| DC29231 |
VGSC blocker 4 |
VGSC blocker 4 is a potent, small molecule blocker of neonatal isoform of the VGSC subtype, Nav1.5 (nNav1.5), blocks INa peak currents 25% at 1 uM; inhibits cell invasion 28% at 1 uM in human breast cancer cell line MDA-MB-231, without affecting the cell viability.. |
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| DC29233 |
PF-06526290 (PF06526290) |
PF-06526290 is a potent, selective Nav1.3 inhibitor with IC50 of 5.1 uM, interact with the Domain 4 voltage sensor domain (D4 VSD and shows no activity for Nav1.7. |
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| DC29235 |
Voluloride |
Voluloride is a conjunctival epithelial cell sodium channel (ENaC) blocker. |
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| DC28277 |
AKOS-22 |
AKOS-22 is a potent mitochondrial protein VDAC1 (voltage-dependent anion channel 1) inhibitor (Kd=15.4 μM). AKOS-22 interacts with VDAC1 and inhibiting both VDAC1 oligomerization and apoptosis. AKOS-22 protects against mitochondrial dysfunction. |
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| DC39028 |
BIA
Featured
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BIA is a potential TMBIM6 antagonist, prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, and also regulates TMBIM6-leaky Ca2+, further suppressing tumor formation and progression in cancer xenograft models.It is a potential anticancer agent that prevents the binding between mTORC2 and TMBIM6. |
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| DC39089 |
H3B-120
Featured
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H3B-120 is a competitive, selective and allosteric inhibitor of carbamoyl phosphate synthetase 1 (CPS1) with IC50 of 1.5 μM and Ki of 1.4 μM. H3B-120 exhibits anti-tumor activity. |
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| DC39092 |
Ipragliflozin (L-Proline)
Featured
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Ipragliflozin L-Proline is an orally active and selective inhibitor of SGLT2 with IC50 of 7.38 nM, 6.73 nM and 5.64 nM for human SGLT2, rat SGLT2 and mouse SGLT2, respectively. |
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| DC40065 |
Salfaprodil |
Salfaprodil (Neu2000 potassium) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA), and a free radical scavenger. Salfaprodil has excellent neuroprotection against NMDA- and free radical-induced cell death. |
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| DC40080 |
(2S)-6-Prenylnaringenin |
(2S)-6-Prenylnaringenin is the most efficient compound in forebrain. (2S)-6-Prenylnaringenin acts as a GABAA positive allosteric modulator at α+β- binding interface. |
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| DC40083 |
Dehydrosoyasaponin I |
Dehydrosoyasaponin I (Soyasaponin Be;DHS-I), a triterpene glycoside, is a potent and reversible calcium-activated potassium (maxi-K) channels activator. |
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| DC40097 |
Facinicline hydrochloride |
Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM. |
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| DC40101 |
Phenamil methanesulfonate |
Phenamil methanesulfonate, an analog of Amiloride, is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM. Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca2+ transport with an IC50 of 140 nM in a Ca2+ uptake assay. Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway. Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease.
