Catalog No.
Product Name
Application
Product Information
Product Citation
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P-gp inhibitor
P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance. - Atagabalin is related to gabapentin, which similarly binds to the α2δ calcium channels (1 and 2).
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Serotonin transporter inhibitor
Imipramine Hydrochloride is a tricyclic antidepressant. Inhibits the serotonin and norepinephrine transporters but has little effect on the dopamine transporter. -
SGLT2 Inhibitor
Luseogliflozin is an orally active second-generation sodium-glucose co-transporter 2 (SGLT2) inhibitor developed by Taisho Pharmaceutical for the treatment of patients with type 2 diabetes mellitus (T2DM). -
P-gp inhibitor
Laniquidar is a third-generation P-gp inhibitor, which has been used in clinic trials for modulating multidrug resistance transporters. -
P-gp modulator
Biricodar dicitrate (VX-710 dicitrate) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells. -
SGLT2 inhibitor
Ipragliflozin is a highly potent and selective SGLT2 inhibitor with IC50 of 2.8 nM; little and NO potency for SGLT1/3/4/5/6. -
voltage-gated sodium channel Nav1.7 inhibitor
Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration. -
myosin II inhibitor
Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light. -
AMPA desensitization inhibitor
Cyclothiazide is a benzothiadiazide that acts as a potentiator of AMPA receptors, positively modulating its response to glutamic acid (EC50 = 3.8 M). -
CFTR inhibitor
CFTR inhibitor II, also known as GlyH-101, is a glycine hydrazide that selectively and reversibly blocks the CFTR channel (Ki = 4.3 uM).- Dao-Lai Zhang, .et al. , eLife, 2018, 7: e33432 PMID: 29393851
- CRAC intermediate 2 is a intermediate compound for CRAC inhibitor synthesis, extracted from patent WO 2013059666A1.
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Sodium channel Blocker
QX 314 chloride is a membrane impermeable quaternary derivative of lidocaine, a voltage-activated Na+ channel blocker -
NaV1.3 and NaV1.1 channels inhibitor
ICA-121431 is a potent and selective inhibitor of human NaV1.3 and NaV1.1 channels (IC50 values are 13 and 23 nM respectively). -
AMPA receptor modulator
Farampator has been investigated for its effect on AMPA receptors and researched for potential use in the treatment of schizophrenia and Alzheimer's Disease. It was found to improve short-term memory, but impaired episodic memory. -
VDAC inhibitor
Erastin is a cell-permeable piperazinyl-quinazolinone compound that exhibits oncogene-selective lethality in cells with H-Ras mutations.- Erva Ozkan, .et al. , Life Sci, 2023, Jan 1;312:121222 PMID: 36442526
- Yuki Shibata, .et al. , Biochem Biophys Rep, 2021, Feb 24;26 PMID: 33681481
- Shibata Y, .et al. , PLoS One, 2019, Dec 4;14(12):e0225931 PMID: 31800616
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hASBT inhibitor
GSK2330672 is a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor. -
Sodium channel blocker
Encainide HCl is a sodium channel blocker and class Ic antiarrhythmic. Encainide is a non-chiral antiarrhythmic and benzanilide derivative. -
Sodium channel blocker
Disopyramide is an antiarrhythmic (class IA) and a sodium channel blocker.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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Ca2+ release inhibitor
Dantrolene sodium is a muscle relaxant that acts by abolishing excitation-contraction coupling in muscle cells, probably by action on the ryanodine receptor. -
sodium channel protein inhibitor
Oxcarbazepine is a sodium channel protein inhibitor. -
KCa2.1 channels activator
GW 542573X is an activator of small-conductance Ca2+-activated K+ channels (KCa2). -
SGLT2 inhibitor
