Olopatadine HCl is a histamine blocker used to treat allergic conjunctivitis.Target: Histamine ReceptorOlopatadine is one of the second-generation histamine H1 receptor antagonists that are treated for allergic disorders. Olopatadine significantly inhibited the ear swelling and the increased production of IL-4, IL-1beta, IL-6, GM-CSF and NGF in the lesioned ear [1]. Olopatadine was highly and rapidly absorbed in healthy human volunteers. The urinary excretion of olopatadine accounted for not less than 58% and the contribution of metabolism was considerably low in the clearance of olopatadine in humans. Olopatadine is one of the few renal clearance drugs in antiallergic drugs. Olopatadine was shown to be useful for the treatment of allergic rhinitis and chronic urticaria in double-blind clinical trials [2]. AL-4943A inhibits histamine release in a concentration-dependent fashion (IC50 = 559 microM) from human conjunctival mast cell preparations in vitro. Passive anaphylaxis in guinea pig conjunctiva was attenuated by AL-4943A applied 30 min prior to intravenous or topical ocular antigen challenge (ED50 values 0.0067% and 0.0170%, w/v, respectively) [3].
GSK232 is a highly selective, cellularly penetrant CECR2 inhibitor with excellent physicochemical properties.
6,8-Di-C-β-D-xylopyranoside (compound 3bb) is a xylopyranoside isolated from Dendrobium huoshanensis[1].
Mesembrine ((+)-Mesembrine) a main alkaloid that features an aryloctahydroindole skeleton. Mesembrine is a 5-HT transporter inhibitor with a Ki of 1.4 nM. Mesembrine also inhibits phosphodiesterase 4B (PDE4B) with an IC50 of 7.8 μM[1][2].
Z-PDLDA-NHOH is a potent and specific inhibitor of vertebrate collagenase[1].
1-Stearoyl-2-arachidonoyl-sn-glycerol is a diacylglycerol (DAG) containing polyunsaturated fatty acids. 1-Stearoyl-2-arachidonoyl-sn-glycerol can activate PKC. 1-Stearoyl-2-arachidonoyl-sn-glycerol also can augment nonselective cation channel (NSCC) activity[1][2].
Boc-Arg(Mts)-OH cyclohexylammonium salt is an arginine derivative[1].
Bromo-C10-OBn is a PROTAC linker that can be used in the synthesis of PROTACs.
Lobetyol is a natural compound that can be isolated from Lobelia chinensis. Lobetyol induces apoptosis and cell cycle arrest in MKN45 cells. Lobetyol shows anti-virus, anti-inflammation and anti-tumor activity[1][2].
AZD4721 (RIST4721) is the potent and orally active antagonist of acidic CXC chemokine receptor 2 (CXCR2). AZD4721 has the potential for the research of inflammatory disease[1].
CHMFL-ABL-053 is a potent, selective and orally available Bcr-Abl/Src/p38 kinase inhibitor with IC50 of 70/62/90 nM; no inhibitory activity against c-Kit (>10 uM); inhibits the proliferation of CML cell lines K562 (GI50=14 nM), KU812 (GI50=25 nM), and MEG-01 (GI50=16 nM); completely suppresses tumor progression in the K562 cells inoculated xenograft mouse model with 50 mg/kg/day dosage treatment.
MeTC7 is a Vitamin-D receptor (VDR) antagonist. MeTC7 has potent VDR inhibition activity with an IC50 value of 2.9 μM. MeTC7 shows good antitumor effects[1].
MLS1547 is a highly efficacious G protein-biased dopamine D2 receptor (D2R) agonist (Ki=1.2 μM). MLS1547 stimulates D2R G protein-mediated signaling (EC50=0.37 μM in a calcium mobilization assay). MLS1547 acts as an antagonist for dopamine (DA)-stimulated β-arrestin recruitment to the D2R (IC50=9.9 μM)[1][2].
Boc-Phe(3-Br)-OH is a phenylalanine derivative[1].
KRAS G12C inhibitor 22 is a KRAS G12C inhibitor extracted from patent WO2021219072A1, example 120[1].
Asn-Pro-Val-PABC-MMAE TFA (compound 8) is a potent ADC Linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Desacetylcinobufagin is a natural compound used for microbial transformation.
PTP1B-IN-13 is a selective PTP1B inhibitor targeting the allosteric site with an IC50 value of 1.59 μM.
Diethylamine NONOate (DEA NONOate, diethylammonium salt) is a nitric oxide donor. Diethylamine NONOate is a potent antimicrobial agent, which can inhibit Escherichia coli growth. Diethylamine NONOate also can enhance preservation of the donor rat heart[1][2].
