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Membrane Transporter/Ion Channel

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Cat. No. Product Name Field of Application Chemical Structure
DC80295 BBO-11818
BBO-11818 is an orally active, highly selective (relative to NRAS and HRAS), non-covalent pan-KRAS inhibitor (IC50=28-120 nM). BBO-11818 specifically binds to the Switch-II/Helix 3 pocket, disrupts the KRAS:RAF1 interaction by inducing conformational changes, and blocks the MAPK signaling pathway. BBO-11818 exhibits significant anti-tumor activity, which not only inhibits cell proliferation and induces apoptosis, but also drives tumor regression in xenograft models. BBO-11818 produces synergistic effects when combined with Cetuximab, anti-PD-1 antibody or PI3Kα inhibitor. BBO-11818 is used in the research of KRAS mutation-related malignancies such as pancreatic cancer, non-small cell lung cancer and colorectal cancer.
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DC80264 Asoxime dimesylate
Asoxime dimesylate (HI-6 dimesylate) is an orally active thiosemicarbazone-based antidote. Asoxime dimesylate is a reversible inhibitor of AChE, and its core mechanism of action is to re-activate AChE inhibited by nerve toxins, thereby restoring the cholinergic nerve function. Asoxime dimesylate significantly restores the function of poisoned muscles without reactivating AChE. Asoxime dimesylate is an antagonist of acetylcholine receptors (AChRs), including nicotinic receptor and α7 nAChR. Asoxime dimesylate can serve as an effective immunomodulator, improving the immune effect of the nervous system.
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DC80251 AR ligand-48
AR ligand-48 is an AR (Androgen Receptor) inhibitor and a ligand for the target protein for PROTAC (AR). AR ligand-48 can be used to synthesize PROTAC AR Degrader-12.
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DC80227 Antiparasitic agent-30
Antiparasitic agent-30 is a potent adenosine kinase TbrAK modulator and antitrypanosomal agent. Antiparasitic agent-30 exhibits significant inhibitory activity against Trypanosoma brucei rhodesiense, while enhancing the activity of recombinant TbrAK(EC50=38 nM, Ka=75 nM-497 nM). Antiparasitic agent-30 exerts its pharmacological effects by eliminating intrinsic substrate inhibition and hyperactivating TbrAK in Trypanosoma brucei rhodesiense. Antiparasitic agent-30 serves as a valuable tool molecule for studying acute African human trypanosomiasis (sleeping sickness).
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DC80218 Antileishmanial agent-36
Antileishmanial agent-36 (compound 4f) is an indole-dihydropyrimidinone derivative with anti-leishmanial activity. Antileishmanial agent-36 induces reactive oxygen species (ROS)-mediated mitochondrial dysfunction and apoptosis. Antileishmanial agent-36 exhibits potent activity against L. donovani (IC50 =4.54 μM) with low cytotoxicity against J774.1 macrophage. Antileishmanial agent-36 clears the parasite burden in a visceral leishmaniasis (VL) model. Antileishmanial agent-36 can be used for VL research.
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DC80200 Androgen receptor degrader-6
Androgen receptor degrader-6 is a blood-brain barrier-permeable AR degrader. Androgen receptor degrader-6 inhibits the chaperone activity of HSP27 and disrupts the HSP27-AR complex. Androgen receptor degrader-6 promotes the degradation of wild-type and mutant AR, reduces AR protein levels, and inhibits the growth of glioblastoma cells. Androgen receptor degrader-6 can be used in glioblastoma research.
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DC80136 A-837093 sodium
A-837093 sodium is a potent and orally active inhibitor of the hepatitis C virus (HCV) nonstructural protein 5B (NS5B) polymerase. A-837093 sodium shows potencies against polymerases derived from both HCV genotypes 1a (IC50 = 1.25 nM) and 1b (IC50 = 0.33 nM). A-837093 sodium exhibits antiviral efficacy in HCV-infected chimpanzees. A-837093 sodium can be used for HCV infection research.
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DC80117 6-Iodonordihydrocapsaicin
6-Iodonordihydrocapsaicin is a TRPV1 antagonist. 6-Iodonordihydrocapsaicin functionally blocks TRPV1-mediated responses, including capsaicin-induced ion currents in dorsal root ganglion neurons and distension-induced firing of jejunal spinal afferent fibers in mice. 6-Iodonordihydrocapsaicin can be used in the research of visceral pain and anxiety disorders.
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DC80102 5-Formyl-2-hydroxy-2,4-heptadienedioic acid
5-Formyl-2-hydroxy-2,4-heptadienedioic acid (compound II) is a product of metu-cleavage of 3,4-dihydroxyphenylacetate.