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| DC40108 |
NF023 hexasodium |
NF023 hexasodium is a selective and competitive P2X1 receptor antagonist, with IC50 values of 0.21 μM, 28.9 μM, > 50 μM and > 100 μM for human P2X1, P2X3, P2X2, and P2X4-mediated responses respectively. |
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| DC40109 |
Broflanilide |
Broflanilide is a potential insecticide and metabolized to Desmethyl-Broflanilide, which is a potent antagonist at the insect resistant-to-dieldrin (RDL) GABA Receptor, and inhibits S. litura RDL GABAR, with an IC50 value of 1.3 nM. |
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| DC40123 |
VU0463271 quarterhydrate |
VU0463271 quarterhydrate is a potent KCC2 antagonist, with an IC50 of 61 nM. |
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| DC40133 |
QAQ dichloride |
QAQ dichloride, a photoswitchable voltage-gated Nav and Kv channels blocker, blocks channels in its trans form (of the azobenzene photoswitch), but not in its cis form. QAQ dichloride is membrane-impermeant and only infiltrates pain-sensing neurons that express endogenous import channels. QAQ dichloride acts as a light-sensitive analgesic and can be used for studying of signaling mechanisms in acute and chronic pain. |
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| DC40144 |
TTA-A2 |
TTA-A2 is a potent, selective and orally active t-type voltage gated calcium?channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy. |
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| DC40156 |
PSEM 89S TFA |
PSEM 89S TFA is a selective and brain penetrant agonists for the resulting ion channels. PSEM 89S TFA is orthogonally selective for Q79G and L141F, respectively. |
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| DC40184 |
Etiocholanolone |
Etiocholanolone (5β-Androsterone) is the excreted metabolite of testosterone and has anticonvulsant activity. Etiocholanolone is a less potent?neurosteroid positive allosteric modulator?(PAM) of the GABAA?receptor than its?enantiomer form. |
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| DC40200 |
RO2959 monohydrochloride |
RO2959 monohydrochloride is a potent and selective CRAC channel inhibitor with an IC50 of 402 nM. RO2959 monohydrochloride is a potent blocker of store operated calcium entry (SOCE) mediated by Orai1/Stim1 channels with an IC50 of 25 nM. RO2959 monohydrochloride is also a potent inhibitor of human IL-2 production, and potently blocks T cell receptor triggered gene expression and T cell functional pathways. |
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| DC40208 |
PF-06305591 dihydrate |
PF-06305591 dihydrate is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile. |
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| DC40224 |
3-Methyl-GABA |
3-Methyl-GABA is an activator of GABA aminotransferase with anticonvulsant activity. |
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| DC40241 |
Flufiprole |
Flufiprole is a nonsystemic phenylpyrazole insecticide targeting the GABA receptor used in the rice field. Flufiprole is excellent in controlling a wide range of pests. |
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| DC40291 |
Roemerine |
Roemerine, an aporphine alkaloid, isolated from the leaves of Annona senegalensis, functions by interacting with P-glycoprotein. Roemerine reverses the multidrug-resistance phenotype with cultured cells. |
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| DC40337 |
Brevetoxin B |
Brevetoxin B (Brevetoxin-2; PbTx-2) is a polyketide neurotoxin produced by Karenia species and other dinoflagellates. Brevetoxin B binds to site 5 on the alpha subunit of voltage-gated sodium channels (IC50=15 nM) on neurons at the neuromuscular junction, causing the channel to open irreversibly at potentials more negative than normal, discharging action potentials repetitively. Brevetoxin B is ichthyotoxic at nanomolar concentrations and is responsible for an illness described as neurotoxic shellfish poisoning. |
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| DC40353 |
Quisqualic acid |
Quisqualic acid (L-Quisqualic acid), a natural analog of glutamate, is a potent and pan two subsets (iGluR and mGluR) of excitatory amino acid (EAA) agonist with an EC50 of 45 nM and a Ki of 10 nM for mGluR1R. Quisqualic acid is isolated from the fruits of Quisqualis chinensis. |
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| DC40401 |
AMP-PNP tetralithium |
AMP-PNP tetralithium (Adenylyl-imidodiphosphate tetralithium) is a non-hydrolysable analogue of ATP and inhibits KATP channels. |
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| DC40425 |
Isotachysterol 3 |
Isotachysterol 3 is an analog of 1,25-dihydrox Vitamin D3. Isotachysterol 3 stimulates intestinal calcium transport and bone calcium mobilization in anephric rats. |
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| DC40465 |
Ned-K |
Ned-K is a nicotinic acid adenine dinucleotide phosphate (NAADP) antagonist. Ned-K is effective at dampening simulated ischaemia and reperfusion (sIR)-induced Ca2+ oscillations in cardiomyocytes. |
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| DC40574 |
TPC2-A1-N |
TPC2-A1-N is a novel, lipophilic, membrane permeable isoform-selective small molecule agonist of two-pore channel 2 (TPC2). TPC2-A1-N plays its role by mimicking the physiological actions of NAADP and PI(3,5)P2?through independent binding sites. TPC2-A1-N has inverse effects on key lysosomal activities and increases the pH in the lysosomal lumen in a TPC2-dependent manner. |
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