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T0118
|
Mizolastine
SL 850324,咪唑司汀,咪唑斯汀
|
Histamine Receptor |
GPCR/G Protein;
Immunology/Inflammation;
Neuroscience |
|
Mizolastine (SL 850324) 是组胺 H1 受体拮抗剂，IC50为 47 nM。它用于治疗过敏反应，如花粉热和荨麻疹等。 |
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T2648
|
Pimecrolimus
SDZ-ASM 981,ASM 981,吡美莫司
|
Others |
Others |
|
Pimecrolimus (SDZ-ASM 981) 是一种免疫亲和素配体，能与胞质受体特异性的结合。 |
|
T3148
|
MK-571 sodium
L-660711 (sodium salt),L-660711 sodium salt,Verlukast sodium,L-660711,MK571,MK-571 sodium salt,Propanoic acid
|
Leukotriene Receptor;
LTR |
GPCR/G Protein;
Immunology/Inflammation |
|
MK-571 sodium (L-660711 sodium salt) 是一种可口服的选择性白三烯 D4受体拮抗剂，在豚鼠和人肺膜的 Ki 分别为0.22 和 2.1 nM。 |
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T8239
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Cromoglicic acid
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Others |
Others |
|
Cromoglicic acid 可防止肥大细胞释放炎性化学物质，例如组胺。 |
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T1260
|
Cromolyn sodium
Disodium Cromoglycate,FPL 670 (Cromolyn) Disodium,FPL-670,色甘酸钠,Sodium cromoglycate
|
Others;
Potassium Channel;
GSK-3;
Calcium Channel |
Membrane transporter/Ion channel;
Metabolism;
Others;
PI3K/Akt/mTOR signaling;
Stem Cells |
|
Cromolyn sodium (FPL-670) 是一种GSK-3β抑制剂，IC50为 2.0 µM，有抗过敏作用。 |
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T28972
|
Tiaramide hydrochloride
FK-1160,NTA-194,FK 1160,FK1160,tiaramide
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Others |
Others |
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Tiaramide hydrochloride (FK-1160) 是一种抗炎药，可抑制肥大细胞释放的介质的作用，并具有直接的平滑肌松弛特性。 |
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T1425
|
Pemirolast potassium
BMY 26517,TWT-8152,吡嘧司特钾
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Histamine Receptor |
GPCR/G Protein;
Immunology/Inflammation;
Neuroscience |
|
Pemirolast potassium (TWT-8152) 是 H1组胺受体拮抗剂和肥大细胞稳定剂，是一种具有抗过敏特性的嘧啶酮衍生物。 |
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T1639
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Amlexanox
氨来呫诺,CHX3673,Amoxanox,氨来诺,AA673
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IL Receptor;
FGFR;
Others;
IκB/IKK |
Angiogenesis;
Immunology/Inflammation;
NF-κB;
Others;
Tyrosine Kinase/Adaptors |
|
Amlexanox (AA673) 是一种特异性的 IKKε和 TBK1抑制剂，其 IC50=1-2 μM。 |
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T3520
|
Setipiprant
KYTH-105,塞替匹仑,ACT-129968
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GPR;
Prostaglandin Receptor |
Endocrinology/Hormones;
GPCR/G Protein;
Immunology/Inflammation |
|
Setipiprant (ACT-129968) 是一种口服的选择性 CRTH2 拮抗剂，IC50为6.0 nM。 |
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T22879
|
JNJ 10191584 maleate
JNJ 10191584 maleate salt,VUF6002 maleate
|
Histamine Receptor |
GPCR/G Protein;
Immunology/Inflammation;
Neuroscience |
|
JNJ 10191584 maleate (VUF6002 maleate) 是一种具有口服活性的选择性 H4 受体拮抗剂 (Ki = 26 nM)。 JNJ 10191584 maleate 抑制嗜酸性粒细胞和肥大细胞的趋化性(IC50 = 530 nM 和 138 nM)。 |
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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。 |
|
T0173
|
Nylidrin hydrochloride
