59
11
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
TP1497L |
Mast Cell Degranulating Peptide HR-2 acetate
Mast Cell Degranulating Peptide HR-2 acetate(80388-04-1 free base) |
Others | Others |
Mast Cell Degranulating Peptide HR-2 acetate(80388-04-1 free base) 来自大黄蜂 Vespa orientalis 的肥大细胞脱粒肽,其生物学效应类似于来自蜂毒的肥大细胞脱粒肽。 | |||
TP1568 |
Mast cell degranulating peptide (28-49)
|
||
Mast cell degranulating peptide (28-49) is a bee venom depolarizer that can improve the cGMP content of cerebellum tablets in mice. | |||
TP1497 |
Mast Cell Degranulating Peptide HR-2
|
||
Peptide from giant hornet Vespa orientalis that has biological effects similar to mast cell degranulating peptide from bee venom. | |||
T9689 |
M4205
|
c-Kit | Tyrosine Kinase/Adaptors |
M4205 是一种 c-Kit 抑制剂,对外显子 11、13、17 中的 c-Kit 突变具有高活性。 | |||
T6488 |
Epinastine hydrochloride
Alesion,Epinastine HCl,WAL-801CL HCl,依匹斯汀盐酸盐,Elestat |
5-HT Receptor; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Epinastine hydrochloride (WAL-801CL HCl) 是抗组胺剂和肥大细胞稳定剂,是一种可口服的选择性组胺 H1 受体拮抗剂,可抑制 IL-8 释放,具有抗过敏作用。 | |||
T0994 |
Ketotifen fumarate
HC 20511 fumarate,富马酸酮替芬 |
PDE; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Metabolism; Neuroscience |
Ketotifen fumarate (HC 20511 fumarate) 是组胺 H1 受体和炎症介质释放的环七噻吩阻滞剂。 | |||
T15259 |
Evatanepag
CP-533536 free acid,2-[3-[N-(4-叔丁基苄基)-N-(吡啶-3-基磺酰基)氨基甲基]苯氧基]乙酸 |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
Evatanepag (CP-533536 free acid) 是一种 EP2 受体选择性前列腺素 E2 (PGE2) 激动剂,可诱导局部骨形成,EC50 为 0.3 nM。它在大鼠骨折愈合模型中以单剂量局部给药时表现出愈合骨折的能力。 | |||
T1170 |
Olopatadine hydrochloride
盐酸奥洛他定,Olopatadine HCl,KW4679,ALO4943A |
5-HT Receptor; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Olopatadine hydrochloride (ALO4943A) 是一种抗组胺药,具有稳定肥大细胞的特性,用作治疗过敏性结膜炎的滴眼液。 | |||
T15772 |
Lodoxamide tromethamine
U-42585E |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Lodoxamide tromethamine 是一种的肥大细胞稳定剂,具有抗过敏特性,可用于治疗哮喘和过敏性结膜炎的研究。 | |||
T0211 |
Azelastine
Azelastina,Astelin,Azelastinum,氮卓斯汀 |
SARS-CoV; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Neuroscience |
Azelastine (Azelastinum) 是一种选择性组胺 1 拮抗剂,可研究过敏性鼻炎、哮喘、糖尿病高脂血症和 SARS-CoV-2 。 | |||
T10811 |
Chymase-IN-1
|
Others | Others |
Chymase-IN-1 是一个有效的,有选择性的,口服有活性的人肥大细胞糜蛋白酶抑制剂,IC50 为 29 nM。 | |||
T4566 |
Lodoxamide
Lodoxamidum,洛草氨酸 |
GPR; Histamine Receptor | Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Lodoxamide (Lodoxamidum) 是一种抗过敏药物,作为肥大细胞稳定剂,对治疗哮喘和过敏性结膜炎有效。 | |||
T13623 |
Compound 48/80 trihydrochloride
C48/80 trihydrochloride |
Phospholipase | Metabolism |
Compound 48/80 trihydrochloride (C48/80 trihydrochloride) 是 N-甲基对甲氧基苯乙胺和甲醛发生缩合反应后的混合物。Compound 48/80 trihydrochloride 是一种肥大细胞 (mast cell) 脱颗粒剂和组胺 (histamine) 释放剂。Compound 48/80 trihydrochloride 对人血小板磷脂酰肌醇特异性磷脂酶 C (phosphatidylinositol-specific phospholipase C) 活性有抑制作用。 | |||
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。 | |||
T25360 |
Eclazolast
RHC2871,RHC-2871,REV2871,REV 2871,RHC 2871 |
Others | Others |
Eclazolast (RHC 2871) 是一种亲脂性抗过敏化合物,在肥大细胞模型中抑制介质释放。Eclazolast 通过在细胞内只影响与Fc(epsilon)RI 相关的直接过程而抑制细胞外分泌。Eclazolast 的效果高度依赖于触发细胞的抗原浓度。 | |||
T3979 |
Emedastine
LY188695,依美斯汀,Emadine |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Emedastine (LY188695) 是一种可口服的,选择性和高亲和力的组胺 H1受体拮抗剂,Ki 值为 1.3 nM。它是苯并咪唑衍生物,可用于过敏性鼻炎、过敏性皮肤疾病和过敏性结膜炎的研究。 | |||
T1139 |
Salbutamol
Albuterol,沙丁胺醇,AH-3365 |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
Salbutamol (Albuterol) 是短效的 β2 肾上腺素受体激动剂,用于哮喘和慢性阻塞性肺疾病(COPD) 引发的支气管痉挛的研究。 | |||
