1ethyl2benzimidazolinone

Cyclosporin A is a natural product and an active fungal metabolite, classified as a cyclic polypeptide immunosuppressant. It binds to cyclophilin and inhibits the activity of calcineurin (IC₅₀ = 7 nM) as well as CD11a CD18 adhesion molecules. It is commonly used to induce uremia models.

Cyclophosphamide is an alkylating agent type of anti-tumor drug, and its main target is DNA. Cyclophosphamide inhibits the proliferation of tumor cells by undergoing alkylation reactions with DNA, interfering with the replication and transcription processes of DNA.

Semaxinib (SU5416) is a potent and selective VEGFR2 inhibitor (IC50: 1.23 μM), exhibiting a 20-fold greater selectivity for VEGFR2 over PDGFRβ, with no activity against InsR, EGFR, and FGFR. Semaxinib reversibly inhibits ATP binding to the tyrosine kinase domain of VEGFR2, potentially inhibiting VEGF-stimulated endothelial cell migration and proliferation, thereby reducing tumor microvasculature.

Trimethylamine N-oxide (TMAO) is a gut microbiota-dependent metabolite derived from dietary choline, betaine, and carnitine. It induces inflammation by activating the ROS/NLRP3 inflammasome and promotes fibroblast differentiation through the activation of the TGF-β/Smad2 signaling pathway. TMAO is commonly used to induce cardiac fibrosis models.

Prostaglandin E2 (PGE2) is a natural hormone-like substance involved in various physiological functions, including the contraction and relaxation of smooth muscles, dilation and constriction of blood vessels, regulation of blood pressure, and modulation of inflammation. It can be used to induce neuropathic pain models.

Taurocholic acid (N-Choloyltaurine) is a bile acid involved in fat emulsification, possessing notable biological and immunomodulatory activities. It can inhibit bile duct injury induced by hepatic artery ligation by upregulating VEGF-A expression and protect cholangiocytes from TNF-α-induced damage via a PI3K-mediated pathway, and is commonly used to induce pancreatitis models.

Phorbol 12-myristate 13-acetate (PMA) is a natural phorbol ester that acts as an activator of PKC, SphK, and NF-κB, and is commonly used to induce differentiation of THP-1 cells and establish dermatitis models.

Aspirin is an orally active, selective, and irreversible inhibitor of COX-1 and COX-2 with IC₅₀ values of 5 and 210 μg mL, respectively. It induces apoptosis, inhibits NF-κB activation and platelet prostaglandin synthesis, thereby preventing thrombosis. Additionally, it acts as a histone deacetylase inhibitor that upregulates p21, exhibiting anti-inflammatory, antipyretic, analgesic, and anti-platelet aggregation activities. Aspirin is commonly used to induce gastric ulcer models.

Urethane (Ethyl carbamate; Ethylurethane) is a byproduct formed during the fermentation process of various foods. As an ethyl ester of carbamic acid, it has the ability to inhibit the growth of bacteria, sea urchin eggs, protozoa, and plant tissues, and is commonly used for establishing lung cancer models.

Adenine is a purine-derived nucleobase and one of the four bases of DNA. It is an important chemical component of both DNA and RNA, involved in cellular respiration, the formation of ATP and coenzymes NAD and FAD, as well as protein synthesis. Adenine is commonly used to induce chronic kidney injury models.

Indomethacin is an orally active nonsteroidal anti-inflammatory drug (NSAID) that non-selectively inhibits cyclooxygenase enzymes COX-1 and COX-2, with IC₅₀ values of 18 nM and 26 nM, respectively. It exhibits good blood-brain barrier permeability and shows significant anti-inflammatory, anti-tumor, and anti-infective activities. Indomethacin is widely used in research related to cancer, inflammation, and viral infections, and is also commonly used to induce gastric ulcer models in animals.

