allergic asthma

Mometasone furoate (Sch32088) is a pregnadienediol derivative with anti-allergic and anti-inflammatory properties, used in the management of asthma and allergic rhinitis, as well as a topical treatment for skin disorders.

Ramatroban (BAY u3405) (BAY u3405) is a thromboxane A(2) (TxA(2)) antagonist marketed for allergic rhinitis. It has been used in trials studying the treatment of Asthma.

Budesonide (Pulmicort), an anti-inflammatory corticosteroid, has shown the effective glucocorticoid activitie and few mineralocorticoid activities. According to reports, Budesonide has extensively inhibitory effects against multiple cells types and mediators referred to allergic and nonallergic-mediated inflammatory. What's more, the anti-inflammatory action of budesonide has been revealed to contribute to the effectiveness of asthma.

Trans-Tranilast is an antiallergic drug developed by Kissei Pharmaceuticals. It was approved in 1982 for use in Japan and South Korea for bronchial asthma. Indications for keloid and hypertrophic scar were added in 1993. It has been used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis.

Cetirizine dihydrochloride (UCB P071) is an effective second-generation histamine H1 antagonist that is potent in the therapy of allergic rhinitis, confirmed urticaria, and pollen-induced asthma. Unlike other conventional antihistamines, it does not cause side effects of drowsiness or anticholinergic.

Fluticasone propionate (CCI-187881), derived from fluticasone used to remedy asthma and allergic rhinitis, is a high affinity, selective GR (glucocorticoid receptor) agonist.

Triprolidine hydrochloride monohydrate is a histamine H1 antagonist used in allergic rhinitis, asthma.

Nafamostat mesylate (FUT-175), a synthetic serine protease inhibitor, has been used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis.

KP136 (AL136) is an orally active anti-allergic compound that inhibits histamine release and is used in studies of asthma and allergic edema.

Lyn peptide inhibitor acetate is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of asthma, allergic, and other eosinophilic disorders.

A-69412 (N-1-(Fur-3-ylethyl)-N-hydroxyurea) is a reversible, specific inhibitor of the hydrophilic 5-lipoxygenase. It has the potential to treat ulcerative colitis and asthma, and possibly other inflammatory and allergic conditions.

Cromoglicic acid prevents the release of inflammatory chemicals such as histamine from mast cells.

Azelastine (Azelastinum) is a phthalazine derivative, and is an histamine antagonist and mast cell stabilizer.

AZD8848 is a selective antedrug agonist of toll-like receptor 7 (TLR7). It is developed for the research of asthma and allergic rhinitis.

Picumast shows antiallergic activity and can be utilized in the treatment of asthma. Picumast may be used in the treatment of therapeutic allergic airway diseases.

Azelastine hydrochloride (Astelin) is a phthalazinone derivative with antihistaminergic activity.

1. Kuwanon G (Moracenin B) as dual inhibitors of PTP1B and α-glucosidase enzymes, as well as insulin sensitizers, it may potentially be utilized as an effective treatment for Type II diabetes mellitus. 2. Kuwanon G has anti-inflammatory activity, it can attenuate atherosclerosis through inhibiting foam cell formation and inflammatory response. 3. Kuwanon G is a potent inhibitor of Mycobacterium tuberculosis protein tyrosine phosphatase B. 4. Kuwanon G shows acetylcholinesterase (AChE) and butyrylcholinesterase(BChE) inhibitory activities, it may be a promising candidate for preventive and therapeutic agents for Alzheimer's disease. 5. Kuwanon G prevents the pathological progression of allergic asthma through the inhibition of lung destruction by inflammation and immune stimulation. 6. Kuwanon G has antibacterial activity against oral pathogens. 7. Kuwanon G is a specific antagonist for the GRP-preferring receptor and can be useful for studying the physiological and pathological role of GRP.