T2609 |
Masitinib
AB1010,马赛替尼 |
Apoptosis; FAK; c-Fms; FGFR; Bcr-Abl; PDGFR; Src; c-Kit; Hck | Angiogenesis; Apoptosis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors |
Masitinib (AB1010) 是生物口服可利用的选择性 c-Kit 抑制剂 (对于人重组c-Kit,IC50=200 nM),它还抑制PDGFRα/β(IC50s=540/800 nM),Lyn(对 LynB 的IC50=510 nM),Lck,较小程度上抑制FGFR3和FAK。它有抗增殖,促凋亡活性,且毒性低。 | |||
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。 | |||
T17001 |
Tazanolast
他扎司特,Tazalest,TO 188,Tazanol |
Others | Others |
Tazanolast is a selective mast-cell-stabilizing drug. | |||
T30587 |
Brl 22321
Brl22321,Brl-22321 |
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Brl 22321 is a mast cell stabilizer. | |||
T35319 |
Zy 15109
N-Acetyl-aspartyl magnesium glutamate,Zy15109,Magnesium N-acetyl-aspartylglutamate |
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Zy 15109 can be used as inhaled mast cell stabilizer. | |||
T38326 |
Cromolyn (sodium salt hydrate)
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Cromolyn is a chromone complex that acts as a mast cell stabilizer, preventing the release of histamine. Its mechanism of action is thought to involve an interference with the antigen-stimulated calcium transport across the mast cell membrane, thereby inhibiting mast cell release of histamine, leukotrienes, and other substances that cause hypersensitivity reactions. | |||
T29969 |
AMG-126737
105RSZ5CNS,AMG 126737,SCHEMBL7986111 |
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AMG-126737 is an effective human lung mast cell trypsin inhibitor with potential therapeutic effect in lung diseases. | |||
T30561 |
Bombolitin V
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Bombolitin V is a mast cell degranulosic peptide from the venom of the bumblebee Megabombus Pennsylvanicus. | |||
T68689 | 2',3'-Dihydroxypuberulin | ||
2',3'-Dihydroxypuberulin is a natural inhibitor for FcεRI expression on mast cell from Verbasucum thapsus L. 2',3'-Dihydroxypuberulin was isolated from Pterocaulon balansae and P. lanatum. | |||
T41103 |
Compound 48/80
Poly-p-methoxyphenethylmethylamine |
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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. | |||
T34796 |
TEI-9063
TEI9063 |
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TEI-9063 is a stable and highly specific prostacyclin analogue of prostacyclin receptor in mast cell tumor p-815 cells. | |||
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。 | |||
T40081 |
APC 366 TFA
|
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APC 366 (TFA) is a potent irreversible inhibitor of mast cell tryptase. It is particularly useful in studies related to allergic diseases. | |||
T71711 | ST029248 | ||
ST029248 is a potent mast cell (MC) activator, promoting de novo synthesis of cytokines and inducing the release of eicosanoids from human and mouse MCs. | |||
T14829 |
Bromoenol lactone
(6E)-Bromoenol lactone |
Phospholipase | Metabolism |
Bromoenol lactone is a suicide-based irreversible, selective, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β; IC50: ~7 μM). It inhibits antigen-stimulated mast cell exocytosis without blocking Ca2+ influx. | |||
T17099 |
Timapiprant sodium
OC000459 sodium |
Others | Others |
Timapiprant sodium inhibits mast cell activation of Th2 lymphocytes and eosinophils. Timapiprant sodium is a potent and selective D prostanoid receptor 2 antagonist. Timapiprant sodium potently displaces [3H] PGD2 from human recombinant DP2 (Ki=13 nM), ra | |||