Remogliflozin inhibits the sodium-glucose transport (SGLT2) proteins, which are responsible for glucose reabsorption in the kidney. -
Selective calcium chelator
BAPTA tetrapotassium is a selective calcium chelator with greater affinity for Ca2+ than Mg2+. -
TrpA1 channel agonist
PF-4840154 is a non-electrophilic reference agonist of the TrpA1 channel. The TRPA1 channel is considered an attractive pain target based on the fact that TRPA1 knockout mice showed near complete attenuation of pain behaviors in some pre-clinical development models. -
ATP synthase inhibitor
Oligomycin is a macrolide that acts as a specific inhibitor of the mitochondrial ATP-synthase and blocks oxidative phosphorylation. -
SERCA inhibitor
Cyclopiazonic acid is an inhibitor of SERCA (endoplasmic reticulum Ca2+-ATPase) which induces the release of intracellular stored Ca2+, without increasing IP3 levels. -
AMPA Receptor Blocker
IEM 1754 Dihydrobromide is a voltage-dependent open-channel blocker of AMPA receptors. -
NHE3 inhibitor
Tenapanor acts as an inhibitor of the sodium-proton exchanger NHE3. This antiporter protein is found in the kidney and intestines, and normally acts to regulate the levels of sodium absorbed and secreted by the body.- Kuniko Hunter, .et al. , Tissue Eng Part A, 2022, Nov 18 PMID: 36274231
- Xingjie Tan, .et al. , Authorea, 2022, May 25
- Kunyan Zhou, .et al. , Am J Physiol Cell Physiol, 2021, Sep 1;321(3):C471-C488 PMID: 34288721
- Qinghai Tan, .et al. , Br J Pharmacol, 2021, Mar;178(5):1018-1036 PMID: 33179259
- Y Liu, .et al. , Biochem Pharmacol, 2020, May 16;178:114040 PMID: 32422138
- Yu Y, .et al. , Cell Physiol Biochem, 2019, 52(5):1017-1038 PMID: 30977986
- Thammayon N, .et al. , Amino Acids, 2017, Apr;49(4):725-734 PMID: 27981415
- Charoenphandhu N, .et al. , Mol Cell Biochem, 2017, Mar;427(1-2):201-208 PMID: 27995414
- Jantarajit W, .et al. , Am J Physiol Cell Physiol, 2017, Jul 1;313(1):C118-C129 PMID: 28490422
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Selective calcium chelator
BAPTA/AM, an intracellular calcium chelator, induces delayed necrosis by lipoxygenase-mediated free radicals in mouse cortical cultures.- Jiunn-Chang Lin, .et al. , Toxicol Appl Pharmacol, 2023, Jul 15;471:116568 PMID: 37245555
- Liying Wu, .et al. , Phytother Res, 2022, Feb;36(2):938-950 PMID: 35076979
- Shichen Xu, .et al. , Cell Signal, 2020, Aug 6;75:109733 PMID: 32771398
- Miho Akimoto, .et al. , Cell Death Dis, 2018, Aug; 9(8): 804 PMID: 30038429
- Zhang L, .et al. , Medicine (Baltimore), 2018, Jun;97(24):e11095 PMID: 29901626
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TrxR1/CRM1 inhibitor
Piperlongumine selectively kills cancer cells regardless of p53 status without harming normal cells. It binds to and inihbits proteins known to regulate oxidative stress, in particular, Glutathione S-transferase pi 1 (GSTP1). -
TRPA1 channel blocker
TCS 5861528 is a TRPA1 channel blocker and an antagonizer of AITC- and 4-HNE-evoked calcium influx. -
MCT1 inhibitor
AZD3965 is a selective inhibitor of monocarboxylate transporter 1 (MCT1) with a binding affinity of 1.6 nM, is 6 fold selective over MCT2 and does not inhibit MCT4 at 10 μM.- Lu Gao, .et al. , Int J Biol Sci, 2022, Jan 1;18(2):599-616 PMID: 35002512
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TRPV4 blocker
GSK2193874 was identified as a selective, orally active TRPV4 blocker that inhibits Ca(2+) influx through recombinant TRPV4 channels and native endothelial TRPV4 currents. -
Sodium channel blocker/DNMT inhibitor
Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor. -
sodium-potassium pump inhibitor
Digoxin is a sodium-potassium pump inhibitor.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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proton pump inhibitor
Tenatoprazole is a prodrug of the proton pump inhibitor (PPI) class, which inhibits proton transport with IC50 of 3.2 uM.
