Propamocarb-d7 is the deuterium labeled Propamocarb[1]. Propamocarb is a systemic fungicide. Propamocarb is widely used to protect cucumbers, tomatoes and other plants from pathogens[2].
SQ 28853 is an inhibitor of ACE with diuretic properties.
Palvanil is a capsaicin analogue, shows strong desensitizing capability against the TRPV1 receptor. Palvanil shows anti-nociceptive and anti-inflammation effects[1][2].
Fmoc-D-Glu-ODmab is a glutamic acid derivative[1].
(Ser(Ac)3)-Ghrelin (mouse, rat) is a biologically active peptide.
Edoxaban(DU-176) is an oral factor Xa (FXa) inhibitor in clinical development for stroke preventionIC50 Value:Target: factor XaEdoxaban is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention in patients with atrial fibrillation, an elderly population that frequently receives aspirin (ASA) and/or nonsteroidal anti-inflammatory drugs for concurrent illnesses[1].in vitro: Edoxaban PK was not affected by concomitant low-dose ASA or naproxen, but high-dose ASA increased systemic exposure of edoxaban by approximately 30%. The effects of edoxaban on prothrombin time, activated partial thromboplastin time, international normalized ratio, anti-FXa, and intrinsic FXa activity were not influenced by administration with ASA or naproxen. Inhibition of platelet aggregation by high-dose ASA, low-dose ASA, or naproxen was not affected by edoxaban[1].in vivo: Forty-eight subjects, aged 18 to 45 years, received either edoxaban 60 mg once daily × 7 days (n = 24) or digoxin 0.25 mg twice daily × 2 days and once daily × 5 days (n = 24) and then concomitantly for 7 days. Serial blood and urine samples were collected for digoxin and edoxaban concentrations on days 7 and 14. Serial coagulation assays were measured for edoxaban on days 7 and 14. Edoxaban PK parameters demonstrated mild increases in area under the curve and peak concentrations of 9.5% and 15.6%, respectively[2],Clinical trial: Pharmacokinetics, biotransformation, and mass balance of edoxaban, a selective, direct factor Xa inhibitor, in humans was reported[3].
Citalopram hydrobromide is an antidepressant drug of the selective serotonin reuptake inhibitor (SSRI) class. It has US FDA approval to treat major depression.
Procion Blue HB (Reactive Blue 2) is a purinergic antagonist.
Penconazole is a typical triazole fungicide, and mainly applied on apples, grapes, and vegetables to control powdery mildew. Penconazole inhibits sterol biosynthesis in fungi. Penconazole decrease AChE activity in the cerebrum and cerebellum of rats[1][2].
(-)-Blebbistatin is an S enantiomer of blebbistatin. Blebbistatin is a potent and selective myosin II inhibitor with IC50s ranging from 0.5 to 5 μM.
Mycalolide-B is a specific inhibitor of actomyosin ATPase isolated from marine sponge. Mycalolide-B inhibits ATP-induced contraction and Mg2+-ATPase activity in the absence of Ca2+[1].
Gemcitabine monophosphate (Gemcitabine 5′-phosphate) is one of the active intermediates of Gemcitabine (HY-17026). Gemcitabine monophosphate shows synergistic anti-cancer effects[1][2].
(Rac)-Moxifloxacin ((Rac)-BAY 12-8039 free base) is the isoform of Moxifloxacin Hydrochloride (HY-66011), which is an oral 8-methoxyquinolone antimicrobial for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia[1][2].
GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively.
Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 1.94 nM.Target: ACEEnalaprilat has high affinity for human endothelial ACE with IC50 of 1.94 nM in vitro binding assay by displacing a saturating concentration of [125I]351A, a radiolabeled lisinopril analogue from ACE binding sites, and shows bradykinin/angiotensin I selectivity ratio of 1.00 calculated from double displacement experiments [1]. Enalaprilat attenuates the IGF-I induced neonatal rat cardiac fibroblast growth (30% reduction) in a concentration-dependent fashion, with IC50 of 90 mM [2].Administration of Enalaprilat induces a significant reduction of MAP at 70 minutes compared with the placebo group during haemorrhagic shock in rats, and results in a 50% reduction of CO, a general tendency of EB extravasation which is significant in the kidney and lungs, and a significant increase in ileal EB extravasation (53%) [3].
C12-NBD Sphinganine is a fluorescent ceramidase substrate. C12-NBD Sphinganine can be used for the measurement of alkaline and neutral ceramidase activity from a variety of sources[1][2][3].
SSR69071 is a potent, orally active and selective inhibitor of neutrophil elastase. SSR69071 reduces myocardial infarct size following ischemia-reperfusion injury[1]. SSR69071 displays a higher affinity for human elastase (Ki=0.0168 nM) than for rat (Ki=3 nM), mouse (Ki=1.8 nM), and rabbit (Ki= 58 nM) elastases[2].
NFAT Inhibitor (VIVIT peptide) is a selective inhibitor of calcineurin-mediated dephosphorylation of nuclear factor of activated T cells (NFAT). Sequence: Met-Ala-Gly-Pro-His-Pro-Val-Ile-Val-Ile-Thr-Gly-Pro-His-Glu-Glu;MAGPHPVIVITGPHEE.
D1N8 is a potent SARS-CoV-2 3CLpro inhibitor with an IC50 and CC50 values of 0.44 μM and >20 μM, respectively. D1N8 has the potential for the research of anti-SARS-CoV-2 agents targeting 3CLpro[1].
MUN57694 is 26S proteasome inhibitor. MUN57694 was reported in WO 2006128196. This product has not formal name. For the convenience of scientific communication, we named it by combining its Inchi key (3 letters from the first letter of each section) with the last 5 digits of its CAS number or its molecule weight if its CAS number is not available
Felbamate-d5 is the deuterium labeled Felbamate[1]. Felbamate (W-554) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA)[2][3].
CC-90002 is a humanized anti-CD47 monoclonal antibody (mAb). CC-90002 has a high affinity for binding to CD47 with a subnanomolar Kd value. CC-90002 can be used for the research of hematologic malignancies and solid tumors[1][2].
SARS-CoV-2 Mpro-IN-6 is a covalent, irreversible and selective SARS-CoV-2 Mpro inhibitor with an IC50 of 0.18 μM. SARS-CoV-2 Mpro-IN-6 does not inhibit human cathepsins B, F, K, and L, and caspase 3[1].
Z-D-Ser(TBu)-OH is a serine derivative[1].
Influenza virus-IN-5 (Compound 5f) is an inhibitor of influenza virus hemagglutinin (HA) with an EC50 of 1 nM against influenza A/H3N2 virus[1].
A potent and selective inhibitor of FAK phosphorylation with biochemical IC50 of 1.2 pM (pFAK Y397), cellular IC50 of 1 nM; displays 8-fold selectivity over PYK2, 26-fold selectivity over RSK1/2 , and >1000-fold selectivity over SRC, AURKA, AURKB, INSR, and KDR; suppresses pFAK Y397 and pFAK Y861 in tumors and liver, shows tumor growth inhibition in TOV21G xenografts in mice.
Benzyl D-serinate hydrochloride is a serine derivative[1].
Fluphenazine decanoate is a long-acting phenothiazine neuroleptic that used to treat schizophrenia. Fluphenazine decanoate is also a high and continuous dopamine D2 receptor blocker[1][2][3].
Picrotoxin is a noncompetitive antagonist of GABAA receptor.
Fmoc-HoPhe-OH is a phenylalanine derivative[1].