T70193 |
APC-366 HCl
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APC-366 is a selective inhibitor of the mast cell tryptase that inhibits tryptase-induced histamine release from human tonsil and lung cells. | |||
T71814 | ST026567 | ||
ST026567 is a potent mast cell (MC) activator which promotes de novo synthesis of cytokines and induces the release of eicosanoids from human and mouse MCs. | |||
TP1408 |
Peptide 401
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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 | |||
T76621 |
Suc-Ala-Ala-Pro-Phe-SBzl
|
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Suc-Ala-Ala-Pro-Phe-SBzl 是一种化合物,可以作为大鼠小肠肥大细胞蛋白酶(RMCP I)、大鼠骨骼肌肥大细胞蛋白酶(RMCP II)和胰凝乳蛋白酶(Chymotrypsin)的底物。此外,Suc-Ala-Ala-Pro-Phe-SBzl 能够被甘氨酸(R208G)水解。 | |||
T21462 |
Olopatadine
Opatanol,Patanol,KW-4943A,KW-4679 |
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Olopatadine, an antihistamine, as well as anticholinergic and mast cell stabilizer, is used for the treatment of itching associated with allergic conjunctivitis (eye allergies). There is also a potential for Olopatadine to treat steroid rebound (red skin | |||
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。 | |||
T76095 |
Granuliberin R
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Granuliberin R, 一种两栖动物来源的新型肥大细胞脱颗粒肽,可从(Rana rugosa)蛙皮肤中分离得到。作为一种十二肽,Granuliberin R能促使大鼠腹膜肥大细胞释放颗粒和组胺。 | |||
T81515 |
Peptide 12d
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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。 | |||
T69059 |
Cromoglicate sodium hydrate
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Cromoglicic acid , cromolyn (USAN), cromoglycate (former BAN), or cromoglicate, is traditionally described as a mast cell stabilizer, and is commonly marketed as the sodium salt sodium cromoglicate or cromolyn sodium. This drug prevents the release of inflammatory chemicals such as histamine from mast cells. Because of their convenience (and perceived safety), leukotriene receptor antagonists have largely replaced it as the non-corticosteroid treatment of choice in the treatment of asthma. Cro... | |||
T73433 |
MS47134
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MS47134是一种MRGPRX4激动剂,具有高效性和选择性,其EC50为149 nM。该化合物可应用于疼痛、瘙痒以及肥大细胞介导的超敏反应研究。 | |||
T35669 |
Neuromedin C (trifluoroacetate salt)
|
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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... | |||
T60366 |
Epinastine
|
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Epinastine (WAL801) 是一种抗组胺剂和肥大细胞稳定剂。Epinastine 是一种有效的,选择性的,口服活性的组胺 H1 受体 (histamine H1 receptor) 拮抗剂。Epinastine 还抑制人嗜酸性粒细胞释放 IL-8 并具有抗过敏作用。 | |||
T36545 |
Prostaglandin D2 methyl ester
Prostaglandin D2 methyl ester |
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Prostaglandin D2 (PGD2) is the major eicosanoid product of mast cells and is produced in large quantities by hematopoietic PGD synthase during allergic and asthmatic anaphylaxis. It causes vasodilation, flushing, hypotension, and is an inhibitor of platelet aggregation. Prostaglandin D2 methyl ester (PGD2 methyl ester) is a more lipid-soluble, cell-permeable prodrug form of PGD2. It binds to the human and mouse PGD2 receptors (DP1 and CRTH2/DP2) with 5-10 fold lower affinity than PGD2. | |||
TP1956 |
PKC ζ pseudosubstrate
|