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DC80075 41-O-Demethylrapamycin
41-O-Demethylrapamycin is a metabolite of Rapamycin produced by Bacillus megaterium.
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DC80055 3-Amino-5-hydroxybenzoic acid-13C
3-Amino-5-hydroxybenzoic acid-13C is the 13C-labeled 3-Amino-5-hydroxybenzoic acid. 3-Amino-5-hydroxybenzoic acid is a biosynthetic precursor of the mC7N unit of ansamycin antibiotics, including ansatrienin A and geldanamycin, as well as the antitumor antibiotic mitomycin C. 3-Amino-5-hydroxybenzoic acid may be an early intermediate in the shikimic acid pathway from glucose.
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DC79982 11β-HSD1-IN-25
11β-HSD1-IN-25 is a selective and orally active 11β-HSD1 inhibitor. 11β-HSD1-IN-25 effectively reduces glucocorticoid levels in vitro and serum, and diminishes lipid accumulation in both vitro and vivo. 11β-HSD1-IN-25 modulates lipid metabolism through dual mechanisms: inhibition of 11β-HSD1 and activation of the AMP-activated protein kinase (AMPK) signaling pathway. 11β-HSD1-IN-25 can be used for obesity and related metabolic disorders research.
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DC79976 10(Z)-Pentadecenoic acid methyl ester
10(Z)-Pentadecenoic acid methyl ester is an unsaturated fatty acid methyl ester (FAME)。
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DC80052 3-(Pyridin-2-yl)-1,2,4-triazole
3-(Pyridin-2-yl)-1,2,4-triazole is a metal-organic framework (MOF).
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DC79940 1,1-Dimethoxyhexadecane
1,1-Dimethoxyhexadecane is an ether lipid. Ether lipids are mainly found in cell membranes.
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DC79932 (S,R,S)-AHPC-Me-NHBoc
(S,R,S)-AHPC-Me-NHBoc is an E3 ubiquitin ligase VHL ligand used to recruit the VHL protein. (S,R,S)-AHPC-Me-NHBoc can be linked to a target protein ligand via a linker to form a PROTAC.
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DC46392 N-Arachidonylglycine Featured
N-Arachidonylglycine (NA-Gly), a carboxylic analog of the endocannabinoid anandamide (AEA), is a GPR18 agonist (EC50 = 44.5 nM). Unlike AEA, N-Arachidonylglycine has no activity at either CB1 or CB2 receptors. N-Arachidonylglycine inhibits GLYT2 (IC50 = 5.1 μM). N-Arachidonylglycine also is an effective activator of endometrial cell migration.
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DC71153 Chlorisondamine diiodide Featured
Chlorisondamine (diiodide) is a potent nicotinic acetylcholine receptor (nAChR) antagonist and a ganglion blocker. Chlorisondamine antagonizes some of nicotine's central actions in a potent, long-lasting and pharmacologically selective way.
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DC73603 OV350 Featured
OV350 (OV-350) is a potent, selective and direct K+-Cl- cotransporter KCC2 agonist with EC50 of 261.4 nM, with no effect on KCC2 plasma membrane accumulation and phosphorylation.
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DC73682 DS43260857 Featured
DS43260857 is a potent, selective NaV1.7 inhibitor with IC50 of 15 nM (hNaV1.7), shows 440-fold and 930-fold selectivity over hNaV1.1 and hNaV1.5, respectively.
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DC70477 EC18 HCN inhibitor Featured
EC18 HCN inhibitor is a HCN channel inhibitor. EC18 acts as a potent HCN4 inhibitor in a human iPSC-derived sinus node model with proven HCN4 expression. EC18 is an attractive pharmacological tool, enabling HCN channel-modulation studies with some specificity for HCN4 (EC50 [HCN4] = 3.98 ± 1.16 µM) over HCN1 (EC50 = 21.00 ± 3.98 µM) and HCN2 (EC50 = 19.35 ± 4.48 µM). EC18 abolishes HCN4 triggered pace making in a human iPSC (hiPSC) pacemaker model.
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DC46699 9-Phenanthrol Featured
9-Phenanthrol (9-Hydroxyphenanthrene, Phenanthren-9-o, 9-Phenanthrenol) is a selective TRPM4 inhibitor with an IC50 in the range of 0.02 μM, without effects on TRPM5.