Astemizole (Laridal) is a synthetic piperidinyl-benzimidazol derivative with antiallergic properties, acts as a reversible competitive inhibitor of histamine H1 receptors, with less anticholinergic effects compared to related agents. It is a long-acting, non-sedative antihistaminic used in the treatment of seasonal allergic rhinitis, asthma, allergic conjunctivitis, and chronic idiopathic urticaria.

Ayanin has vasorelaxant activity, it also may have the potential for use in treating allergic asthma.The IC(50) value of Ayanin (quercetin-3,7,4'-O-trimethylether) is 2.2microM for inhibiting interleukin (IL)-4 production from purified basophils.

TR-14035 (MDK-1191) is a dual antagonist of α4β7 α4β1 integrins (IC50s: 7 87nM).

AZD5423 is an inhaled, potent, selective, and non-steroidal modulator of the glucocorticoid receptor (GR) that effectively reduces allergen-induced responses in individuals with mild allergic asthma.

Lodoxamide (Lodoxamidum) is an antiallergic drug acting as a mast-cell stabilizer. It is effective in the treatment of asthma and allergic conjunctivitis.

GGTI 2133, a peptidomimetic inhibitor of geranylgeranyl transferase type I (GGTase I; IC50= 38 nM), exhibits 140-fold selectivity towards GGTase I compared to farnesyltransferase (IC50= 5,400 nM). The compound effectively inhibits the geranylgeranylation of RAP1A (IC50= 10 µM) without affecting the farnesylation of H-Ras (IC50= >30 µM). Moreover, GGTI 2133 reduces the growth, migration, and invasion of oral squamous cell carcinoma (OSSC) cells to 75, 45, and 27% of control levels, respectively. When administered intraperitoneally at 5 mg/kg per day, it prevents eosinophil infiltration into the airways in a mouse model of allergic bronchial asthma, although it does not reduce chemokine levels. Additionally, GGTI 2133 thwarts naloxone-induced contraction of ileum in rats experiencing morphine withdrawal syndrome and mitigates the severity of withdrawal symptoms in vivo (ED50= 0.076 mg/kg).

Mometasone furoate-d3 is a deuterated compound of Mometasone furoate. Mometasone furoate has a CAS number of 83919-23-7. Mometasone furoate is a pregnadienediol derivative ANTI-ALLERGIC AGENT and ANTI-INFLAMMATORY AGENT that is used in the management of ASTHMA and ALLERGIC RHINITIS. It is also used as a topical treatment for skin disorders.

Dihydro montelukast is a potential impurity found in commercial montelukast preparations. Montelukast (sodium salt) is a potent and selective cysteinyl leukotriene 1 (CysLT1) receptor antagonist. Formulations containing montelukast are used for the treatment of asthma as well as for the symptoms associated with allergic rhinitis.

(±)9(10)-DiHOME, the diol derivative of (±)9(10)-EpOME—a cytochrome P450-derived epoxide of linoleic acid also known as leukotoxin—is formed through the action of soluble epoxide hydrolase (sEH) in neutrophils. It exhibits toxicity towards Sf21 cells expressing sEH as well as tolacZ-expressing control cells, differing from leukotoxin which only harms sEH-containing cells. Furthermore, combined exposure to 9(10)- and 12(13)-DiHOME leads to cell death in rabbit renal proximal tubule cells by disrupting mitochondrial respiration, and causes lung injury, respiratory distress, and mortality in mice, highlighting its role as a toxic lipid mediator. Specifically, 9(10)-DiHOME has been associated with acute respiratory distress syndrome (ARDS), a severe and often deadly complication in patients with major burns. Elevated levels of this compound have been detected in the bronchoalveolar lavage fluid (BALF) of women, but not men, with chronic obstructive pulmonary disease (COPD), and its levels are also increased in patients with allergic asthma, indicating its significance in respiratory conditions.

HSR6071 is a novel orally active and potent anti-allergic agent with inhibitory effects on passive cutaneous anaphylaxis. HSR6071 showed anti-asthmatic activity in a rat model of experimental asthma.