Buphenine HCl,布芬宁盐酸盐
|
Adrenergic Receptor |
GPCR/G Protein;
Neuroscience |
|
Nylidrin hydrochloride (Buphenine HCl) 是被动致敏大鼠腹腔肥大细胞中IgE 介导的组胺释放抑制剂，具有抗过敏的功效。它也是被动致敏的豚鼠肺切片中 IgG1 介导的组胺释放抑制剂。 |
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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。 |
|
T4657
|
WHI-P97
4-(3',5'-二溴-4-羟基苯基)氨基-6,7-二甲氧基喹唑啉
|
JAK |
Angiogenesis;
Chromatin/Epigenetic;
JAK/STAT signaling;
Stem Cells |
|
WHI-P97 是一种选择性 JAK-3抑制剂，可用于预防过敏性哮喘的研究。 |
|
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。 |
|
T26470
|
A1777
AA1777,AA-1777,AA 1777
|
|
|
|
A1777, a selective 5-lipoxygenase inhibitor, reduces leukocytes proliferation without affecting the eosinophils of mast cells. |
|
T19472
|
Nedocromil sodium
Nedocromil disodium salt,FPL 59002KP
|
Others |
Others |
|
Nedocromil sodium is a pharmacologic stabilizer of mast cells, has been shown to normalize cytokine levels and attenuate cardiac remodeling. |
|
T34796
|
TEI-9063
TEI9063
|
|
|
|
TEI-9063 is a stable and highly specific prostacyclin analogue of prostacyclin receptor in mast cell tumor p-815 cells. |
|
T11473
|
GSK-5498A
|
Others |
Others |
|
GSK-5498A is a selective blocker of CARC (IC50, 1 μM). It inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species. |
|
T70193
|
APC-366 HCl
|
|
|
|
APC-366 is a selective inhibitor of the mast cell tryptase that inhibits tryptase-induced histamine release from human tonsil and lung cells. |
|
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 |
|
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... |
|
TQ0032L
|
Rosiptor acetate
AQX-1125,AQX 1125,AQX1125,AQX-1125 acetate
|
|
|
|
Rosiptor is a potent and selective SHIP1 activator. AQX-1125 inhibits Akt phosphorylation in SHIP1-proficient but not in SHIP1-deficient cells, reduces cytokine production in splenocytes, inhibits the activation of mast cells and inhibits human leukocyte |
|
T76919
|
Barzolvolimab
|
|
|
|
Barzolvolimab (CDX 0159)为人源化抗KIT IgG1单克隆抗体。其特异性地抑制KIT激活，有效降低慢性诱导性荨麻疹中皮肤肥大细胞数量及疾病活动程度。 |
|
T76095
|
Granuliberin R
|
|
|
|
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。 |
|
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) |
|
T69059
|
Cromoglicate sodium hydrate
|
|
|
|
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... |
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T82176
|
HR1
|
|
|
|
HR1是一种乳突蛋白酶，可增加人红细胞膜渗透性，并能诱导细菌细胞质膜和肥大细胞质膜透化。 |
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TP1946
|
QWF
|
|
|
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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 |
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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... |
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T36545
|
Prostaglandin D2 methyl ester
Prostaglandin D2 methyl ester
|
|
|
|
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. |
|
T80764
|
Xenopsin-Related Peptide 2
XP-2
|
|
|
|
Xenopsin-Related Peptide 2 (XP-2)，作为Xenopsin在鸟类中的对应物，具有诱导分离大鼠肥大细胞释放组胺的能力，其效力与合成Bradykinin相媲美。 |
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T38126
|
PMX 53c
|
|
|
|
Negative control for PMX 53. Active Analog also available.
