| DC47246 |
SB 452533 |
SB 452533 is a potent and selective TRPV1 antagonist with the pKb of 7.8. |
|
| DC47255 |
Co 101244 hydrochloride |
Co 101244 (PD 174494) hydrochloride is a NR2B-containing NMDA receptor antagonist. |
|
| DC47315 |
ML-SI3
Featured
|
ML-SI3 is a potent TRPML channel inhibitor with IC50s of 4.7 µM and 1.7 µM for TRPML1 and TRPML2, respectively. |
|
| DC47321 |
Endovion (NS 3728)
Featured
|
Endovion (NS 3728, SCO-101) is an potent anion channel inhibitor that blocks the Volume Regulated Anion Channels (VRAC). |
|
| DC47322 |
4-(Phenyldiazenyl)benzoic acid |
4-(Phenyldiazenyl)benzoic acid is a photosensitive and photoswitchable TRPA1 agonist that can be used as pharmacological tools for study of pain signaling. |
|
| DC47323 |
TRPA1 Antagonist 3 |
TRPA1 Antagonist 3 is a photoswitchable TRPA1 agonist that enables optical control of the TRPA1 channel. |
|
| DC47333 |
TC-N 1752 |
TC-N 1752 is a potent and orally active inhibitor of Nav1.7, with IC50s of 0.17 μM, 0.3 μM, 0.4 μM, 1.1 μM and 2.2 μM at hNav1.7, hNav1.3, hNav1.4, hNaV1.5 and rNav1.8, respectively. TC-N 1752 also inhibits tetrodotoxin-sensitive sodium channels. TC-N 1752 shows analgesic efficacy in the Formalin model of pain. |
|
| DC47375 |
Guangxitoxin 1E |
Guangxitoxin 1E is a potent and selective blocker of KV2.1 and KV2.2 channels. Guangxitoxin 1E inhibits KV2 with an IC50 of 1-3 nM. KV2 channels underlie delayed-rectifier potassium currents in various neurons. |
|
| DC47376 |
Rimtuzalcap
Featured
|
Rimtuzalcap (CAD-1883) is a first-in-class selective positive allosteric modulator of small-conductance calcium-activated potassium channels (SK channels). Rimtuzalcap can be used for the research of movement disorders including essential tremor (ET) and spinocerebellar ataxia (SCA). |
|
| DC47392 |
WS-898 |
WS-898 is a highly effective ABCB1 inhibitor capable of reversing paclitaxel (PTX) resistance in drug-resistant SW620/Ad300, KB-C2, and HEK293/ABCB1 cells (IC50 = 5.0, 3.67, and 3.68 nM, respectively). |
|
| DC47412 |
P2X receptor-1 |
P2X receptor-1 is a potential inhibitor of P2X receptor for the treatment of pain and inflammation. |
|
| DC47413 |
Eliapixant |
Eliapixant (BAY1817080) is a highly potent and selective P2X3 receptor antagonist with a mean IC50 of 8 nM. |
|
| DC47554 |
Anabaseine |
Anabaseine, an alkaloid, stimulates a wide variety of animal nicotinic acetylcholine receptors (AChRs), especially the neuromuscular receptors and α7 AChRs. |
|
| DC47555 |
CP-601932 |
CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (EC50=~ 3 μM). CP-601932 has the same high-binding affinity at α3β4 (Ki=21 nM) as at α4β2 nAChRs (Ki=21 nM) and an order of magnitude lower affinity for α6 and α7 nAChR subtypes. CP-601932 selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure. CP-601932 readily penetrates the CNS. |
|
| DC47556 |
nAChR agonist 2 |
nAChR agonist 2 (compound 8) is a selective alpha4beta2 (α4β2) nAChR agonist (Kd=26 nM). |
|
| DC47562 |
VB124
Featured
|
VB-124 is a potent and selective MCT4 inhibitor. VB124 might redirect glycolytic carbon flux into mitochondrial pyruvate oxidation. VB 124 bolcks lactate import (IC50=8.6nM), and export (IC50=19nM) in MDA-MB-231 cells that are engineers to express MCT4 as the only major plasma membrane lactate transporter. |