PknB-IN-2 (Compound 10) is a Mycobacterium tuberculosis protein kinase B (PknB) inhibitor with an IC50 of 12.1 μM[1].
Casein Kinase inhibitor A86 (CKIα inhibitor A86) is a novel pan-specific CKI (CSNK1) inhibitor (Kd=1-10 nM, CKIα Kd=9.8 nM) that co-targets the transcriptional kinases CDK7 and CDK9, with hardly inhibition of CDK8, CDK13, CDK11a, CDK11b, and CDK19; target both CDK7 and CDK9 with low nM Kd values; induces leukemia cell apoptosis at <160 nM, in correlation to the capacity to stabilize p53; shows high and selective sensitivity against leukemic CFUs in colony-forming unit (CFU) assay, without effect on normal hematopoietic CFUs; blocking CKIα together with CDK7 and/or CDK9 synergistically stabilize p53, deprive leukemia cells of survival and proliferation-maintaining SE-driven oncogenes, induce apoptosis, abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1; demonstrates therapeutic efficacy with preserved hematopoiesis and leukemia cure potential in AML mouse models.
Z-VEID-FMK is a selective inhibitor of caspase-6. Z-VEID-FMK can be used for the research of tumor[1].
K-(D-1-Nal)-FwLL-NH2 is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
Pitavastatin (NK-104) is a potent HMG-CoA reductase inhibitor, Pitavastatin inhibited cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in a human liver cancer cell line (HepG2).IC50 value: 5.8 nM(cholesterol synthesis from aceticacid in HepG2) [1]Target: HMG-CoA reductasein vitro: Pitavastatin inhibited cholesterol synthesis from aceticacid with an IC50 of 5.8 nM in a human liver cancer cell line (HepG2), which indicates that is 2.9 and 5.7 times as potent as simvastatin and atorvastatin, respectively. When the inhibitory activity interms of the ED50 was compared with that of simvastatin,pitavastatin showed a 3-fold stronger activity in the rat and 15-fold stronger activity in a guinea pig model.22 The inhibitory effect of pitavastatin on sterol synthesis is thought to be liver-selective [1]. pitavastatin reduces total and phosphorylated tau levels in a cellular model of tauopathy, and in primary neuronal cultures. The decrease caused by pitavastatin is reversed by the addition of mevalonate, or geranylgeranyl pyrophosphate. The maturation of small G proteins, including RhoA was disrupted by pitavastatin, as was the activity of glycogen synthase kinase 3β (GSK3β), a major tau kinase [4].in vivo: Intravenous treatment with pitavastatin-incorporated nanoparticles, but not with control nanoparticles or pitavastatin alone, inhibited plaque destabilization and rupture associated with decreased monocyte infiltration and gelatinase activity in the plaque[2].The EAM model was established in BALB/c mice by immunization with murine α-myosin heavy chain. Mice were fed pitavastatin (5 mg/kg) or vehicle once daily for 3 weeks from day 0 to day 21 after immunization [3].
Misoprostol acid D5 is deuterium labeled Misoprostol acid. Misoprostol acid is an active metabolite of Misoprostol. Misoprostol is a synthetic analogue of prostaglandin E1 (PGE1), extensively absorbed, and undergoes rapid de-esterification to Misoprostol acid in the gastrointestinal tract after oral administration. Misoprostol can be used for non-steroidal anti-inflammatory drug-induced (NSAID) gastric ulcers[1]. Misoprostol is an oral agent used to induce labor[2].
PF-03622905 is a potent and ATP-competitive PKC inhibitor with IC50s of 5.6 nM, 14.5 nM, 13 nM, 37.7 nM, and 74.1 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCθ, respectively. PF-03622905 shows high specificity for PKC over other protein kinases[1].
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent[1].
Glucagon exhibits marked effects on protein and amino acid metabolism. Glucagon inhibits the incorporation of amino acids into protein of liver, muscle, and pancreas, to increase excretion of nitrogen, to promote hepatic urea synthesis, and to increase the concentration of hepatic transaminases and urea cycle enzymes. Glucagon can promote the hepatic uptake of amino acids, to enhance their incorporation into liver glycogen, and to depress the concentration of amino acids in blood[1].
AC-265347 is a calcium-sensing receptor (CaSR) agonist and positive allosteric modulator (ago-PAM) with the functional affinity (pKB) of 5.1. AC-265347 can be used for the research of hyperparathyroidism and related diseases[1].
Biotinyl-ACTH (1-39) (human) is abiotinylated Adrenocorticotropic Hormone (ACTH) (1-39), human (HY-P1211).