Cholesterol is the primary sterol in mammals, accounting for approximately 20–25% of the plasma membrane structure. It plays a key role in regulating membrane fluidity, permeability, and protein function. As an endogenous agonist of estrogen-related receptor α (ERRα), cholesterol is widely involved in metabolic regulation and serves as a precursor for the synthesis of hormones and bile acids. It is commonly used in experimental models of hyperlipidemia.

L-DOPA (Levodopa) is an orally active metabolic precursor of the neurotransmitter dopamine. It can cross the blood-brain barrier and be converted into dopamine in the brain. L-DOPA exhibits anti-hyperalgesic effects and holds potential in Parkinson’s disease research, and it can also be used to induce Parkinson’s disease models.

Monocrotaline is an 11-membered macrocyclic pyrrolizidine alkaloid extracted from the seeds of Crotalaria plants. It inhibits organic cation transporters OCT-1 and OCT-2, with IC50 values of 36.8 µM and 1.8 mM, respectively. Monocrotaline exhibits antitumor activity and shows certain cytotoxicity against liver cancer cells such as HepG2. It is also commonly used to induce pulmonary arterial hypertension models in rodents.

5-Hydroxytryptophan (NSC-92523) is a metabolite of tryptophan and a direct precursor of serotonin. It is a substrate of aromatic amino acid decarboxylase and can be used to induce depression models.

L-Arginine (L-Arg) is a substrate of endothelial nitric oxide synthase (eNOS). L-Arginine is transported to vascular smooth muscle cells via a family of cationic amino acid transporters and is metabolized to nitric oxide, polyamines, or L-proline. L-Arginine is a potent vasodilator and can be used to induce experimental acute pancreatitis.

Norepinephrine is an alkaloid neurotransmitter and an effective adrenergic receptor (AR) agonist that activates α1, α2, and β1 receptors. It is commonly used as a vasoactive agent for the treatment of shock and can also be used to induce cardiomyopathy models.

Terephthalic acid is an isomer and a precursor of the polyester PET. It is used in the production of textiles and plastics, and can also be used to establish skin cancer models.

Sodium taurocholate is a biologically active compound that can inhibit bile duct injury induced by hepatic artery ligation by upregulating VEGF-A expression. It also exhibits immunomodulatory effects and can be used to induce pancreatitis models.

Bicuculline is an alkaloid extracted from Corydalis decumbens, acting as a competitive antagonist of the neurotransmitter GABAA receptor (IC50 = 2 μM). It also blocks Ca2+-activated potassium (SK) channels and inhibits slow afterhyperpolarization (slow AHP). Bicuculline has anticonvulsant effects and is commonly used to establish mouse seizure models.

Colchicine is an orally active natural alkaloid that acts by inhibiting microtubule polymerization (IC50 = 3 nM) and as a competitive antagonist of the α3 glycine receptor. It possesses broad anti-inflammatory, immunosuppressive, and antifibrotic activities, can inhibit NLRP3 inflammasome activation to prevent NSAID-induced small intestine injury, holds potential for gouty arthritis and rheumatoid arthritis research, and is commonly used to establish Alzheimer’s disease models.

Capsaicin is an active natural component found in chili peppers and acts as a TRPV1 agonist (EC50 = 0.29 μM). It possesses multiple activities, including pain relief, antitumor, anti-inflammatory, antioxidant, and neuroprotective effects, as well as some neurotoxicity. Capsaicin can be used to establish itch models.

PLX5622 hemifumarate is a highly selective, blood-brain barrier-permeable, and orally active CSF1R inhibitor with an IC50 of 0.016 μM and a Ki of 5.9 nM. It can be used to eliminate proliferating and specific microglia before and during disease progression and is applicable for inducing Alzheimer's disease models.

Amiodarone is an antiarrhythmic compound that inhibits ATP-sensitive potassium channels (IC₅₀ = 19.1 μM) and can induce pulmonary toxicity. It has shown some antiviral activity in diseases caused by SARS-CoV-2 and is commonly used to establish animal models of pulmonary fibrosis.