Desamino(D-3-(3′-pyridyl)-Ala2,Arg8)-Vasopressin, a synthetic analog of vasopressin (AVP), is a weak agonist at antidiuretic receptor. However, Desamino(D-3-(3′-pyridyl)-Ala2,Arg8)-Vasopressin is a potent agonist at pituitary corticotrope receptor[1].
Quercetin 7-O-rutinoside is a flavonoid compound from Siparuna glycycarpa[1].
Robustaflavone is a biflavonoid isolated from Doradilla that has natriuretic properties[1].
Vinblastine sulfate is a cytotoxic alkaloid used against various cancer types. Vinblastine sulfate inhibits the formation of microtubule and suppresses nAChR with an IC50 of 8.9 μM.
Galanin (1-19), human is the 1-19 fragment of the human galanin. Galanin (GAL) is a widely distributed neuropeptide with diverse biological effectsincluding modulation of hormone release, antinociception and modification of feeding behavior[1].
Praeroside (Baihuaqianhuoside), a coumarin glycoside. Praeroside can be extracted from the root of Peucedanum praeruptorum and Heracleum dissectum. Praeroside shows anti-inflammatory activity in vitro. Praeroside can be used for the research of inflammation[1][2].
Shizukaol G is a dimeric sesquiterpene. Shizukaol G can be isolated from the roots of Chloranthus japonicus[1].
Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A agonist, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT2, a1-adrenergic receptor, dopamine D2, histamine H1 and a2-adrenergic receptor, respectively, and a pEC50 and pKi of 7.60 and 8.08 for h5-HT1A.
CMX001 (Brincidofovir; HDP-CDV) was developed as an orally active, lipophilic form of cidofovir (CDV); has enhanced activity in vitro and in vivo compared to CDV against certain herpesviruses, adenoviruses and orthopoxviruses.IC50 Value: 5.5 nM (EC50, in PDA at 7 dpi) [3]Target: anti-CMVCMX001 is currently in Phase II clinical studies for development as a therapeutic agent for human CMV, adenovirus and BK virus infections, as well as, for adverse events following smallpox vaccinations.in vitro: In PDA at 7 dpi, the CMX001 50% effective concentration (EC50) was 5.55 nM, the 50% cytotoxic concentration (CC50) was 184.6 nM, and the 50% selectivity index (SI50) was 33.3. The EC90 was 19.7 nM, the CC90 was 5,054 nM, and the SI90 was 256.1. In COS-7 cells, JCV replication was faster and the EC50 and EC90 were 18- and 37-fold higher than those in PDA, i.e., 0.1 μM and 0.74 μM (CC50, 0.67 μM; SI50, 6.7; CC90, 12.2 μM; SI90, 16.5) at 5 dpi [3].in vivo: CMX001 and CDV are equally efficacious at protecting mice from mortality following high ectromelia virus doses (10,000 x LD(50)) introduced by the intra-nasal route or small particle aerosol. Using CMX001 at a 10mg/kg dose followed by 2.5mg/kg doses every other-day for 14 days provided solid protection against mortality and weight loss following an intra-nasal challenge of (100-200) x LD(50) of ectromelia virus [1]. When CMX001 was administered orally to mice infected with HSV-1, mortality was reduced significantly (p≤0.001) with all three dose levels when treatments were initiated 24 h post viral inoculation. When treatments were started 48 h post viral inoculation, 5 and 2.5 mg/kg significantly reduced mortality (p≤ 0.001). If treatments were delayed until 72 h post viral inoculation, CMX001 did not reduce mortality or increase the mean day to death. When mice were infected intranasally with HSV-1 and treatments initiated 24 h post viral inoculation using CMX001 at 5 mg/kg or ACV at 100 mg/kg, virus replication in target organs was reduced by both CMX001 and ACV when compared to vehicle treated mice [2]. Toxicity: Diarrhea was the most common adverse event in patients receiving CMX001 at doses of 200 mg weekly or higher and was dose-limiting at 200 mg twice weekly. Myelosuppression and nephrotoxicity were not observed [4].
