Ceranib-2 is a potent and nonlipid ceramidase inhibitor that inhibits cellular ceramidase activity with an IC50 of 28 μM in SKOV3 cells. Ceranib-2 induces the accumulation of multiple ceramide species, decreases levels of sphingosine and sphingosine-1-phosphate (S1P), and induces cell apoptosis. Anticancer activity[1][2].
Benalaxyl is a fungicide. Benalaxyl has good control of blue mould (Peronospora tubacina)[1].
Succinyl phosphonate trisodium salt (SP) is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts[1][4].Succinyl phosphonate trisodium salt (SP) is an 2-Oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner[2].Succinyl phosphonate trisodium salt (SP) inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ[3].
Antiviral agent 5 is an intermediate used in antiviral agents targeting 3C and 3CL proteases including SARS-CoV-2 Mpro.
Pancreatic Polypeptide, rat is an agonist of NPY receptor, with high affinity at NPYR4.
Lamivudine 13C,15N2 is a labelled impurity of Lamivudine (BCH-189). Lamivudine is a nucleoside reverse transcriptase inhibitors (NRTIs), and can inhibit HIV reverse transcriptase 1/2 and the reverse transcriptase of hepatitis B virus[1][2].
N-ε-propargyloxycarbonyl-L-lysine hydrochloride is a modified amino acid (L-lysine) for cancer therapy development[1].
Chamaechromone is a biflavonoid ingredient isolated from the roots of Stellera chamaejasme L. (Thymelaeaceae). Chamaechromone possesses anti-hepatitis B virus (HBV) effects against the surface antigen of HBV (HBsAg) secretion and has insecticidal activities[1].
Hydroxyfasudil is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively.
Dabigatran etexilate(BIBR-1048) is the orally active prodrug of dabigatran; Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI) with Ki value of 4.5 nM.IC50 Value: 4.5 nM (Ki); 10 nM(Thrombin-induced platelet aggregation) [1]in vitro: Dabigatran selectively and reversibly inhibited human thrombin(Ki: 4.5 nM) as well as thrombin-induced platelet aggregation (IC(50): 10 nM), while showing no inhibitory effect on other platelet-stimulating agents.Thrombin generation in platelet-poor plasma (PPP), measured as the endogenous thrombin potential (ETP) was inhibited concentration-dependently (IC(50): 0.56 microM). Dabigatran demonstrated concentration-dependent anticoagulant effects in various species in vitro, doubling the activated partial thromboplastin time (aPTT), prothrombin time (PT) and ecarin clotting time (ECT) in human PPP at concentrations of 0.23, 0.83 and 0.18 microM, respectively [1]. in vivo: Dabigatran prolonged the aPTT dose-dependently after intravenous administration in rats (0.3, 1 and 3 mg/kg) and rhesus monkeys (0.15, 0.3 and 0.6 mg/kg). Dose- and time-dependent anticoagulant effects were observed with dabigatran etexilate administered orally to conscious rats (10, 20 and 50 mg/kg) or rhesus monkeys (1, 2.5 or 5 mg/kg), with maximum effects observed between 30 and 120 min after administration, respectively [1]. Patients treated with dabigatran etexilate experienced fewer ischaemic strokes (3.74 dabigatran etexilate vs 3.97 warfarin) and fewer combined intracranial haemorrhages and haemorrhagic strokes (0.43 dabigatran etexilate vs 0.99 warfarin) per 100 patient-years [2].Clinical trial: An Evaluation of the Pharmacokinetics and Pharmacodynamics of Oral Dabigatran Etexilate in Hemodialysis Patients . Phase1
RXFP1 receptor agonist-6 (Example 7) is a RXFP1 receptor agonist. RXFP1 receptor agonist-6 inhibits cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 12 nM[1].
Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
O4I2 is a potent Oct3/4 inducer in various human cell lines including human fibroblasts.Target: Oct3/4O4I2 activates Oct3/4 in HEK293 and embryonal NCCIT cells, and also in Oct-deficient HeLa and terminally differentiated human fibroblasts. O4I2 activates also other pluripotencyassociatedgenes such as Lin28 and Nanog in a drug-like manner. O4I2 shows high activity in enforcing Oct3/4 expression. O4I2 activates Oct3/4 on the transcriptional and translational level in human fibroblasts. O4I2 promotes the expression of pluripotency-associated genes as analyzed by qRT-PCR in human neonatal foreskin fibroblasts (HFFs). O4I2 markedly stimulates Oct3/4 even at 5 μM after 72 h treatment on the translational level.
Glucosamine (hydrochloride) is a natural product.IC50 value:Target:In vitro: Glucosamine hydrochloride exhibited dose-dependent DPPH antioxidant activity [1]. Short-term (4 h) glucosamine hydrochloride treatment inhibited HIF-1α at the protein level, decreased phosphorylation of p70S6K and S6, translation-related proteins [2]. In the obstructed kidneys and TGF-β1-treated renal cells, glucosamine hydrochloride significantly decreased renal expression of α-smooth muscle actin, collagen I, and fibronectin [3]. In vivo:
Apitegromab (SRK-015) is an anti-promyostatin monoclonal antibody. Apitegromab can be used for the research of neuromuscular disease including spinal muscular atrophy[1].
DPLG3 is a specific chymotryptic-like β5i subunits inhibitor. DPLG3 inhibits mouse i-20S with IC50 of 9.4 nM. DPLG3 can be used for immune disease research[1].
Angiotensinogen (1-14) porcine is a polypeptide, which is the N-terminal fragment of angiotensinogen, including amino acid residues 1 to 14[1].
Iodochloromethane-d2 is the deuterium labeled Iodochloromethane[1].
4-Hydroxyacetophenone (P-hydroxyacetophenone) is a key hepatoprotective and choleretic compound in Artemisia capillaris and A. morrisonensis, also has an anti-hepatitis B virus effect and anti-inflammatory effect[1].
Urocortin III, mouse is a corticotropin-releasing factor (CRF)-related peptide. Urocortin III preferentially binds and activates CRF-R2[1].
Absinthin is a structurally unique triterpene, and is responsible for the high bitter value of wormwood. Absinthin is an agonist of the bitter taste receptor hTAS2R46, which reduces cytosolic Ca2+-rises induced by histamine by a receptor-specific mechanism mediated by hTAS2R46[1][2][3].
Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity.
BET-IN-2 is a BET inhibitor with an IC50 of 52 nM for BRD4-BD1.
ZCZ011 is a potent and brain penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain[1].
T807 a novel tau positron emission tomography (PET) tracer.
INT-767 is a dual farnesoid X receptor/TGR5 agonist with mean EC50s of 30 and 630 nM, respectively.
Thalidomide-5-propoxyethanamine is the Thalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein[1].
Magainin 1 is an antimicrobial peptide discovered in the skin of Xenopus laevis.
(Phe2,Orn8)-Oxytocin is a selective V1 vasopressin agonist. (Phe2,Orn8)-Oxytocin induces a sustained contractility of rabbit epididymis with EC50 value of 280 nM[1].
Azelastine HCl is a potent, second-generation, selective, histamine antagonist.Target: Histamine ReceptorAzelastine is a selective H(1)-receptor antagonist that inhibits histamine release and interferes with activation of several other mediators of allergic inflammation. Azelastine can inhibit CHMCs activation and release of IL-6, tryptase, and histamine. On an equimolar basis, azelastine was a more potent inhibitor than olopatadine [1]. Topical azelastine progressively improved itching and conjunctival redness in PAC patients compared to placebo and was at least as effective as levocabastine. Rapid relief is consistent with H(1)-receptor antagonist action, while continued improvement up to 6 weeks may be consistent with mechanisms involving other mediators of allergic inflammation [2]. Azelastine nasal spray was reported to control all rhinitis symptoms, including nasal congestion, regardless of rhinitis diagnosis during the 2-week study period. Patients with seasonal allergic rhinitis and patients with seasonal allergic rhinitis plus nonallergic triggers were identified as patient types most likely to respond to azelastine nasal spray [3].