Theophylline-d6 is intended for use as an internal standard for the quantification of theophylline by GC- or LC-MS. Theophylline is an inhibitor of phosphodiesterase. It is also an adenosine A1 and A2 receptor antagonist. Theophylline induces relaxation of isolated cat bronchial smooth muscle segments precontracted with acetylcholine. It inhibits ovalbumin-induced increases in bronchoalveolar lavage fluid (BALF) eosinophil infiltration in an ovalbumin-sensitized mouse model of allergic asthma. Formulations containing theophylline have been used in the treatment of asthma and chronic obstructive pulmonary disease (COPD).

Sappanone A is a high isoflavanone that exhibits anti-inflammatory effects by modulating Nrf2.Sappanone A attenuates allergic airway inflammation in ovalbumin-induced asthma.

Sulfuretin is a potent anti-oxidant, has protective effect against t-BHP-induced oxidative damage in human liver-derived HepG2 cells is attributable to its ability to scavenge ROS and up-regulate the activity of HO-1 through the Nrf2/ARE and JNK/ERK signa

C5a Anaphylatoxin (human) is a pro-inflammatory peptide that acts as a leukocyte chemoattractant and is used in research on inflammation and immune responses, including allergic asthma [1] [2].

(±)12(13)-DiHOME is the diol form of (±)12(13)-EpOME , a cytochrome P450-derived epoxide of linoleic acid also known as isoleukotoxin. [1] It is formed from 12(13)-EpOME by soluble epoxide hydrolase (sEH) in neutrophils. [2] 12(13)-DiHOME is toxic to Sf21 cells expressing sEH and to lacZ-expressing control cells, unlike isoleukotoxin, which is only toxic to cells containing sEH.[1] [2] Levels of 12(13)-DiHOME are increased in rat spinal cord following burn injury, and it enhances cold tolerance, increases fatty acid uptake into brown adipocytes, and decreases serum triglyceride levels in mice. Levels are also elevated in bronchoalveolar lavage fluid (BALF) in humans following exposure to biodiesel exhaust and in exhaled breath condensate in patients with allergic asthma following allergen exposure.[5] [6] Plasma levels of 12(13)-DiHOME are increased immediately following moderate-intensity exercise in mice and humans, an effect that can be prevented by brown adipose tissue removal in the mouse.[7]

3-Bromotyrosine, a product of protein oxidation, is generated after eosinophil activation during allergic responses. It serves as a biomarker for eosinophil peroxidase-induced protein oxidation both in vitro and in vivo. Beyond its association with eosinophils, 3-bromotyrosine levels are significantly elevated in peritoneal exudate from K. pneumoniae-infected mice, indicating a fivefold increase compared to uninfected controls, which implies that neutrophils may release increased levels of oxidized products during inflammation. Furthermore, in humans, allergen-challenged lung samples from patients with allergen-induced asthma show a tenfold increase in 3-bromotyrosine, highlighting its potential as a marker for oxidative stress in allergic conditions.

Chlorpheniramine maleate (NCI-C55265) is a histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma.

Cendakimab (RPC4046; ABT 308; CC-93538) is a selective humanized recombinant monoclonal antibody that targets the IL-13 molecule with high specificity, demonstrating potent affinity for both the wild-type and variant forms of human IL-13. It effectively inhibits IL-13's interaction with its receptors, IL-13Rα1 and IL-13Rα2, with IC50 values of 352 pM and 631 pM, respectively, as determined via ELISA. Furthermore, Cendakimab binds with comparable affinities of 52 pM and 50 pM to the wild-type human IL-13 and its common R110Q polymorphic variant. This antibody holds therapeutic potential for treating IL-13-related allergic and inflammatory conditions, such as asthma and eosinophilic esophagitis.

Lodoxamide tromethamine is a mast cell stabilizer with anti-allergic properties and can be used in studies about the treatment of asthma and allergic conjunctivitis.

YM-341619 (AS1617612) is a potent, orally active STAT6 inhibitor (IC50: 0.70 nM) that inhibits IL-4-induced Th2 differentiation in mouse splenic T cells with an IC50 value of 0.28 nM, without affecting Th1 cell differentiation. YM-341619 holds potential for research into allergic diseases, such as allergic asthma.

