽，充当C5a受体激动剂。此化合物在调控细胞炎症反应中起关键作用，包括促进趋化性、白细胞脱颗粒、增加血管通透性以及刺激细胞因子的产生。化合物的结构中，第5位环己基丙氨酸对激动剂功能至关重要，同时末端的Arg采用d-异构体形式。
T35955	PAR2 (1-6) amide (human) (trifluoroacetate salt) PAR2 (1-6) amide (human) (trifluoroacetate salt)
	PAR2 (1-6) amide is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR2 and residues 37-42 of the full-length sequence.1It binds to NCTC 2544 cells expressing human PAR2 (Ki= 9.64 μM in a radioligand binding assay) and induces calcium mobilization in the same cells (EC50= 0.075 μM).2PAR2 (1-6) amide (100 μM) reduces colony formation of A549 lung cancer cells.1It induces superoxide prod...

化合物

Cat.No: T15666

Synonym: AL136

Target: Others

Cat.No: T29221

Synonym: ZINC 3573

Target: Others

Cat.No: T2238

Synonym: 卡立泊来德,HOE-642

Target: Sodium Channel

CALP2 acetate(261969-04-4 free base)

Cat.No: TP1909L1

Target: CaMK, PDE

PKC ζ pseudosubstrate acetate

Cat.No: TP1956L

Synonym: PKC ζ pseudosubstrate acetate (799764-07-1 free base)

Target: PKC

MrgprX2 antagonist-6

Cat.No: T63394

Meclofenamate sodium hydrate

Cat.No: T0260L

Synonym: INF 4668,CI583,CI-583,INF-4668,CI 583,INF4668

Cat.No: T71472

20-hydroxy Leukotriene B4

Cat.No: T38087

Synonym: 20-hydroxy Leukotriene B4

Cat.No: TP1946

Cat.No: T72016

Cat.No: T63298

Cat.No: T41103

Synonym: Poly-p-methoxyphenethylmethylamine

MrgprX2 antagonist-7

Cat.No: T63766

Cat.No: T81515

Cat.No: T38127

Leukotriene B4 dimethyl amide

Cat.No: T37618

Synonym: Leukotriene B4 dimethyl amide

Cat.No: T77034

Synonym: N-803

5(S),15(S)-DiHETE

Cat.No: T37650

20-Carboxy-Leukotriene B4

Cat.No: T73793

Cat.No: T38227

Cat.No: TP1408

Cat.No: T37303

Synonym: 5-KETE,5-OxoETE

BAY 61-3606 HCl

Cat.No: T70377

PKC ζ pseudosubstrate

Cat.No: TP1956

Cat.No: T75790

Neuromedin C (trifluoroacetate salt)

Cat.No: T35669

Cat.No: T35695

Cat.No: T36713

C5a Receptor agonist, mouse, human

Cat.No: T80265

Target: Complement System

PAR2 (1-6) amide (human) (trifluoroacetate salt)

Cat.No: T35955

Synonym: PAR2 (1-6) amide (human) (trifluoroacetate salt)

