PF05020182 is novel potent and selective Kv7.2/4 potassium channel opener. PF-05020182 (2) significantly inhibits convulsions in the MES assay at doses tested, consistent with in vitro activity measure. The physiochemical properties, in vitro and in vivo activities of PF-05020182 support further development as an adjunctive treatment of refractory epilepsy. Facilitating activation, or delaying inactivation, of the native Kv7 channel reduces neuronal excitability, which may be beneficial in controlling spontaneous electrical activity during epileptic seizures.

P7C3A20-analog, as known as defluoro-P7C3-A20, is a structural analogue of P7C3-A20. Compared to P7C3-A20 structure, P7C3-A20 analog has no fluorine atom in the 1,3-diaminopropane-bridge. P7C3-A20 analog was synthesized by mistake during a process to make P7C3-A20. The bioactivity of P7C3-A20 analog is unknown. P7C3-A20 analog may be used for research to compare with P7C3-A20. P7C3-A20 is a proneurogenic, neuroprotective agent. P7C3-A20 displayed increased activity and an improved toxicity profile compared to P7C3. P7C3-A20 demonstrated greater proneurogenic efficacy than a wide spectrum of currently marketed antidepressant drugs. P7C3-A20 showed neuroprotective properties in rodent models of Parkinson's disease, amyotrophic lateral sclerosis, traumatic brain injury and age-related cognitive decline.

BMS-582949 is a potent and selective P38 mitogen-activated protein kinase (P38 MAPK) inhibitor. BMS-582949 is currently under Phase II clinical trials for the treatment of inflammatory diseases. One clinical study showed that, in stable atherosclerosis, 12 weeks of treatment with BMS-582949 did not reduce arterial inflammation or hs-CRP compared to placebo, whereas intensification of statin therapy significantly decreased arterial inflammation. p38α MAP kinase plays a crucial role in regulating the biosynthesis of many inflammatory cytokines including TNFα and IL-1β.

Salmeterol is a long-acting beta2-adrenergic receptor agonist drug used in the maintenance and prevention of asthma symptoms and maintenance of chronic obstructive pulmonary disease (COPD) symptoms. Symptoms include shortness of breath, wheezing, coughing and chest tightness. Salmeterol is also used to prevent breathing difficulties during exercise (exercise induced bronchospasm). It is marketed as Serevent in the US.

CGP-7930 is a positive allosteric modulator at the GABAB receptor. It has anxiolytic effects in animal studies, and has a synergistic effect with GABAB agonists such as baclofen and GHB, as well as reducing self-administration of ethanol and cocaine.

GS-39783 is a novel positive allosteric modulators of the GABA(B) receptor, which is a compound used in scientific research which acts as a positive allosteric modulator at the GABAB receptor. It has been shown to produce anxiolytic effects in animal studies, and reduces self-administration of ethanol, cocaine and nicotine.

SCH-50911 is a selective GABAB antagonist developed by Schering-Plough Corporation. Its main applications are in pharmacology research. SCH-50911 also acts as an anticonvulsant under normal conditions, and so counteracts both the depressant and pro-convulsant effects of GHB overdose. This pharmacological profile makes SCH-50911 a promising candidate as a GHB antidote for human use, and might also make it useful for treating overdoses of other GABAB agonists such as Baclofen.

Nemiralisib, also known as GSK-2269557, is a potent and selective PI3Kδ inhibitor. GSK-2269557 is is currently in clinical trials for the treatment of respiratory diseases such as asthma and COPD. GSK-2269557 is highly selective for PI3Kδ over the closely related isoforms and are active in a disease relevant brown Norway rat acute OVA model of Th2-driven lung inflammation. PI3Kδ is highly enriched in leukocytes, making it an attractive target for the treatment of inflammatory conditions, such as asthma,6 chronic obstructive pulmonary disease (COPD), and autoimmune diseases.

CHF-5074, also known as CSP-1103, is a γ-secretase modulator. CHF-5074 reduces Aβ42 and Aβ40 secretion, with an IC50 of 3.6 and 18.4 μM respectively. CHF5074 reduces brain beta-Amyloid pathology in a transgenic mouse model of Alzheimer's Disease without causing peripheral toxicity. CHF5074 is a non-steroidal anti-inflammatory derivative holding disease-modifying potential for the treatment of Alzheimer's disease.

WWL70 is a potent inhibitor of α/β-hydrolase domain 6 (ABHD6) (IC50 = 70 nM), an enzyme which catalyzes the hydrolysis of 2-arachidonylglycerol.

T-1095 is a potent and selective inhibitor of Na±glucose cotransporters (SGLTs). T-1095 may be a useful antidiabetic drug. Long-term treatment with T-1095 causes sustained improvement in hyperglycemia and prevents diabetic neuropathy in Goto-Kakizaki Rats. Chronic administration of T-1095 (0.1% w w(-1) pellet chow, for 12 weeks) decreased blood glucose and haemoglobin A(1C) levels, and improved glucose intolerance in db/db mice. The age-related decrease in plasma insulin levels was markedly inhibited and there was a 2.5 fold increase of insulin content in the pancreas of T-1095-treated db/db mice. T-1095 improved the metabolic abnormalities and inhibit the development of diabetic complications in db/db mice.

Duvoglustat, also known as AT2220, 1-Deoxynojirimycin, Moranoline, deoxynojirimycin or DNJ, is a potent and selective alpha-glucosidase inhibitor, most commonly found in mulberry leaves. Duvoglustat is used to suppress the elevation of postprandial hyperglycemia. Duvoglustat acts as an antihyperglycemic agent by slowing the rate of carbohydrate degradation to monosaccharides. Duvoglustat inhibits glucose absorption by suppressing intestinal glucose transport. Duvoglustat accelerates glucose utilization by regulating hepatic glucose metabolism enzymes. Duvoglustat directly regulates expression of hepatic enzymes involved in glucose metabolism.

