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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC28125 Cyclo(his-pro) TFA
Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) TFA could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) TFA can cross the brain-blood-barrier and affect diverse inflammatory and stress responses.
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DC28124 γ-Glu-Phe TFA
γ-Glu-Phe TFA (γ-Glutamylphenylalanine TFA) is synthesized by Bacillus amyloliquefaciens (GBA) and Aspergillus oryzae (GAO). γ-Glu-Phe TFA or the post-enzymatic reaction mixture enhances the umami intensity of commercial soy sauce and model chicken broth.
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DC28123 Otenzepad
Otenzepad (AF-DX 116) is a selective and competitive M2 muscarinic acetylcholine receptor antagonist, with IC50 values of 640 nM and 386 nM for rabbit peripheral lung and rat heart, respectively.
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DC28122 8-M-PDOT
8-M-PDOT (AH-002) is a selective melatonin MT2 receptor agonist. 8-M-PDOT is 5.2-fold selective for MT2 over MT1 receptors. 8-M-PDOT binds human recombinant MT2 and MT2 receptors with pKi values of 8.23 and 8.95 respectively. 8-M-PDOT has anxiolytic-like activity.
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DC28120 QX-314 bromide
QX-314 bromide is a membrane-impermeable permanently charged sodium channel blocker.
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DC28119 (R)-VU 6008667
(R)-VU 6008667, the less active (R)-enantiomer to VU 6008667, is devoid of M5 NAM activity (IC50>10 μM).
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DC28118 ATPA
ATPA is a selective glutamate receptor GluR5 activator with EC50s of 0.66, 9.5, 1.4, 23, 32, 18, and 14 μM for GluR5wt, GluR5(S741M), GluR5(S721T), GluR5(S721T, S741M), GluR5(S741A), GluR5(S741L), and GluR5(S741V), respectively.
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DC28116 Tiotidine
Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors.
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DC28115 Tin-protoporphyrin IX
Tin-protoporphyrin IX (SnPPIX) is a potent Heme oxygenase-1 (HO-1) inhibitor. Tin-protoporphyrin IX (SnPPIX) sensitizes pancreatic ductal adenocarcinoma (PDAC) tumors to chemotherapy in mice model.
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DC28114 2-Iodomelatonin
2-Iodomelatonin is a potent agonist of melatonin receptor 1 (MT1) with a Ki value of 28 pM, it is more 5-fold selective for MT1  over MT2. 2-iodomelatonin can be used to identify, characterize and localize melatonin binding sites in the brain and peripheral tissues.
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DC28112 Propargyl-PEG4-C2-acid
Propargyl-PEG5-acid is a non-cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Propargyl-PEG5-acid can used to synthesize ADC inhibitors of Galectin-3.
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DC28111 PPADS tetrasodium
PPADS tetrasodiuma is a non-selective P2X receptor antagonist. PPADS tetrasodiuma blocks recombinant P2X1, -2, -3, -5 with IC50s ranging from 1 to 2.6 μM. PPADS tetrasodiuma blocks native P2Y2-like (IC50~0.9 mM) and recombinant P2Y4 (IC50~15 mM) receptors. PPADS tetrasodiuma is an inhibitor of the reverse mode of the Na/Ca²⁺exchanger in guinea pig airway smooth muscle.
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DC28108 Flurofamide
Flurofamide is a potent bacterial urease inhibitor with potential clinical utility in the treatment of infection induced urinary stones.
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DC28107 Cinanserin hydrochloride
Cinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity 5-HT2 receptor antagonist with a Ki of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the 5-HT2 than for the 5-HT1 receptor (Ki of 3500 nM). Cinanserin is also an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro.
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DC28106 ML-9 Free Base
ML-9 (Free Base) is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 (Free Base) inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 (Free Base) induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
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DC28105 OGT 2115
OGT 2115 is a potent, cell-permeable and orally active heparanase inhibitor with an IC50 of 0.4 μM. OGT 2115 has anti-angiogenic properties (IC50 of 1 μM). OGT 2115 also inhibits heparan sulfate degradation activity.
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DC28104 F1324 acetate
F1324 acetate is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM. F1324 acetate exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI.
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DC28103 F1324 TFA
F1324 TFA is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM. F1324 TFA exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI.
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DC28101 Dehydroaripiprazole
Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole. Dehydroaripiprazole has with antipsychotic activity equivalent to Aripiprazole.
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DC28100 Didesethyl chloroquine
Didesethyl chloroquine (Bisdesethylchloroquine) is a major metabolite of the antimalarial drug Chloroquine. Didesethyl chloroquine is a potent myocardial depressant.
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DC28099 Didesmethyl cariprazine
Didesmethyl cariprazine is a metabolite of Cariprazine and acts as the predominant circulating active moiety. Didesmethyl cariprazine has a long half-life of 1-3 weeks. Cariprazine is a antipsychotic drug candidate that exhibits high affinity for the D3 and D2 receptors, and moderate affinity for the 5-HT1A receptor.
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DC28098 meta-Fexofenadine
meta-Fexofenadine (meta-MDL-16455) is an impurity of Fexofenadine. Fexofenadine, a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial.
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DC28097 Desmethyl cariprazine
Desmethyl cariprazine is an active metabolite of Cariprazine. Cariprazine, an antipsychotic drug candidate, exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (2.6 nM).
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DC28096 O-Desmethyl apixaban
O-Desmethyl apixaban is a metabolite of Apixaban (BMS-562247-01). Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.
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DC28095 O-Desmethyl apixaban sulfate sodium
O-Desmethyl apixaban sulfate sodium is a major circulating metabolite of Apixaban in humans. O-Desmethyl apixaban sulfate sodium inhibits factor X (FXa) with a Ki of 58 μM.
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DC28094 Desmethylnortriptyline
Desmethylnortriptyline is a metabolite of Nortriptyline. Nortriptyline is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and is used to relieve the symptoms of depression.
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DC28092 Hydroxy ziprasidone
Hydroxy ziprasidone is an impurity of Ziprasidone. Ziprasidone, an antipsychotic agent, is a combined 5-HT (serotonin) and dopamine receptor antagonist.
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DC28091 Keto Ziprasidone
Keto Ziprasidone is an impurity of Ziprasidone. Ziprasidone, an antipsychotic agent, is a combined 5-HT (serotonin) and dopamine receptor antagonist.
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DC28090 (Z)-10-Hydroxy Nortriptyline
(Z)-10-Hydroxy Nortriptyline is a metabolite of Nortriptyline. Nortriptyline is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and is used to relieve the symptoms of depression.
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DC28089 (E)-10-Hydroxy Nortriptyline maleate
(E)-10-Hydroxy Nortriptyline maleate is a metabolite of Nortriptyline. Nortriptyline is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and is used to relieve the symptoms of depression.
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