models

MPP+ iodide, the metabolite of a neurotoxin MPTP, causes symptom of Parkinson's disease (PD) in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ induces dopamine transporter (DAT) externalization in dopaminergic (DA)

Streptozocin (NSC-85998) is an antibiotic that induces DNA methylation. Streptozocin is toxic to insulin-producing pancreatic islet B-cells and is commonly used in the construction of animal models of type 1 diabetes. The product is unstable in solution and is recommended to be dispensed now.

AVN-101 is a potent 5-HT7 receptor antagonist.

MPTP hydrochloride is a precursor of MPP+, a dopamine neurotoxin with blood-brain barrier permeability. MPTP hydrochloride is toxic to dopaminergic neurons, which can lead to Parkinson's disease, and is widely used in the construction of animal models of Parkinson's disease.

1. Chelidonine (Stylophorin) isolated from Chelidonium majus efficiently induced apoptosis in HeLa cells through possible alteration of p38-p53 and AKT/PI3 kinase signalling pathways. 2. Chelidonine is a promising model compound for overcoming MDR and for enhancing cytotoxicity of chemotherapeutics, especially against leukaemia cells, its efficacy needs to be confirmed in animal models. 3. Chelidonine may be a potential therapeutic agent against metastasis of invasive human cancer cells, exhibits antimigratory and antiinvasive effects in MDA-MB-231 cells, by suppressing COL-induced integrin signaling, through inhibiting the formation of the IPP complex and subsequent downregulation of IPP downstream signaling molecules, such as Akt and ERK1/2.

MW01-2-151SRM is a novel small molecule inhibitor of microglia activation that crosses the blood-brain barrier, has anti-neuroinflammatory effects, attenuates the up-regulation of glial cytokines in models of neuroinflammation, and can be used in studies of traumatic brain injury, Alzheimer's disease, and alginate toxicity.

Belnacasan (VX-765) is an orally active IL-converting enzyme/caspase-1 inhibitor.

D-Galactose (Alpha-D-galactose) is an aldohexose that exists naturally in the D-form in lactose, cerebrosides, gangliosides, and mucoproteins and is converted enzymatically into D-glucose for metabolism or polysaccharides for storage. It accelerates senescence in invertebrates and mammals and has been used as a model for aging.

Tangeretin (NSC-618905), a flavonoid from citrus fruit peels, has been proven to play an important role in anti-inflammatory responses and neuroprotective effects in several disease models and was also selected as a Notch-1 inhibitor.

1. Oxyresveratro can inhibit tyrosinase activity. 2. Oxyresveratro is useful to trauma models, as toxicity to glia could be beneficial by inhibiting reactive gliosis. 3. Oxyresveratrol (trans-Oxyresveratrol) has antioxidant activity, can reduce neuronal oxidative damage and protect hepatocytes against oxidative stress and mitochondrial dysfunction, which may be associated with activation of Nrf2.

Quercetin, a flavonoid natural product, is a SIRT1 activator. It is also a PI3K inhibitor, inhibiting PI3Kγ, PI3Kδ, and PI3Kβ with IC50 values of 2.4, 3.0, and 5.4 μM, respectively. Recognized as a heat shock protein inhibitor, Quercetin can significantly reduce exosome release in TII models by downregulating Hsp70 or Hsp90.

Hemopressin (rat) acetate is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB2 cannabinoid receptors. Hemopressin exerts antinocicep

LCB 03-0110 Dihydrochloride is a potent inhibitor of the c-Src kinase (IC50 = 1.3 nM) and tyrosine kinases in the BTK and SYK family, as well as in the DDR2 family. It inhibits LPS-induced activation of macrophages and TGF-β1-induced activation of fibroblasts in vitro, inhibits activation of macrophages and fibroblasts, and inhibits scarring in wound healing models.

Fendosal (HP-129) is a non-steroidal anti-inflammatory agent. It is 6.9 to 9.5 times more active than aspirin in the prophylactic and therapeutic adjuvant-induced polyarthritis models of chronic inflammation.

Rabeximod is a potent immunomodulator that reduces the severity of autoimmune diseases in rat models. Rabeximod inhibits arthritis in a time-dependent manner by stimulating TLR2 and TLR4 downstream to block the activation of inflammatory cells, most likely macrophages. Rabeximod effectively reduces brain antigen presentation in mice during anti-inflammatory therapy for traumatic brain injury.

Aucuparin (2,6-dimethoxy-4-phenylphenol) is a plant antibiotic with anti-inflammatory activity. Aucuparin inhibited pulmonary fibrosis in mouse models induced by bleomycin (BLM). ABTS and FRAP showed clear scavenging activity. Aucuparin inhibited superoxide production of human neutrophils induced by fmlp, and its IC50 was 17.0μM.