|
| DC47600 |
NMDA receptor antagonist-3 |
NMDA receptor antagonist-3, a NMDA receptor antagonist, stands out with a remarkable percentage of recovery (40.0%, at 100 μM) and safe toxicological profile in SH-SY5Y and human adipose mesenchymal stem cells. |
|
| DC47638 |
CGP35348 |
CGP 35348 is a selective, brain penetrant, centrally active GABAB receptor antagonist with an EC50 of 34 μM. CGP 35348 shows affinity for the GABAB receptor only. CGP 35348 has a potential to improve neuromuscular coordination and spatial learning in albino mouse following neonatal brain damage. |
|
| DC47639 |
3-Aminopropylphosphinic acid |
3-Aminopropylphosphinic acid (3-APPA), a phosphonic analog of GABA, is a GABAB receptor agonist. |
|
| DC47702 |
Posenacaftor |
Posenacaftor (PTI-801) is a cystic fibrosis transmembrane regulator (CFTR) protein modulator that corrects the folding and trafficking of CFTR protein. Posenacaftor is used for the research of cystic fibrosis (CF). |
|
| DC47716 |
(-)-Denudatin B |
(-)-Denudatin B is an antiplatelet agent. (-)-Denudatin B relaxed vascular smooth muscle by inhibiting the Ca2+ influx through voltage-gated and receptor-operated Ca2+ channels. And (-)-Denudatin B has nonspecific antiplatelet action |
|
| DC47771 |
PNU-282987 |
PNU-282987 is a novel selective agonist of the alpha7 nAChR with Ki of 26 nM for rat alpha7 nAChR. PNU-282987 shows no activity at all tested monoamine, muscarine, glutamate, and GABA receptors, except 5-HT3 receptors with Ki of 930 nM. |
|
| DC47864 |
γ-Acetylenic GABA |
γ-Acetylenic GABA (4-Aminohex-5-ynoic acid) is an irreversible inhibitor of GABA-transaminase. γ-Acetylenic GABA can increase the concentration of GABA in rat brain. |
|
| DC47876 |
TRPM8 antagonist 3 |
TRPM8 antagonist 3 is a novel TRPM8 blocker with an IC50 value of 11 nM. |
|
| DC47920 |
PHA 568487 free base |
PHA 568487 free base is a selective alpha 7 nicotinic acetylcholine receptor (α-7 nAchR) agonist. PHA 568487 free base reduces neuroinflammation. |
|
| DC47921 |
PHA 568487 |
PHA 568487 a selective agonist of alpha-7 nicotinic acetylcholine receptor (α-7 nAchR).PHA 568487 reduces neuroinflammation and oxidative stress. PHA-568487 has rapid brain penetration. |
|
| DC47930 |
OSK-1 |
OSK-1 is a potent Kv channel blocker with IC50s of of 0.6 nM, 5.4 nM, 0.014 nM for Kv1.1, Kv1.2 and Kv1.3, respectively. OSK1 is a moderate blocker of Ca2+-activated KCa3.1 channel with an IC50 of 225 nM. OSK-1 belongs to α-KTx3 toxins and is used as a immunosuppressive drug. |
|
| DC47935 |
NJH-2-057 |
NJH-2-057 is an EN523 OTUB1 recruiter linked to lumacaftor, a drug used to treat cystic fibrosis that binds ΔF508-CFTR. |
|
| DC47936 |
Nipecotic acid |
Nipecotic acid ((±)-β-Homoproline) is a potent inhibitor of neuronal and glial-aminobutyric acid (GABA) uptake in vitro. Nipecotic acid can also directly activate GABAA-like chloride channels, with an EC50 of approximately 300 μM. |
|
| DC47937 |
Nemadipine-A |
Nemadipine-A is a specific inhibitor of the EGL-19 L-type Ca2+ channel. Nemadipine-A, a cell-permeable L-type calcium channel inhibitor, sensitizes TRAIL-resistant cancer cells to this ligand. |
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