Capsiate, as a capsaicin analogue extracted from a non-pungent cultivar of CH-19 sweet red pepper, is an orally active agonist of TRPV1[1].
QNZ46 is a NR2C/NR2D-selective NMDA receptor non-competitive antagonist (IC50 values are 3, 6, 229, and >300, >300 μM for NR2D, NR2C, NR2A, NR2B, and GluR1, respectively). IC50 value: 3 μM (for NR2D), 6 μM (for NR2C), 229 μM (for NR2D NR2A)Target: NR2D, NR2C, NR2Ain vitro: QNZ46 is a noncompetitive inhibitor of GluN2C/D containing NMDA receptors. KD and IC50 values for binding and inhibition of GluN1/Glun2D receptors by QNZ46 are 4.9 and 3.9 μM, respectively. QNZ46 does not compete for binding of glutamate or glycine, but QNZ46 receptor binding requires the binding of glutamate to the GluN2 subunit.
Nicorandil is potassium channel activator.Target: Potassium ChannelNicorandil is a vasodilatory drug used to treat angina. Nicorandil stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP). cGMP activates protein kinase G (PKG) which phosphorylates and inhibits GTPase RhoA and decreases Rho-kinase activity. Reduced Rho-kinase activity permits an increase in myosin phosphatase activity, decreasing the calcium sensitivity of the smooth muscle. PKG also activates the sarcolemma calcium pump to remove activating calcium. PKG acts on K+ channels to promote K+ efflux and the ensuing hyperpolarization inhibits voltage-gated calcium channels. Overall, this leads to relaxation of the smooth muscle and coronary vasodilation [1, 2].
Brompheniramine ((±)-Brompheniramine) is a potent and orally active antihistamine of the alkylamine class. Brompheniramine is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research[1][2][3][4].
Ranolazine(RS-43285) is an antianginal agent with antiarrhythmic properties that achieves its effects via a novel mechanism of action (inhibition of the late phase of the inward sodium current), without affecting heart rate or blood pressure (BP). IC50 value:Target: sodium-dependent calcium channelRanolazine is currently approved for use in chronic angina. The basis for this use is likely related to inhibition of late sodium channels with resultant beneficial downstream effects. Randomized clinical trials have demonstrated an improvement in exercise capacity and reduction in angina episodes with ranolazine.
MCHr1 antagonist 2 is an antagonist of melanin concentrating hormone receptor 1, with an IC50 of 65 nM; MCHr1 antagonist 2 also inhibits hERG, with an IC50 of 4.0 nM in IMR-32 cells.
T16Ainh-A01, an aminophenylthiazole, is a potent transmembrane protein 16A (TMEM16A) inhibitor, inhibiting TMEM16A-mediated chloride currents with an IC50 value of ~1 µM. TMEM16A (ANO1) functions as a calcium-activated chloride channel (CaCC)[1][2].
Sinapine is an alkaloid from seeds of the cruciferous species which shows favorable biological activities such as antioxidant and radio-protective activities.
(E)-4-Oxo-2-nonenal (4-ONE) is one of the major hemolytic decomposition products of lipid hydroperoxides. (E)-4-Oxo-2-nonenal is a major product of the FeII-mediated breakdown of lipid hydroperoxides. (E)-4-Oxo-2-nonenal is a potent transient receptor potential ankyrin 1 (TRPA1) agonist[1][2][3].
Ruzinurad is a highly selective URATl inhibitor (WO2020088641, compound I). Ruzinurad can be used in the study of hyperuricemia[1].
UBP 302, the S enantiomer, is a potent and selective GluK1 (GluR5)-subunit containing kainate receptor antagonist (apparent Kd=402 nM), and displays very little affinity on GluK2 (GluR6) kainate receptors. Anxiolytic effects[1][2][3].
L-364,373 (R-L3) is a voltage-gated Kv7.1 (KCNQ1)/mink channels activator. L-364,373 activates Iks (slow delayed rectifier potassium current) and shortens action potential duration in guinea pig cardiac myocytes, and suppresses early afterdepolarizations in rabbit ventricular myocytes[1].
Camphor ((±)-Camphor) is a topical anti-infective and anti-pruritic and internally as a stimulant and carminative. However, Camphor is poisonous when ingested. Antiviral, antitussive, and anticancer activities[1]. Camphor is a TRPV3 agonist[2].
L-Phenylalanine-13C9,d8,15N ((S)-2-Amino-3-phenylpropionic acid-13C9,d8,15N) is the deuterium, 13C-, and 15-labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].