Cat. No.	Product Name	Target	Signaling Pathways
T8266	(R)-Citronellol D-Citronellol,(R)-(+)-β-Citronellol,(R)-3,7-二甲基-6-辛烯醇	Others; Endogenous Metabolite	Metabolism; Others
	(R)-Citronellol ((R)-(+)-β-Citronellol) 是一种存在于天竺葵精油中的醇单萜。它抑制肥大细胞的脱颗粒，并且不影响咖啡因的苦味感。它能够用于装饰性化妆品，盥洗用品以及非化妆品中。
TN1516	Cnidicin 蛇床素,4,9-双[(3-甲基-2-丁烯-1-基)氧基]-7H-呋喃并[3,2-G][1]苯并吡喃-7-酮	NOS; NO Synthase	Immunology/Inflammation
	Cnidicin 是一种香豆素，对肥大细胞脱颗粒及 RAW 264.7 细胞产生一氧化氮具有抑制作用。
TN1136	Procyanidin A1 原花青素 A1,Proanthocyanidin A1,原花色素A1	LDL; Calcium Channel; PKC	Chromatin/Epigenetic; Cytoskeletal Signaling; Membrane transporter/Ion channel; Metabolism
	Procyanidin A1 (Proanthocyanidin A1) 是一种原花青素二聚体，具有抗过敏作用，可抑制蛋白激酶 C 激活下游脱粒或 RBL-213 细胞内部储存的 Ca2+流入。
TN7075	Linocinnamarin 3-[4-(beta-D-Glucopyranosyloxy)phenyl]acrylic acid methyl ester	Phospholipase; Syk	Angiogenesis; Metabolism; Tyrosine Kinase/Adaptors
	Linocinnamarin (3-[4-(beta-D-Glucopyranosyloxy)phenyl]acrylic acid methyl ester) 是从 Fragaria ananassa Duch 中分离出来的。它对抗原刺激脱粒的抑制主要是由于 Syk/磷脂酶 Cgamma (PLCgamma) 途径的失活。
T4518	Licochalcone D	ERK; NF-κB	MAPK; NF-κB
	Licochalcone D 是一种 NF-κB p65的有效抑制剂，是一种存在于 Glycyrrhiza inflate 中的黄酮类化合物，具有抗氧化、抗炎、抗癌等作用。
T5S2343	Acetylshikonin 乙酰紫草素,Acetyl shikonin	Others; P450; AChE	Metabolism; Neuroscience; Others
	Acetylshikonin 来源于紫草根，具有抗癌、抗炎作用。它是一种 AChE 抑制剂，具有很强的抗凋亡活性。它是一种非选择性的细胞色素 P450抑制剂，对所有 P450 亚型抑制的 IC50值范围为 1.4-4.0 μM。
TN4303	Isokaempferide	ATPase; Potassium Channel; Calcium Channel; TNF; Prostaglandin Receptor	Apoptosis; GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism
	Isokaempferide shows hepatoprotective, antiproliferative, and anti-inflammatory effects, the anti-inflammatory effects can be explained, at least in part, by reducing neutrophil degranulation, myeloperoxidase activity, mediators as well as TNF-alpha secretion. Isokaempferide is used as a bronchodilator, can induce relaxation of guinea-pig isolated trachea.
TN5079	Sulochrin	HCV Protease; Antifection	Microbiology/Virology; Proteases/Proteasome
	Sulochrin shows antifungal and antibacterial activities, it can inhibit hepatitis C virus (HCV) infection in a dose-dependent manner without any apparent cytotoxicity up to 50 uM. Sulochrin has an inhibitory activity to eosinophil degranulation.
T35895	Ingenol 3,20-dibenzoate
	Ingenol 3,20-dibenzoate is a powerful activator of protein kinase C (PKC) isoforms. It effectively induces the translocation of nPKC-delta, -epsilon, and -theta as well as PKC-mu from the cytosolic fraction to the particulate fraction. Through de novo synthesis of macromolecules, it triggers apoptosis with characteristic morphology. Moreover, Ingenol 3,20-dibenzoate enhances IFN-γ production and degranulation in NK cells, particularly when stimulated by NSCLC cells[1][2].
TN5221	(-)-Variabilin
	Variabilin, a novel inhibitor of human platelet aggregation, it is a potent RGD (Arg-Gly-Asp)-containing antagonist of the fibrinogen receptor glycoprotein IIb-IIIa (GPIIb-IIIa; αIIbβ3) and the vitronectin receptor αvβ3.Variabilin is also an antimicrobial furanosesterterpene. Variabilin is an inhibitor of human secretory and cytosolic phospholipase A2 (PLA2) activities that controls eicosanoid production in vitro and in vivo, inhibits neutrophil degranulation and superoxide generation in vitro a...
TN2511	Britannilactone diacetate 1,6-O,O-Diacetylbritannilactone	IL Receptor; PARP; ROS; MAPK; Caspase; JAK; JNK; STAT	Angiogenesis; Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Immunology/Inflammation; JAK/STAT signaling; MAPK; Proteases/Proteasome; Stem Cells
	1,6-O,O-Diacetylbritannilactone(OODBL) has anti-inflammatory activity, it has a potential therapeutic efficacy on inflammatory diseases especially allergic airway disease as a lead compound. OODBL has anti-asthmatic activity, it reduces leukotriene C4 pro
T37272	9(S),12(S),13(S)-TriHOME
	9(S),12(S),13(S)-TriHOME is a linoleic acid-derived oxylipin that has diverse biological activities.1,2,3,4It has been found in various plants and is produced in human eosinophils in a 15-lipoxygenase-dependent, soluble epoxide hydrolase-independent manner.1,59(S),12(S)13(S)-TriHOME inhibits antigen-induced β-hexosaminidase release from RBL-2H3 mast cells (IC50= 28.7 μg/ml).2It inhibits LPS-induced nitric oxide (NO) production in BV-2 microglia (IC50= 40.95 μM).3In vivo, 9(S),12(S),13(S)-TriHOME...

天然产物

(R)-Citronellol

Cat.No: T8266

Synonym: D-Citronellol,(R)-(+)-β-Citronellol,(R)-3,7-二甲基-6-辛烯醇

Target: Others, Endogenous Metabolite

Cat.No: TN1516

Synonym: 蛇床素,4,9-双[(3-甲基-2-丁烯-1-基)氧基]-7H-呋喃并[3,2-G][1]苯并吡喃-7-酮

Target: NOS, NO Synthase

Cat.No: TN1136

Synonym: 原花青素 A1,Proanthocyanidin A1,原花色素A1

Target: LDL, Calcium Channel, PKC

Cat.No: TN7075

Synonym: 3-[4-(beta-D-Glucopyranosyloxy)phenyl]acrylic acid methyl ester

Target: Phospholipase, Syk

Cat.No: T4518

Target: ERK, NF-κB

Cat.No: T5S2343

Synonym: 乙酰紫草素,Acetyl shikonin

Target: Others, P450, AChE

Cat.No: TN4303

Target: ATPase, Potassium Channel, Calcium Channel, TNF, Prostaglandin Receptor

Cat.No: TN5079

Target: HCV Protease, Antifection

Ingenol 3,20-dibenzoate

Cat.No: T35895

Cat.No: TN5221

Britannilactone diacetate

Cat.No: TN2511

Synonym: 1,6-O,O-Diacetylbritannilactone

Target: IL Receptor, PARP, ROS, MAPK, Caspase, JAK, JNK, STAT

9(S),12(S),13(S)-TriHOME

Cat.No: T37272

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