L-Homocysteic acid L-Homocysteic acid (L-HCA) is an endogenous excitatory amino acid that acts as a NMDA receptor agonist (EC50: 14 μM). L-Homocysteic acid is neurotoxic, and can be used in the research of neurological disorders.
Dimethyl L-glutamate Dimethyl L-glutamate (Dimethyl glutamate), a membrane-permeable analog of Glutamate, can stimulate insulin release induced by Glucose. Dimethyl L-glutamate suppresses the KATP channel activities. Dimethyl L-glutamate inhibits E. gracilis growth and causes abnormal cell division. Dimethyl L-glutamate can be used in the research of diabetes, glucose transport, phosphorylation, and further metabolism.
SW157765 SW157765 is a selective non-canonical glucose transporter GLUT8 (SLC2A8) inhibitor. KRAS/KEAP1 double mutant NSCLC cells are selectively sensitive to the SW157765, due to the convergent consequences of dual KRAS and NRF2 modulation of metabolic and xenobiotic gene regulatory programs.
FEMA 4809 FEMA 4809 is a TRPM8 receptor agonist (EC50=0.2 nM) for use as a cooling agent. TRPM8 is the ion channel responsible for the cool perception.
(R)-Lercanidipine-d3 hydrochloride (R)-lercanidipine D3 (hydrochloride) is a deuterium labeled (R)-Lercanidipine hydrochloride. (R)-Lercanidipine D3 (hydrochloride), the R-enantiomer of Lercanidipine, is a calcium channel blocker.
(E)-3,4,5-Trimethoxycinnamic acid (E)-3,4,5-Trimethoxycinnamic acid (TMCA) is a cinnamic acid substituted by multi-methoxy groups. (E)-3,4,5-Trimethoxycinnamic acid is an orally active and potent GABAA/BZ receptor agonist. (E)-3,4,5-Trimethoxycinnamic exhibits favourable binding affinity to 5-HT2C and 5-HT1A receptor, with IC50 values of 2.5 and 7.6 μM, respectively. (E)-3,4,5-Trimethoxycinnamic acid shows anticonvulsant and sedative activity. (E)-3,4,5-Trimethoxycinnamic acid can be used for the research of insomnia, headache and epilepsy.
Lei-Dab7 TFA Lei-Dab7 TFA is a high affinity, selective KCa2.2 (SK2) channel blocker (Kd=3.8 nM). Lei-Dab7 TFA exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, Kv and Kir2.1. Lei-Dab7 TFA increases theta-burst responses and increases LTP in rat hippocampal slices in vitro.
Flupyradifurone Flupyradifurone is a systemic nAChR agonist that interferes with signal transduction in the central nervous system of sucking pests. Flupyradifurone can be used as a butenolide insecticide.
PF-06649298 PF-06649298 is a sodium-coupled citrate transporter (NaCT or SLC13A5) inhibitor. PF-06649298 specifically interacts with NaCT with an IC50 value of 16.2 μM to inhibits the transport of citrate in human hepatocytes. PF-06649298 can be used for the research of regulating glucose metabolism and lipid metabolism.
Evifacotrep Evifacotrep, a short transient receptor potential channel 5 (TRPC5) antagonist (WO2020061162, compound 100), can be used for the research of neurological diseases.
piCRAC-1 piCRAC-1 is a potent, photoinducible Ca2+ release-activated Ca2+ (CRAC) channel inhibitor. piCRAC-1 alleviates thrombocytopenia and hemorrhage.
CaV1.3 antagonist-1 CaV1.3 antagonist-1 is a potent and highly selective CaV1.3 L-type calcium channel (LTCC) antagonist with an IC50 of 1.7 μM. CaV1.3 antagonist-1 inhibits CaV1.3 LTCC >600-fold more potently than CaV1.2 LTCC. CaV1.3 antagonist-1, a cyclopentyl derivative, has the potential for Parkinson's disease research.
Plazinemdor Plazinemdor is a N-methyl-D-aspartate(NMDA) receptor positive allosteric modulator. Plazinemdor can be uses in the research of psychiatric, neurological, and neurodevelopmental disorders, as well as diseases of the nervous system..
Zandatrigine Zandatrigine (NBI-921352) is a sodium channel protein type 8 subunit alpha (Scn8α) blocker.
AMG 333 AMG 333 is a potent and highly selective TRPM8 antagonist with an IC50 of 13 nM.
6-Benzoylheteratisine 6-Benzoylheteratisine is a naturally occurring antagonist of the Na+ channel activator aconitine.
TRPV4 agonist-1 TRPV4 agonist-1 is a transient receptor potential vanilloid 4 (TRPV4) agonist with an EC50 of 60 nM in the hTRPV4 Ca2+ assay.
Hardwickiic acid Hardwickiic acid ((-)-Hardwikiic acid) is an antinociceptive compound that blocks Tetrodotoxin-sensitive voltage-dependent sodium channels.