Ser-Ala-alloresact is a sperm activating peptide (SAP). The peptides released from eggs of marine invertebrates play a central role in fertilization[1][2].
6-Benzoylheteratisine is a naturally occurring antagonist of the Na+ channel activator aconitine[1].
LY 233536 is a competitive NMDA receptor antagonist[1].
TDN345 is a Ca2+ antagonist, used for the treatment of vascular and senile dementia including Alzheimer's disease.
Lesogaberan (AZD-3355) is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. Binding affinity (Kis) of 5.1 nM and 1.4 μM for rat brain GABAB and GABAA receptors, respectively[1].
HC-067047 is a potent and selective TRPV4 antagonist with IC50s of 48 nM, 133 nM, and 17 nM for human, rat, and mouse TRPV4.
tracurium (BW-33A free acid) is a potent, competitive and non-depolarizing neuromuscular blocking agent.Atracurium also is an AChR receptor antagonist. Atracurium induces bronchoconstriction and neuromuscular blockade. Atracurium promotes astroglial differentiation[1][2][3][4][5].
Bumetanide D5 is a deuterium labeled Bumetanide. Bumetanide is a selective Na+-K+-Cl- (NKCC1) inhibitor, weakly inhibits NKCC2, with IC50s of 0.68 and 4.0 μM for hNKCC1A and hNKCC2A, respectively[1].
JNc-440 is a small molecule that significantly and specifically strengthens the TRPV4-KCa2.3 interaction in mouse endothelial cells, but does not systemically activate TRPV4 and KCa2.3; shows affinity for both TRPV4 and KCa2.3, enhances vasodilation and exerts antihypertensive effects in mice.
Piperidine-4-sulfonic acid is a potent GABA agonist with an IC50 of 0.034 μM for the inhibition of the binding of H-GABA[1].
Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
Talampanel is a potent and selective AMPA-receptor antagonist, is a potential new antiepileptic drug (AED). Target: AMPA [1]in vitro: Talampanel is a glutamate receptor inhibitor with anti-seizure activity.in vivo： Talampanel reduces motoneuronal calcium in a mouse model of ALS, but its effi cacy declines as the disease progresses, suggesting that medication initiation in the earlier stages of the disease might be more effective. [2]
PEAQX(NVP-AAM 077) is a potent and orally active NMDA antagonist with a 15-fold preference for human NMDA receptors with the 1A/2A(IC50=270 nM), rather than 1A/2B(29,600 nM).IC50 value: 270 nM(hNMDA A1/A2) [1]Target: NR2A antagonistin vitro: PEAQX has a high binding affinity for NMDA receptors (IC50=8 nM), and a functional preference in excess of 100-fold for hNMDA 1A/2A (IC50=of 270 nM) over 1A/2B receptors (IC50=29,600 nM) [1].in vivo: PEAQX is practically inactive in Xenopus oocytes expressing hNMDA 1A/2B receptors, displays an ED50 value of 23 mg/kg in the MES test [1]. Sprague-Dawley rats were treated on PN7, PN9, and PN11 with PCP (10 mg/kg), PEAQX (NR2A-preferring antagonist; 10, 20, or 40 mg/kg), or ifenprodil (selective NR2B antagonist; 1, 5, or 10 mg/kg) and sacrificed for measurement of caspase-3 activity (an index of apoptosis) or allowed to age and tested for locomotor sensitization to PCP challenge on PN28-PN35. PCP or PEAQX on PN7, PN9, and PN11 markedly elevated caspase-3 activity in the cortex; ifenprodil showed no effect. Striatal apoptosis was evident only after subchronic treatment with a high dose of PEAQX (20 mg/kg). Animals treated with PCP or PEAQX on PN7, PN9, and PN11 showed a sensitized locomotor response to PCP challenge on PN28-PN35 [2].
Dihydrocapsiate, as a compound of capsinoid family, is an orally active TRPV1 agonist. Dihydrocapsiate can be used for the research of metabolism disease[1].
Phellamurin is a plant flavonone glycoside from the leaves of Phellodendron amurense and inhibits intestinal P-glycoprotein. Phellamurin also inhibits egg laying by Papilio protenor. Phellamurin induces cells apoptosis and has anti-tumor activity[1][2][3].
L-Phenylalanine-d5 is the deuterium labeled L-Phenylalanine. L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca+ channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals[1][2][3][4].