| DC44163 |
L-Palmitoylcarnitine chloride |
L-Palmitoylcarnitine chloride, a long-chain acylcarnitine and a fatty acid metabolite, accumulates in the sarcolemma and deranges the membrane lipid environment during ischaemia. L-Palmitoylcarnitine chloride inhibits KATP channel activity, without affecting the single channel conductance, through interaction with Kir6.2. |
|
| DC44164 |
BI-9627 hydrochloride |
BI-9627 hydrochloride is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride shows low DDI (drug-drug interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury. |
|
| DC44165 |
WEHI-9625 |
WEHI-9625 is a tricyclic sulfone, first-in-class inhibitor of apoptosis with an EC50 of 69 nM. WEHI-9625 binds to VDAC2 and promotes its ability to inhibit apoptosis driven by mouse BAK. WEHI-9625 is completely inactive against both human BAK and the closely related apoptosis effector BAX. |
|
| DC44561 |
CGP 78608 hydrochloride |
CGP 78608 hydrochloride is a highly potent and selective antagonist at the glycine-binding site of the NMDA receptor, with an IC50 of 6 nM. CGP 78608 acts as a potentiator of GluN1/GluN3A-mediated glycine currents, with an estimated EC50 in the low nM ran |
|
| DC44562 |
8-Bromo-ATP |
8-Bromo-ATP (8-Bromoadenosine 5'-triphosphate), an ATP analogue, is a purinergic P2X receptor agonist. 8-Bromo-ATP shows cytotoxic to multiple myeloma cells with an IC50 of 23.1 μM. |
|
| DC44563 |
8-Azido-ATP |
8-Azido-ATP, a photoreactable nucleotide analog, is useful for the identification of proteins, such as DNA-dependent RNA polymerase. |
|
| DC44564 |
Methionine |
Methionine (MRX-1024, D-Methionine) is an activitor of GABAA receptor that modulates neuronal activity. |
|
| DC44565 |
Etomidate hydrochloride |
Etomidate (Amidate, R 16659) hydrochloride is a general anesthetic that produces its effects by enhancing GABA(A) receptor activity. |
|
| DC44566 |
Quinidine hydrochloride monohydrate |
Quinidine hydrochloride monohydrate is an anti-arrythmic agent and a potent potassium channel inhibitor with IC50 of 19.9 μM. |
|
| DC44567 |
Ertugliflozin L-pyroglutamic acid |
Ertugliflozin (MK-8835, PF-04971729) L-pyroglutamic acid is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2) with IC50 of 0.877 nM for h-SGLT2. Ertugliflozin has the potential for the treatment of typ |
|
| DC44774 |
Propafenone |
Propafenone (SA-79) is an orally active sodium channel blocking agent and a beta-adrenoceptor (β-adrenergic receptor) antagonist. Propafenone offers a broad spectrum of activity in the treatment of cardiac arrhythmias. |
|
| DC44828 |
(Rac)-MEM 1003 |
(Rac)-MEM 1003 is the racemate of MEM 1003. MEM 1003, a dihydropyridine compound, is a potent L-type Ca2+ channel antagonist and has the potential for Alzheimer’s disease research. |
|
| DC44829 |
1,2,4-Trihydroxybenzene |
1,2,4-Trihydroxybenzene (Hydroxyhydroquinone), a by-product of coffee bean roasting, increases intracellular Ca2+ concentration in rat thymic lymphocytes. |
|
| DC44830 |
UK-59811 hydrochloride |
UK-59811 hydrochloride, a Br-dihydropyridine derivative, is a potent bacterial homotetrameric model voltage-gated Ca2+ (CaV) channel CaVAb inhibitor with an IC50 of 194 nM. |
|
| DC44831 |
MCU-i4
Featured
|
MCU-i4 is a negative modulator of the mitochondrial calcium uniporter (MCU) complex that directly binds a specific cleft in MICU1 and decreases mitochondrial Ca2+ influx.,MCU-i4 decreases mitochondrial Ca2+ influx. Docking simulations reveal that MCU-i4 directly binds a specific cleft in MICU1, a key element of the MCU complex that controls channel gating. Accordingly, in MICU1-silenced or deleted cells, the inhibitory effect of MCU-i4 is lost. Moreover, MCU-i4 fails to inhibit mitochondrial Ca2+ uptake in cells expressing a MICU1 mutated in the critical amino acids that forge the predicted binding cleft.[1] |
|
| DC44910 |
GABAA receptor agent 2 TFA |