(R)-DOI hydrochloride is a 5-HT2 receptor agonist, inhibiting TNF-α-mediated proinflammatory signaling cascades and inflammation via 5-HT2A receptor activation and preventing the development of, and inflammation associated with, acute allergic asthma.

Budesonide-d8 is a deuterated compound of Budesonide. Budesonide has a CAS number of 51333-22-3. Budesonide, an anti-inflammatory corticosteroid, has shown the effective glucocorticoid activitie and few mineralocorticoid activities. According to reports, Budesonide has extensively inhibitory effects against multiple cells types and mediators referred to allergic and nonallergic-mediated inflammatory. What's more, the anti-inflammatory action of budesonide has been revealed to contribute to the effectiveness of asthma.

APC 366 is a selective inhibitor of mast cell tryptase with a Ki of 7.1 μM. It inhibits antigen-induced early asthmatic response (EAR), late asthmatic response (LAR), and bronchial hyperresponsiveness (BHR) in a sheep model of allergic asthma [1] [2].

Lyn Peptide Inhibitor TFA is a powerful, cell-permeable inhibitor specifically targeting the Lyn-coupled IL-5 receptor signaling pathway, without affecting alternative signaling pathways. It effectively prevents Lyn activation and impedes the association between Lyn tyrosine kinase and the βc subunit of IL-3/GM-CSF/IL-5 receptors. This compound is utilized in the investigation of asthma, allergic reactions, and various eosinophilic conditions [1].

Omalizumab is a recombinant humanized monoclonal antibody against human immunoglobulin E IgE)

RPT193 is an orally active CCR4 inhibitor that exhibits an inhibitory effect on the recruitment of Th2 inflammatory immune cells to inflammatory tissues and plays an important role in diseases such as atopic dermatitis, asthma and allergic inflammation.

Aderamastat (FP-025) is an orally active matrix metalloproteinase 12 (MMP-12) inhibitor used for research in allergic asthma, COPD, and pulmonary fibrosis.

Fluticasone Propionate-d5 is a deuterated compound of Fluticasone Propionate. Fluticasone Propionate has a CAS number of 80474-14-2. Fluticasone propionate, derived from fluticasone used to remedy asthma and allergic rhinitis, is a high affinity, selective GR (glucocorticoid receptor) agonist.

Adriforant tartrate hydrate, also known as ZPL-3893787 tartrate hydrate, PF-3893787 tartrate hydrate and ZPL-389 tartrate hydrate, is a novel histamine H4 receptor antagonist. Adriforant tartrate hydrate shows an excellent in vitro profile that warrants their further investigation in relevant models of human disease. Histamine H4 receptor (H4R) has become a promising target for immuno-inflammatory diseases, such as allergic rhinitis, asthma or dermal allergies.

Bakkenolide B has suppressive properties for allergic and inflammatory responses and may be utilized as a potent agent for the treatment of asthma.

AS1810722, a fused bicyclic pyrimidine derivative, is an orally active and potent inhibitor of STAT6, demonstrating an IC50 of 1.9 nM. It exhibits effective inhibition of CYP3A4, positioning it as a promising candidate for research into allergic diseases, including asthma and atopic conditions.

Desmethylazelastine, the primary active metabolite of Azelastine, undergoes oxidative metabolism via the cytochrome P450 enzyme system, exhibits a 97% protein binding rate, and has an elimination half-life of 54 hours. Azelastine, an orally active, selective, and high-affinity histamine H1-receptor antagonist, is utilized in the research of allergic rhinitis, asthma, diabetic hyperlipidemia, and SARS-CoV-2 [1] [2] [3] [4] [5].

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 allergic hypersensitivity. The concentration of LTC4 required to produce marked contractions of lung parenchymal strips and isolated tracheal rings is about 1 nM. LTC4 methyl ester is a more lipid soluble form of LTC4. The biological activity of LTC4 methyl ester has not been reported.