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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 ... | |||
T22189 |
APC 366
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APC 366 是肥大细胞类胰蛋白酶 (tryptase) 的选择性抑制剂,Ki 值为7.1 μM。在羊过敏性哮喘模型中,APC 366 抑制抗原诱导的早期哮喘反应 (EAR)、晚期哮喘反应 (LAR) 和支气管高反应性 (BHR)。 | |||
T70377 |
BAY 61-3606 HCl
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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... | |||
TP2058 |
Catestatin
|
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Non-competitive nicotinic cholinergic antagonist; selectively inhibits nicotinic-stimulated catecholamine secretion from chromaffin cells and noradrenergic neurons (IC50 ~ 200 nM). Blocks nicotinic-induced cationic signaling (IC50 ~ 200 - 250 nM) and inhi |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T4946 |
(+)-Columbianetin acetate
二氢欧山芹醇醋酸酯,COLUMBIANETIN ACETATE |
Others | Others |
(+)-Columbianetin acetate (COLUMBIANETIN ACETATE) 是一种 Columbianetin 异构体。其中Columbianetin 是植物抗毒素,与芹菜贮藏过程中对病原体的抗性有关,表现出良好的抗炎及抗真菌活性。 | |||
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。 | |||
T6943 |
Picropodophyllin
AXL1717,苦鬼臼脂素,Picropodophyllin (PPP),Picropodophyllotoxin,PPP,苦鬼臼毒素 |
Apoptosis; IGF-1R | Apoptosis; Tyrosine Kinase/Adaptors |
Picropodophyllin (Picropodophyllin (PPP)) 是一种选择性的胰岛素样生长因子-1受体抑制剂,IC50为1 nM。 | |||
T5S1286 |
(+)-Columbianetin
二氢山芹醇,(S)-Columbianetin,Columbianetin |
Antifungal | Microbiology/Virology |
(+)-Columbianetin ((S)-Columbianetin) 是 Columbianetin 的异构体。其中Columbianetin 是一种植物抗毒素,与芹菜贮藏过程中对病原体的抗性有关,具有良好的抗真菌和抗炎作用。 | |||
T3S0027 |
Picropodophyllotoxin
AXL 1717,Picropodophyllin,苦鬼臼毒素 |
IGF-1R | Tyrosine Kinase/Adaptors |
Picropodophyllotoxin (AXL 1717) 是一种环木脂素生物碱,存在于五月树(Podophyllum peltatum) 中,是一种具有潜在抗肿瘤活性的胰岛素样生长因子 1 受体 (IGF1R) 的小分子抑制剂。它特异性抑制 IGF1R 的活性并下调细胞表达,而不干扰其他生长因子受体的活性,例如胰岛素受体、表皮生长因子、血小板衍生生长因子、成纤维细胞生长因子和肥大/干细胞生长因子 (KIT) )。该药剂在抑制肿瘤细胞增殖和诱导肿瘤细胞凋亡方面显示出有效的活性。 IGF1R 是一种在多种人类癌症中过度表达的受体酪氨酸激酶,在多种癌细胞的生长和存活中起关键作用。 | |||
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。 | |||
TN2895 |
3,5-Dicaffeoyl-epi-quinic acid
金银花 |
IL Receptor; p38 MAPK; TNF; Caspase; JNK; Histamine Receptor | Apoptosis; GPCR/G Protein; Immunology/Inflammation; MAPK; Neuroscience; Proteases/Proteasome |
3,5-Dicaffeoyl-epi-quinic acid shows anti-inflammatory activity, it may improve mast cell-mediated inflammatory diseases. | |||
TN5647 |
Confluentin
|
||
Confluentin has antimicrobial activity against the gram-positive bacteria.Confluentin significantly inhibits compound 48/80-induced histamine release from rat peritoneal mast cells. Confluentin also shows weak cytotoxicity against four human tumor cell li | |||
TN5279 |
Zeorin
|
ATPase; Calcium Channel; Antifection; Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Neuroscience |
Zeorin shows strong inhibition activity against bacteria and fungi. It markedly exhibits inhibitory activity on histamine release from mast cell induced by DNP24-BSA, it shows potent inhibitory effect by 40% decrease of histamine release. | |||
TN3325 |
9-O-Feruloyl-5,5'-dimethoxylariciresinol
|
IL Receptor; TNF | Apoptosis; Immunology/Inflammation |
(+)-9'-O-trans-feruloyl-5,5'-dimethoxylariciresinol may have anti-allergic inflammatory effect, it can inhibit release of histamine from mast cells. It shows cytotoxicity against a small panel of human tumor cell lines, with ED50 values of 9.86 to approxi | |||
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... |