Duoperone is a neuroleptic agent. Duoperone shows antiemetic activity in animal models.

Tefludazine, a novel neuroleptic with a benzindone structure, is a compound with good oral activity and antagonistic effects on dopamine and 5-hydroxytryptamine receptors. Tefludazine has shown potent dopamine (DA) antagonistic activity in in vitro and in vivo test models in mice, rats and dogs. Tefludazine is a therapeutic agent used to treat psychiatric disorders.

Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting and orally active neurokinin 1 (NK1) receptor antagonist with a K i of 0.66 nM. Rolapitant hydrochloride (Rolapitant HCl) does not interact with CYP3A4. Rolapitant hydrochloride shows potent centrally-mediated anti-emetic activity in both acute and delayed ferret emesis models [1] [2].

MSC 2032964A is a potent selective ASK1 inhibitor (IC50 = 93 nM) that is oral bioavailable and brain permeable. It inhibited neuroinflammation in mouse EAE models and blocked LPS-induced phosphorylation of ASK1 and p38 in cultured mouse astrocytes.

CS1 peptide is present within type III homology connecting segment (IIICS) as well as C-274 (cell-binding domain). Fibronectin CS1 Peptide lacks the Arg-Gly-Asp-containing domain, actively inhibits tumor metastases in spontaneous and experimental metastas

DSP-0565 exhibits anti-convulsant activity and good safety margin in various models including scPTZ, 6 Hz, MES, and amygdala kindling. DSP-0565 can be used in studies about acting as a broad-spectrum anti-epileptic drug.

LCC-12 FA is a dimer composed of metformin that induces a decrease in the NAD(H) pool by targeting mitochondrial copper(ii).LCC-12 FA reduces inflammation in mouse models of bacterial and viral infections and may be used in the study of metabolic diseases.

Exisulind (CP248) induces apoptosis through the activation of protein kinase G (PKG). Exisulind exhibits antineoplastic activity in solid tumour and haematological cancer cell lines and is an inhibitor of tumour growth in rodent models of colon, prostate, bladder, mammary and lung cancer.

MIV-247 is a selective and potent inhibitor of cathepsin S (Kis 2.1, 4.2, and 7.5 nM for human, mouse, and wild monkey cathepsin S, respectively), which attenuates mechanical anomalies in preclinical models of neuropathic pain, and can be used to study cardiac muscle injury.

Beta-Sheet Breaker Peptide iAβ5 Acetate (C33H43N5O8) inhibit amyloidogenesis in rat brain models.

N4-Benzoyl-2′-deoxycytidine is a synthetic nucleoside analog of the natural nucleoside deoxycytidine (dC), a competitive inhibitor of DNA polymerase. In vitro studies have shown that it inhibits replication in viruses, bacteria and eukaryotic cells. It has also been shown to inhibit tumor cell growth in animal models.

Vatanidipine (AE0047) is a novel dihydropyridine (DHP)-type calcium channel blocker with slow-onset pharmacological actions.A slow-onset and long-lasting hypotensive action was observed in various experimental hypertensive models.

GSK778 hydrochloride hydrochloride is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 hydrochloride hydrochloride phenocopies the effects of pan-BET inhibitors in cancer models[1].

(S, R)-LSN 3318839 is an allosteric modulator of the glucagon-like peptide-3318839 receptor (GLP-1R) that has demonstrated powerful hypoglycemic effects in animal models alone or in combination with sitagliptin.

PU-H71 HCl (Zelavespib HCl) is a novel Hsp90 inhibitor, a novel purine-based analog, and a radiosensitizer that may be a promising agent for CIRT. PU-H71 HCL shows antitumor activity in many preclinical models of malignancy. PU-H71 HCL has an inhibitory effect on the protein expression levels of Rad51 and Ku70, which may be associated with the double chain break repair in the homologous recombination pathway and non-homologous end-joining pathway.

UK-240455 is a potent and selective N-methyl-D-aspartic acid (NMDA) glycine receptor antagonist with neuroprotective effects and improved motor function in Parkinson's disease models, and is a potential candidate compound for treatment of Parkinson's disease.

Eltoprazine dihydrochloride is a drug that had previously been developed for aggression, has recently been investigated for L-DOPA-induced dyskinesia in animal models of Parkinson´s disease (PD) and in dyskinetic PD patients.

ALX-1393 is a selective GlyT2 inhibitor that effectively reduces neuronal action potential activity in a concentration-dependent manner and inhibits the activity of spontaneous networks by inducing glycinergic tetanic currents in the abdominal horn of the spinal cord. Antiinjurious effects on thermal, mechanical and chemical stimuli in rat models of acute pain.