Subramanian et al (2011) PMX-53 as a dual CD88 antagonist and an agonist for Mas-related gene 2 (MrgX2) in human mast cells. Mol.Pharmacol. 79 1005 PMID:21441599 |
|
T35453
|
β-Defensin-4 (human) (trifluoroacetate salt)
|
|
|
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β-Defensin-4 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts. It induces migration of monocytes in vitro when used at a concentration of 10 nM but does not affect migration of neutrophils and eosinophils. β-Defensin-4 (30 μg/ml) stimulates gene expression and production of IL-6, IL-10, CXCL10, CCL2, MIP-3α, and RANTES by keratinocytes. It also stimulates calcium mobilization, migration, and pro... |
|
T35452
|
β-Defensin-3 (human) (trifluoroacetate salt)
|
|
|
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β-Defensin-3 is a peptide with antimicrobial properties that protects the skin and mucosal membranes of the respiratory, genitourinary, and gastrointestinal tracts. It inhibits the growth of the periodontopathogenic and cariogenic bacteria F. nucleatum, S. mutans, S. sobrinus, S. salivarius, and L. casei (MICs = 12.5-100 mg/l). It also inhibits the growth of S. aureus, S. pyogenes, P. aeruginosa, E. coli, and C. albicans. β-Defensin-3 stimulates gene expression and production of IL-6, IL-10, CXC... |
|
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... |
|
T38834
|
LYP-IN-1
|
|
|
|
LYP-IN-1 is a powerful LYP inhibitor that demonstrates high potency, selectivity, and specificity, with a Ki of 110 nM and an IC 50 of 0.259 μM. Beyond its primary target, LYP-IN-1 also exhibits selectivity towards a wide range of PTPs, including SHP1 (IC 50 = 5 μM) and SHP2 (IC 50 = 2.5 μM). Additionally, LYP-IN-1 demonstrates remarkable efficacy in T- and mast cells, making it a valuable tool for investigating autoimmune disorders. |
|
TP2058
|
Catestatin
|
|
|
|
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 |
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T37492
|
11-trans Leukotriene C4
11-trans Leukotriene C4
|
|
|
|
11-trans Leukotriene C4 (11-trans LTC4) is a C-11 double bond isomer of LTC4. LTC4 undergoes slow temperature-dependent isomerization to 11-trans LTC4 during storage. 11-trans LTC4 is produced in smaller amounts relative to LTC4 in ionophore-stimulated HMC-1 cells (a human mast cell line) and equine eosinophils, but not in human neutrophils or RBL-1 cells. It is nearly equipotent with LTC4 for contraction of guinea pig parenchymal and ileum. In a radioligand binding assay using guinea pig ileum ... |
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T68701
|
Abarelix acetate
|
|
|
|
Abarelix acetate is a synthetic third generation gonadotropin-releasing hormone receptor (GnRHR) antagonist. It increases histamine release from rat peritoneal mast cells in vitro and from a human skin model ex vivo. In vivo, abarelix decreases plasma luteinizing hormone (LH) levels six hours post-treatment in castrated rats, with levels returning to baseline within 24 hours.3 Abarelix (2 mg/kg) also transiently decreases plasma testosterone levels in intact rats, with levels returning to baseli... |
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T38296
|
Alamethicin F50
Alamethicin F50
|
|
|
|
Alamethicin F50 is a peptaibol isolated from Trichoderma. It is a polymer of 20 amino acids that includes modified and non-proteinogenic amino acids. Alamethicin F50 is a mixture of 13 different peptides, with the most abundant designated as alamethicin F50/5. Alamethicin F50 forms voltage-dependent ion channels in lipid membranes and acts as a lytic agent. It induces lysis of leukocytes (IC50 = 54 and 80 μM for rat mast cells and mouse spleen lymphocytes, respectively) and exhibits antibacteria... |
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T76869
|
Lirentelimab
|
|
|
|