AB05831, also known as 2-Acetamido-1,2-dideoxynojirimycin, is a highly potent and specific inhibitor of beta-hexosaminidase. N-Acetyl-3-hexosaminidase (HEX) is a member of lysosomal hydrolases, which catalyzes hydrolysis of terminal, non-reducing N-acetyl-|3-D-glucosamine (GlcNAc) andN-acetyl-(3-D-galactosamine (GalNAc) residues in glycoproteins, gan-gliosides, and glycosaminoglycans (GAGs). HEX, released by chondrocytes into the extracellular compartment, promotes cartilage matrix degradation. Osteoarthritis patients have increased HEX activity in synovial fluid.

U-73343 is a negative control (or inactive analogue) of U73122, which is a putative phospholipase C inhibitor. U73343 was found to inhibit TxA2 formation; it therefore partially inhibited the rise in [Ca2+]i evoked by low concentrations of thrombin, by thapsigargin or by collagen. U73343 had a greater effect than aspirin on the action of collagen, indicating an action on the TxA2-independent component of the signal, via PLC gamma-U73343 lowered TxA2 production by inhibiting the activation of cPLA2, probably at a tyrosine phosphorylation step. U73343 seems to inhibit only the tyrosine kinases involved in the activation of PLC gamma and the generation of TxA2.

MCOPPB is a drug which acts as a potent and selective agonist for the nociceptin receptor, with a pKi of 10.07 and much weaker activity at other opioid receptors. It has only moderate affinity for the mu opioid receptor, weak affinity for the kappa opioid receptor and negligible binding at the delta opioid receptor. In animal studies, MCOPPB produces potent anxiolytic effects, with no inhibition of memory or motor function, and only slight sedative side effects which do not appear until much higher doses than the effective anxiolytic dose range. (http://en.wikipedia.org/wiki/MCOPPB)

Oliceridine, also known as TRV130, is a μ- opioid receptor agonist, that is currently under evaluation in human clinical trials for the treatment of acute severe pain. It is a functionally selective μ-opioid receptor agonist developed by Trevena Inc. TRV130 elicits robust G protein signaling, with potency and efficacy similar to morphine, but with far less β-arrestin 2 recruitment and receptor internalization, it displays less adverse effects than morphine. (http://en.wikipedia.org/wiki/TRV130).

ML-314 is a brain penetrant nonpeptidic β-arrestin biased ggonist of the neurotensin NTR1 receptor, which exhibits full agonist behavior against NTR1 (EC50 = 2.0 μM) in the primary assay and selectivity against NTR2. The effect of ML314 is blocked by the NTR1 antagonist SR142948A in a dose-dependent manner. Unlike peptide-based NTR1 agonists, ML314 has no significant response in a Ca2+ mobilization assay and is thus a biased agonist that activates the β-arrestin pathway rather than the traditional Gq coupled pathway. This bias has distinct biochemical and functional consequences that may lead to physiological advantages. ML314 displays good brain penetration in rodents, and studies examining its in vivo properties are underway.

ML3403 is a potent and selective p38 MAP kinase inhibitor. ML3403 has potent anti-inflammatory activity in airway smooth muscle.

TPT-197 is a thiophene thiourea derivative with molecule weight 197 in free base form. There is no formal name yet, we temporally call this molecule as TPT-197. Please also see similar products: TPT-197; TPT-260; TPT-172.

Chlorin E6 is a natural molecule and a promising photosensitizer. Chlorin E6 usually can be made from Live chlorella and other green plants . Chlorin E6 is an attractive photodynamic therapy (PDT) drug candidate because of (1) its high absorption in the red spectral region , and (2) its low cost to make compared to other porphyrin-based PDT drugs . Chlorin E6 exhibits advantageous photophysical properties for PDT such as having long lifetimes in their photoexcited triplet states and high molar absorption in the red region of the visible spectrum. Moreover, a 664-nm laser light can penetrate tissue deeper that the 630-nm laser light used for Photofrin. Chlorin E6 is also an important starting material for making PDT drug Talaporfin sodium (mono-L-aspartyl chlorin e6, NPe6).

Pyropheophorbide-a methyl ester (MPPa) is a PDT photosensitizer, and is also a semisynthetic natural product derived from chlorophyll a. The absorption peak of MPPa in organic solvent and in cells was at 667 and 674 nm, respectively. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide reduction assay showed that MPPa had no dark cytotoxicity.

RJR 2429 (dihydrochloride) is a nicotinic acetylcholine receptor (AChR) agonist that displays selectivity for α4β2

LH1307 is an inhibitor of the interaction between programmed cell death 1 (PD-1) and its ligand PD-L1.

(±)-Liquiritigenin is a flavonoid that has anticancer activity.

GSK 2239633A, is a potent CCR4 antagonist.

MB-0223 is a novel potent and selective STING agonist.

ST 045849 is an O-GlcNAc transferase (OGT) inhibitor, it can reduce proliferation and viability of prostate cancer cells in vitro.

Quazinone, is a phosphodiesterase 3 (PDE3) inhibitor and novel cardiotonic agent with vasodilating properties.

Nepodin, also know as Musizin; is a naphthol that has been found in Rumex and has diverse biological activities

L-778123 is an inhibitor of FPTase and GGPTase-I, which was developed in part because it can completely inhibit Ki-Ras prenylation. The combination of L-778,123 and radiotherapy at dose level 1 showed acceptable toxicity in patients with locally advanced pancreatic cancer. Radiosensitization of a patient-derived pancreatic cancer cell line was observed.