GABAA receptor agent 2 TFA is a potent and high-affinity GABAA receptor antagonist with an IC50 of 24 nM (human α1β2γ2 GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAA receptors). GABAA receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3). |
|
| DC44911 |
Lesogaberan napadisylate |
Lesogaberan (AZD-3355) napadisylate 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. |
|
| DC44930 |
(S)-(-)-HA 966 |
(S)-(-)-HA 966 ((-)-HA 966), a γ-Hydroxybutyrate-like agent, is weakly active as an NMDA-receptor antagonist. (S)-(-)-HA 966 possesses muscle relaxant action and prevents enhanced mesocorticolimbic dopamine metabolism and behavioral correlates of restraint stress, conditioned fear. |
|
| DC44931 |
N-Methyl-DL-aspartic acid |
N-Methyl-DL-aspartic acid is a glutamate analogue and acts as a potent neuronal excitant. N-Methyl-DL-aspartic acid is a NMDA receptor agonist and can be used for neurological diseases research. |
|
| DC44932 |
UBP-282 |
UBP-282 is a potent, selective and competitive AMPA and kainate receptor antagonist. UBP-282 inhibits the fast component of the dorsal root-evoked ventral root potential (fDR-VRP) with an IC50 value of 10.3 μM. UBP-282 antagonizes kainate-induced depolarisations of dorsal roots with a pA2 value of 4.96. |
|
| DC44933 |
Caroverine hydrochloride
Featured
|
Caroverine hydrochloride is a potent, competitive and reversible antagonist of NMDA and AMPA glutamate receptor. Caroverine hydrochloride is also an antioxidant and calcium-blocking agent that exhibits vasorelaxant action. Caroverine hydrochloride can be used for the research of inner ear tinnitus. |
|
| DC44965 |
FFN200 dihydrochloride |
FFN200 dihydrochloride, a fluorescent substrate of VMAT2, selectively trace monoamine exocytosis in both neuronal cell culture and brain tissue. The fluorescence excitation and emission maxima of FFN200 are determined to be 352 and 451 nm, respectively. |
|
| DC44966 |
AR-C141990 hydrochloride |
AR-C141990 hydrochloride is a potent lactate transporters (monocarboxylate transporters; MCTs) inhibitor with pKi values of 7.6, 6.6 for MCT-1 and MCT-2, respectively. AR-C141990 hydrochloride has immunosuppressive properties and inhibits graft versus host response. |
|
| DC44969 |
Furosemide sodium |
Furosemide (Frusemide) sodium is a potent and orally active inhibitor of Na-K-Cl cotransporter (NKCC). Furosemide sodium is a subtype-selective antagonist of gamma-aminobutyric acid type A (GABAA) receptor.,NKCC [1]()
GABAA receptor [1]() |
|
| DC45198 |
Lei-Dab7 |
Lei-Dab7 is a high affinity, selective KCa2.2 (SK2) channel blocker (Kd=3.8 nM). Lei-Dab7 exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, Kv and Kir2.1. Lei-Dab7 increases theta-burst responses and increases LTP in rat hippocampal slices in vitro. |
|
| DC45273 |
Phrixotoxin 3 |
Phrixotoxin 3 is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current. |
|
| DC45274 |
Mambalgin 1 |
Mambalgin 1 is a selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 binds to closed/inactive channel. Mambalgin 1 is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 increases latency of withdrawal response in mouse tail-flick and paw-flick tests. |
|
| DC45275 |
ProTx II |
ProTx II is a selective blocker of Nav1.7 sodium channels with an IC50 of 0.3 nM, and is at least 100-fold selective for Nav1.7 over other sodium channel subtypes. ProTx-II inhibits sodium channels by decreasing channel conductance and shifting activation to more positive potentials and blocks action potential propagation in nociceptors. |
|
| DC45276 |
PF-04885614 |
PF-04885614 is a potent NaV1.8 inhibitor, extracted from patent US2018328915. PF-04885614 has potential for neurological and neurodevelopmental diseases treatment. |
|
| DC45285 |
IA-Alkyne |
IA-Alkyne (Iodoacetamide-alkyne; N-Hex-5-ynyl-2-iodo-acetamide) is a TRP channel (TRPC) agonist and has the potential for the study of respiratory infection. IA-Alkyne can be used to develop an isotopically tagged probe for quantitative cysteine-reactivity profiling. |
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