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DC70804 SSCI-1 Featured
SSCI-1 is a highly potent, selective NaV1.7 inhibitor with IC50 of 27 and 82 nM on human and rhesus Nav1.7 channels, respectively.SSCI-1 showed robust selectivity over other human and rhesus Nav channel paralogs, with the exception of Nav1.2 channels (IC50 252 nM for hNaV1.2), shows no other channels and receptors in 114 enzymatic, radioligand binding, and cellular assays.SSCI-1 also exhibits high potency in manual patch clamp experiments (IC50=66/295 nM for huma/rhesus Nav1.7 channels).SSCI-1 does not affect myelinated nerve excitability as measured by TT, SSCI-1 inhibits odorant-induced olfaction in the olfactory bulb of rhesus monkeys, measured by fMRI.SSCI-1 inhibits withdrawal responses to noxious heat in rhesus monkeys.
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DC10874 GlyT2-IN-1(YODA 1) Featured
Yoda 1 is a potent and selective Piezo1 agonist. Yoda 1 activates purified Piezo1 channels. Yoda 1 potently inhibits macropinocytosis induced by epidermal growth factor (EGF). Yoda 1 enhances Ca2+ influx followed by activation of the calcium-activated potassium channel KCa3.1 and inhibition of Rac1 activation.
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DC70312 CLC-2-IN AK42 Featured
CLC-2-IN-AK42 (CLC-2 inhibitor AK42, AK42) is a potent, specific small-molecule inhibitor of voltage-gated chloride channel CLC-2 with IC50 of 17 nM (human CLC-2).AK42 displays unprecedented selectivity (>1,000-fold) over CLC-1, the closest CLC-2 homolog, and no off-target engagement a diverse panel of 61 CNS receptors, channels, and transporters expressed in brain tissue.AK-42 binds to an extracellular vestibule above the channel pore. AK-42 is almost three orders-of-magnitude more potent than MCFA, demonstrates high potency (IC50=14 nM for rat CLC-2) in manual patch-clamp experiments on CHO cells transiently transfected with rat CLC-2.AK-42 inhibits hyperpolarization-activated current in hippocampal cells, attenuates steady-state currents and eliminated relaxation currents in recorded neurons.AK-42 is a powerful tool for investigating CLC-2 neurophysiology.
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DC73692 GNE551 Featured
GNE551 is a potent, selective, non-covalent agonist of TRPA1 ion channel with EC50 of 254 nM in Ca2+ influx assays.
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DC70647 Neurounina-1 Featured
Neurounina-1 is a small molecule Na+/Ca2+ exchanger (NCX) activator, stimulates NCX1 and NCX2 activities with EC50 of 1.1-2.7 nM, does not affect NCX3 activity.Neurounina-1 (10 nM) reduced cell death of primary cortical neurons exposed to oxygen-glucose deprivation followed by reoxygenation, also reduced γ-aminobutyric acid (GABA) release, enhanced GABA(A) currents, and inhibited both glutamate release and N-methyl-d-aspartate receptors in vitro.Neurounina-1 effectively protects against stroke damage in vivo.
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DC46528 MCT4-IN-1 Featured
MCT4-IN-1 is an orally active and selective monocarboxylate transporter 4 (MCT4/SLC16A3) inhibitor with an IC50 of 77 nM and a Ki of 11 nM. MCT4-IN-1 targets to the cytosolic domain of MCT4. MCT4-IN-1 results in lactate efflux inhibition and reduction of cellular viability in MCT4 high expressing cells. MCT4-IN-1 has the potential for MCT4 transporter inhibition research.
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DC70430 GDC-0334 Featured
GDC-0334 (GDC0334) is a highly potent, selective, orally bioavailable TRPA1 antagonist with IC50 of 1.7 nM in cell-based assays.GDC-0334 demonstrated potent TRPA1 inhibition in several species, including human (IC50=1.7 nM), cynomolgus (IC50=3.6 nM), mouse (IC50=2.7 nM), guinea pig (IC50=11.1 nM), and dog (IC50=102 nM).GDC-0334 displays good selectivity against human TRPV1, TRPM8, and TRPC6 (all IC50s>10 uM).GDC-0334 also inhibits calcium flux in human primary cells, HASMCs and HLFs, treated with the TRPA1 agonist AITC.GDC-0334 suppresses AITC-induced edema in vivo in rat (1-10 mg/kg), reduces OVA-induced asthma model in rats and guinea pigs and guinea pig model of cough.GDC-0334 is a potent inhibitor of AITC-induced dermal blood flow (DBF) in vivo in rats and guinea pigs, reduces AITC-induced perfusion and nocifensive behavior in rats and itch and pain scores in humans.
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DC72214 Pyrantel Featured
Pyrantel is an orally active anthelmintic and an agonist of the nicotinic acetylcholine receptor (nAChR). Pyrantel can cause spasmodic muscle paralysis in parasites. Pyrantel can be used in the study of parasitic infections such as ascariasis, hookworm infections, intestinal worms (pinworm infections), trichinosis and trichinosis.
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