Ameltolide is an anticonvulsant agent. It has been shown to be effective at inhibiting seizures in animal models.

Flucycloxuron ((E)-flucycloxuron) is a chitin synthesis inhibitor used as a pesticide. In insect models, the inhibitor has been shown to affect several reproductive events such as the duration of preovipostion.

Aldoxorubicin hydrochloride is an albumin-binding prodrug of Doxorubicin, a DNA topoisomerase II inhibitor. Aldoxorubicin hydrochloride is released from albumin under acidic conditions. Aldoxorubicin hydrochloride exhibits potent antitumor activities in various cancer cell lines and in murine tumor models.

Tallimustine HCl is a DNA inhibitor, an AT-specific alkylated antitumor derivative of diamycin.Tallimustine HCl can be used in severe combined immunodeficiency mouse models of adult myelogenous leukemia, which can be used for the treatment of leukemia.

AMG-1694, a potent disruptor of the glucokinase–glucokinase regulatory protein (GK-GKRP) complex, operates by promoting the dissociation of this complex, thereby indirectly enhancing GK enzymatic activity with an IC50 of 7 nM. It effectively normalizes blood glucose levels in various rodent diabetes models [1] and lowers blood glucose specifically in diabetic animals without affecting normoglycemic ones. Additionally, AMG-1694 reverses the GKRP-induced inhibition of GK activity and facilitates GK translocation.

NBQX Disodium (FG9202 disodium) is a highly selective, competitive AMPA receptor antagonist with neuroprotective and anticonvulsant activity. NBQX Disodium is a salt of NBQX. NBQX is a potent and selective AMPA/rhodosinate receptor antagonist that can be used to antagonize the excitatory toxicity of glutamate. It has anticonvulsant effects in rodent models.

Hemopressin (human, mouse) acetate is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts an

Pyrazolo[1,5-a]pyrimidine 4h is a morpholine derivative that is a selective antagonist of the adenosine A2A receptor. It has been shown to be neuroprotective in animal models of Parkinson's disease and Huntington's chorea.

Ganaplacide phosphate exerts multi-stage antimalarial activity against Plasmodium symptomatic asexual blood-stage infections, and is able to prevent transmission and block infection in animal models.

Hederacolchiside E has antioxidant activity and shows neuroprotective effects in Alzheimer's disease (AD) models via modulating oxidative stress. Hederacolchiside E exhibits inhibition on lipid peroxidation of linoleic acid emulsion. Hederacolchiside E ma

CM-352 is a metalloproteinase inhibitor that reduces brain damage and improves functional recovery in rat models of cerebral hemorrhage.

Tetrahydroxystilbene-2-O-β-D-glucoside (EH-201) is a low MW inducer of erythropoietin. Tetrahydroxystilbene-2-O-β-D-glucoside induces expression of erythropoietin, PPAR-γ coactivator 1α (PGC-1α) and haemoglobin in astrocytes and PC12 neuronal-like cells. In vivo, Tetrahydroxystilbene-2-O-β-D-glucoside treatment restores memory impairment, as assessed by the passive avoidance test, in SD, Aβ and KA mouse models. In the hippocampus of mice given Tetrahydroxystilbene-2-O-β-D-glucoside in their diet, levels of erythropoietin, PGC-1α and haemoglobin were increased. Treatment with Tetrahydroxystilbene-2-O-β-D-glucoside might be a therapeutic strategy for memory impairment in neurodegenerative disease, physiological ageing or traumatic brain injury.

Talotrexin ammonium is a non-polyglutamic acid antifolate. Talotrexin ammonium inhibits tumor growth by targeting dihydrofolate reductase (DHFR), thereby improving anti-tumor activity in a wide range of cancer models, helping to inhibit tumor growth.

Lesopitron is an anxiolytic with pre- and postsynaptic 5-HT1A agonist activity and is more effective than 5-HT1A agonists in rat social interaction and marmoset anxiety models. lesopitron counteracts benzodiazepine withdrawal-induced anxiety in rodents with low acute toxicity and does not potentiate the effects of alcohol or barbiturates.

Methoxychlor, an organochlorine pesticide, is thought to be an endocrine disrupter that affects Ca2 homeostasis and cell viability in different cell models.

TC-N 22A is a strong, selective, oral active mGlu4 forward allosteric regulator (PAM) that can cross the blood-brain barrier. EC50 expression of TC-N 22A in BHK cells expressing human mGlu4 was 9 nM. TC-N 22A showed very low activity against mGlu 1, 2, 3, 5, and 7 receptors in excitation and forward allosteric models (EC50 >10 μM). TC-N 22A can be used in the study of central nervous system diseases.