Lirentelimab (AK002) 是一种人源化IgG1单克隆抗体，目标为唾液酸结合Ig样凝集素8 (SIGLEC8)。该化合物通过诱导IL-5激活的嗜酸性粒细胞细胞凋亡并抑制IL-5介导的肥大细胞激活，用于嗜酸性胃炎、十二指肠炎的研究。 |
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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 ... |
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T35731
|
Deethylindanomycin
|
|
|
|
Deethylindanomycin is a polyether antibiotic that has been found in S. setonii. It is active against a variety of Gram-positive bacteria, including various strains of S. aureus and Streptococcus, as well as one strain of S. pneumoniae (MICs = 4, 4, and 2 μg/ml, respectively). It is also active against coccidia in vitro, inhibiting E. tenella development, but is inactive against E. tenella infection in chicks when administered at a dose of 200 μg/g in the diet. Deethylindanomycin acts as an ionop... |
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T37604
|
ITK inhibitor
|
|
|
|
Interleukin-2-inducible T cell kinase (ITK) is a non-receptor tyrosine kinase expressed in T cells, NKT cells and mast cells which plays a crucial role in regulating the T cell receptor (TCR), CD28, CD2, chemokine receptor CXCR4, and FcepsilonR-mediated signaling pathways. ITK inhibitors can be used for the treatment of inflammation and immune-mediated disorders. ITK inhibitor (N-[5-[[3-[(4-Acetylpiperazin-1-yl)carbonyl]-4-methyl-6-methoxy-phenyl]thio]thiazol-2-yl]-4-(N-1,2-dimethylpropylaminome... |
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TP1910
|
CALP1
|
|
|
|
Cell-permeable calmodulin (CaM) agonist that binds to the EF-hand/Ca2+-binding site; produces CaM-dependent activation of phosphodiesterase. Also binds to cytoplasmic sites on other Ca2+ channels, including NMDA and HIV-1 gp120-activated channels, inhibit |
|
T78641
|
ER-27319
|
Syk |
Angiogenesis;
Tyrosine Kinase/Adaptors |
|
ER-27319为吖啶酮衍生物，高效选择性抑制SYK，阻断其酪氨酸磷酸化和活性。本化合物阻止抗原刺激下人及大鼠肥大细胞释放过敏介质，IC50约为10 μM，适用于过敏性疾病研究。 |
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T38306
|
tetranor-PGDM
|
|
|
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Prostaglandin D2 is synthesized by hematopoietic-type PGD-synthase (H-PGDS) in mast cells and is released in large quantities during allergic and asthmatic anaphylaxis. PGD2 is also produced in the brain by lipocalin-PGD-synthase also known as β-trace. In the brain, PGD2 produces normal physiological sleep and lowering of body temperature. Further pharmacological actions include inhibition of platelet aggregation and relaxation of vascular smooth muscle. tetranor-PGDM is a major metabolite of PG... |
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T37262
|
14,15-Leukotriene E4
14,15-Leukotriene E4
|
|
|
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Leukotrienes (LTs) are a group of acute inflammatory mediators derived from arachidonic acid in leukocytes. The majority of these metabolites are formed through the 5-lipoxygenase (5-LO) pathway. 14,15-LTE4 is a metabolite of 14,15-LTC4 and 14,15-LTD4, an alternate class of LTs synthesized by a pathway involving the dual actions of 15- and 12-LOs on arachidonic acid via 15-HpETE and 14,15-LTA4 intermediates. These metabolites are classified as eoxins because they are formed mostly by eosinophils... |
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T37620
|
Leukotriene C4 methyl ester
|
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Leukotriene C4 (LTC4) is the parent cysteinyl-leukotriene produced by the LTC4 synthase-catalyzed conjugation of glutathione to LTA4. LTC4 is produced by neutrophils, macrophages, and mast cells, and by transcellular metabolism in platelets. It is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) and exhibits potent smooth muscle contracting activity. LTC4-induced bronchoconstriction and enhanced vascular permeability contribute to the pathogenesis of asthma and acute all... |
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