Nebracetam hydrochloride, a nootropic M1-muscarinic agonist, induces a rise of intracellular Ca2+ concentration. Nebracetam hydrochloride exhibits an EC50 of 1.59 mM for elevating [Ca2+]i[1].
1alpha, 25-Dihydroxy VD2-D6 is a deuterated form of vitamin D.
Cyanidin, an antioxidant, has protective effect on DNA cleavage, free radical scavenging activity and significant inhibition of XO activity[1].
Netupitant N-oxide is the metabolite of Netupitant, which is a highly selective NK1 receptor antagonist.
IST5-002, a potent Stat5a/b inhibitor, selectively inhibits transcriptional activity of Stat5a/b (IC50s: 1.5 μM for Stat5a, 3.5 μM for Stat5b). IST5-002 inducs cell apoptotic and death of prostate cancer cells and chronic myeloid leukemia (CML) cells. IST5-002 can be used in the research of prostate cancer and chronic myeloid leukemia (CML)[1].
Beauveriolide III is an inhibitor of lipid droplet formation in mouse macrophages[1].
Mebendazole-d3 is the deuterium labeled L-Methionine-34S[1].
5-Hydroxycytosine-13C,15N2 is the 13C and 15N labeled 5-Hydroxycytosine[1].
Exendin-3 is a biologically active peptides isolated from venoms of the Gila monster lizards, Heloderma horridurn .
Pinacyanol iodide is a fluorescent cyanine dye. Pinacyanol iodide exhibits ultrafast excited state isomerization[1].
Metallo-β-lactamase-IN-7 is a potent VIM-Type metallo-β-lactamase inhibitor with IC50s of 0.019 μM, 13.64 μM, 0.38 μM for VIM-2, VIM-1 and VIM-5. Metallo-β-lactamase-IN-7 potentiate antibacterial activity of Meropenem against the Gram-negative bacterial strains[1].
(D)-PPA 1 is a hydrolysisresistant d-peptide antagonist. (D)-PPA 1 serves as a potent PD-1/PD-L1 inhibitor. (D)-PPA 1 binds to PD-1 with the affinity 0f 0.51 μM with in vitro and in vivo efficacy[1].
Lasmiditan (COL-144; LY573144) is a high-affinity, highly selective 5-HT1F receptor agonist(Ki=2.1 nM), compared with Ki of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, respectively.IC50 value: 2.1 nM (Ki, 5-HT1F); >1000 nM (Ki, 5-HT1B/5-HT1D) [1]Target: 5-HT1F receptorin vitro: In vitro binding studies Lasmiditan showed a K(i) value of 2.21 nM at the 5-HT(1F) receptor, compared with K(i) values of 1043 nM and 1357 nM at the 5-HT(1B) and 5-HT(1D) receptors, respectively, a selectivity ratio greater than 470-fold. Lasmiditan showed higher selectivity for the 5-HT(1F) receptor relative to other 5-HT(1) receptor subtypes than the first generation 5-HT(1F) receptor agonist LY334370. Unlike the 5-HT(1B/1D) receptor agonist sumatriptan, lasmiditan did not contract rabbit saphenous vein rings, a surrogate assay for human coronary artery constriction, at concentrations up to 100 μM [1].in vivo: In two rodent models of migraine, oral administration of lasmiditan potently inhibited markers associated with electrical stimulation of the trigeminal ganglion (dural plasma protein extravasation, and induction of the immediate early gene c-Fos in the trigeminal nucleus caudalis) [1]. Two RCTs in the phase II development of lasmiditan was reviewed. In the intravenous placebo-controlled RCT, lasmiditan doses of 2.5-45 mg were used, and there was a linear association between headache relief (HR) rates and dose levels (P < 0.02). For lasmiditan 20 mg, HR was 64 % and for placebo it was 45 % (NS). In the oral placebo-controlled RCT, lasmiditan doses of 50, 100, 200 and 400 mg were used. For HR, all doses of lasmiditan were superior to placebo (P < 0.05). For lasmiditan 400 mg, HR was 64 % and it was 25 % for placebo. Adverse events (AEs) emerging from the treatment were reported by 22 % of the patients receiving placebo and by 65, 73, 87 and 87 % of patients receiving 50, 100, 200 and 400 mg, respectively [2].
3-Hydroxy-3-(4-hydroxyphenyl)-lactic acid is a key metabolite in the P. roqueforti fermentation approach, with quantitative data of 10.2 ± 1.1 µM in Tyr1 (presence of L-tyrosine) of [1].
Glecaprevir is a novel HCV NS3/4A protease inhibitor, with IC50 values ranging from 3.5 to 11.3 nM.
Trx-red (NBL-SS perchlorate) is a red-emitting fluorescent probe derivatized from the nile blue fluorophore. Trx-red is used for selectively imaging thioredoxin (Trx) in live cells and in vivo (λex=615 nm, λem=661 nm)[1].
MPG peptides, Pβ is a primary amphiphilic peptide consisting of three domains[1].
Gatralimab (GZ-402668) is an IgG1 anti-CD52 monoclonal antibody[1].
Tubulin inhibitor 26 (compound 3c) is a potent inhibitor of tubulin. Tubulin inhibitor 26 is an indazole derivative compound. Tubulin inhibitor 26 shows noteworthy low nanomolar potency against HepG2, HCT116, SW620, HT29 and A549 cancer cell lines. Tubulin inhibitor 26 arrests tumor cell in G2/M phase and induced cell apoptosis. Tubulin inhibitor 26 suppresses tumor growth in vivo without affecting the mice body weight[1].
Ivachtin (Caspase-3 Inhibitor VII; compound 7a) is a nonpeptide, noncompetitive and reversibl caspase-3 inhibitor with an IC50 of 23 nM. Ivachtin has modest selectivity for the remaining caspases[1].
Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis treatment[1].
Boc-Glu-OtBu is a glutamic acid derivative[1].
Pirfenidone D5 (AMR69 D5) is a deuterium labeled Pirfenidone. Pirfenidone is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities[1][2][3].
Aplodan is an antiischemic and antiarrhythmic agent. Aplodan has a protective action on cell membrane. Aplodan has the potential for the research of ischemic heart or ischemic heart disease with persistent ventricular premature beats (VPB) [1][2].
Urolithin D is competitive and reversible antagonist of EphA receptors. Urolithin D exhibits intra-classes selectivity[1].
Boc-D-Thr(Bzl)-OH is a threonine derivative[1].
TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) (Free Fatty Acid Receptor) agonist with a pEC50 of 7.39. TUG-499 exhibits >100-fold selectivity over the related receptors FFA2, FFA3, and the nuclear receptor PPARγ and other diverse receptors, ion channels, and transporters. TUG-499 can be used for the research of type 2 diabetes[1].
KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.
SF0166 is a topically administered αvβ3 integrin antagonist, inhibits integrin-ligand interactions with IC50 of 0.6 nM to 13 nM for human αvβ3, αvβ6, and αvβ8; inhibits cellular adhesion to vitronectin across human, rat, rabbit, and dog cell lines with IC50 of 7.6 pM-76 nM; significantly decreases neovascularization in the oxygen-induced retinopathy mouse models. Other Indication Phase 2 Clinical
EZH2-IN-13 is a potent EZH2 inhibitor, for details please refer to compound 73 in patent WO2017139404. EZH2-IN-13 can be used to study cancers or precancerous lesions associated with EZH2 activity[1].