Radequinil Radequinil (AC-3933) is a benzodiazepine receptor (BzR) partial inverse agonist.
Flecainide Flecainide is a potent and orally active antiarrhythmic agent.
Ganoderenic acid B Ganoderenic acid B is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderenic acid B exhibits potent reversal effect on ABCB1-mediated multidrug resistance of HepG2/ADM cells to Doxorubicin.
URAT1 inhibitor 1 URAT1 inhibitor 1 (1g) is a uric acid transporter 1 (URAT1) inhibitor, with an IC50 of 32 nM.
Nav1.7-IN-3 Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM.
GlyT1 Inhibitor 1 GlyT1 Inhibitor 1 is a potent and selective GlyT1 inhibitor with an IC50 of 38 nM for rGlyT1.
Lotilaner Lotilaner is a parasiticide, acts as a potent non-competitive antagonist of insects GABACl receptors, with an IC50 of 23.84 nM for Drosophila melanogaster GABA receptor.
RU-TRAAK-2 RU-TRAAK-2 is a completely reversible TRAAK (TWIK-related arachidonic acid-stimulated K+ channel) inhibitor.
APETx2 TFA APETx2 TFA, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC50 of 63 nM.
Etripamil Etripamil (MSP-2017) is a short-acting L-type calcium-channel antagonist, can be used for the research of Paroxysmal Supraventricular Tachycardia (PSVT).
N-Bromoacetamide N-Bromoacetamide can irreversibly remove sodium channel inactivation in the cytoplasmic face of the membrane, also decreasing K current rapid inactivation.
Umbellulone Umbellulone is an active constituent of the leaves of Umbellularia californica.
YS-370 YS-370 (compound 44) is a potent, high selective, and orally active inhibitor of P-glycoprotein (P-gp). YS-370 stimulates the P-gp ATPase activity and has moderate inhibition against CYP3A4. YS-370 effectively reverses multidrug resistance (MDR) to paclitaxel and colchicine in SW620/AD300 and HEK293T-ABCB1 cells. YS-370 in combination with paclitaxel achieves much stronger antitumor activity.
P-gp inhibitor 1 P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance.
VU0529331 VU0529331 is a modestly selective non-GIRK1-containing G protein-gated, inwardly-rectifying, potassium channel (non-GIRK1/X) activator, with EC50s of 5.1 ?M and 5.2 ?M for GIRK2 and GIRK1/2 in HEK293 cells, respectively, also effective on GIRK4 homomeric channel.
Gitoxin Gitoxin, a Na+/K+-ATPase inhibitor, usually appears as a result of metabolic degradation of Digitoxin, is just the hydroxyl (ZOH) group close to the C-17β position, which changes the pharmacokinetics and pharmacodynamics of these substances considerably.
GLUT inhibitor-1 GLUT inhibitor-1 is a potent and orally active inhibitor of glucose transporters, targeting both GLUT1 and GLUT3, with IC50s of 242 nM and 179 nM, respectively.
Tivanisiran Tivanisiran (SYL1001) is a siRNA used for the study of dry eye disease.
JNJ-42253432 JNJ-42253432 is a CNS-penetrant, high-affinity and orally active P2X7 antagonist, with pKi values of 9.1 and 7.9 for rat and human P2X7 channels, respectively.
HN37 HN37 as a potent and chemically stable antiepileptic drug candidate, with an EC50 of 37 nM for KCNQ2.
(S)-(-)-Levamisole (S)-(-)-Levamisole (Levamisole), an anthelmintic agent with immunomodulatory properties.
KCNQ1 activator-1 KCNQ1 activator-1 (compound 3) is a potent activator of KCNQ1 channel.
RY796 RY796 is a potent and selective voltage-gated potassium (KV2) channel inhibitor with IC50s of 0.25 μM and 0.09 μM for KV2.1 and KV2.2.
Opiranserin hydrochloride Opiranserin (VVZ-149) hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively.
K41498 TFA K41498 TFA is a potent and highly selective CRF2?receptor antagonist with Ki?values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β?and CRF1 receptors respectively.
Etbicyphat Etbicyphat (Trimethylopropane phosphate) is a potent GABA(A) receptors competitive antagonist.
TAK-653 TAK-653, an AMPA receptor potentiator with minimal agonistic activity, produces an antidepressant-like effect with a favorable safety profile in rats.
BZAD-01 BZAD-01 is a potent, selective and orally active inhibitor of NMDA NR2B subunit, with a Ki of 72 nM.
PF-04745637 PF-04745637 is a potent and selective TRPA1 antagonist with an IC50 of 17 nM for human TRPA1.
DRB18 DRB18 is a potent pan-class GLUT inhibitor. DRB18 alters energy-related metabolism in A549 cells by changing the abundance of metabolites in glucose-related pathways. DRB18 can eventually lead to G1/S phase arrest and increase oxidative stress and necrotic cell death. DRB18 has anti-tumor activity.
Englerin A Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca2+ influx and Ca2+ cell overload.
Guanfu base A Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6).