Glycine-13C2 is the 13C-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
Ammonium chloride-15N is the 15N labeled Ammonium chloride (HY-1269)[1].
Retrorsine is a naturally occurring toxic pyrrolizidine alkaloid. Retrorsine can bind with DNA and inhibits the proliferative capacity of hepatocytes[1][2].
Rituximab (anti-CD20) is an anti-CD20 chimeric monoclonal antibody used to treat certain autoimmune diseases and types of cancer[1].
WY-47766, a proton pump inhibitor, is used potentially for the treatment of postmenopausal osteoporosis.
Oleanolic acid (Caryophyllin) is a natural compound from plants with anti-tumor activities.
AB-506 is a small-molecule inhibitor targeting HBV core protein, inhibits viral replication in vitro (IC50=77 nM).AB-506 binds to HBV core protein, accelerates capsid assembly and inhibits HBV pgRNA encapsidation.AB-506 blocks cccDNA establishment in HBV-infected HepG2-hNTCP-C4 cells and primary human hepatocytes, leading to inhibition of viral RNA, HBsAg, and HBeAg production (EC50=0.64-1.52 uM).AB-506 demonstrated activity across HBV genotypes A-H and maintains antiviral activity against nucleostide analog-resistant variants in vitro.AB-506 showed an 8 to 20-fold increase in EC50 values against L30F, L37Q, and I105T substitutions.AB-506 exhibits good oral bioavailability, systemic exposure, and higher liver to plasma ratios in rodents.
NBD-Pen high-sensitivity, specific fluorescence probe for lipid radicals. NBD-Pen directly detected lipid radicals in living cells by turn-on fluorescence. In a rat model of hepatic carcinoma induced by diethylnitrosamine (DEN), NBD-Pen detected lipid radical generation within 1 hour of DEN administration.
Metconazole-d6 is the deuterium labeled Metconazole. Metconazole is a triazole fungicide agent.
TMB-8 is a novel Ca 2+ antagonist. TMB-8 may exert inhibitory effects in smooth muscle by blocking Ca 2+ release from intracellular bound stores.
9-Hydroxycamptothecin (9-Hydroxycamptothecine) is a Camptothecin derivative with anticancer activities extracted from patent WO1999001456A1, compound 23c[1].
A2793 is an efficient TWIK-related acid-sensitive K+ channel (TASK)-1 inhibitor, with an IC50 of 6.8 μM[1].
Anticancer agent 168 is an orally active retinoic acid receptor (RAR/RXR) beta2 agonist with ameliorating effects on spinal cord injury (SCI)[1].
Mono-n-Decyl Phthalate-3,4,5,6-d4 is the deuterium labeled Mono-n-Decyl Phthalate[1].
Galangin is an agonist/antagonist of the arylhydrocarbon receptor, and also shows inhibition of CYP1A1 activity.
GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.
endo-BCN-PEG4-PFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
HDAC-IN-45 (Compound 14) is a small molecule HDAC inhibitor and has anticancer activity, also can forms a hydrogenbond with residue Y303. HDAC-IN-45 (Compound 14) has substantial inhibitory effects towards HDAC1, 2 and 3 isoforms with IC50 values of 0.108, 0.585 and 0.563 μM respectively[1].
AGN 195183 is a potent and selective agonist of RARα(Kd=3 nM) with improved binding selectivity relative to AGN 193836; no activity on RARβ/γ.IC50 value: 3 nM (Kd); 200 nM (EC80, RAR Trans.)Target: RARα agonistCompound 4(AGN-195183) inhibited the growth of breast cancer cell lines, and was inactive in an in vivo model of topical irritation.Compound 4 and ATRA inhibit growth of the human breast cancer cell lines, T-47D and SK-BR-3, compound 4 does not cause the topical irritation induced by the RARa-selective retinoid, Am-580. Compound 4 (AGN 195183) is currently in Phase I/IIA clinical trials in cancer patients.
Safironil is an antifibrotic compound. Safironil is a competitive inhibitor of collagen protein synthesis. Safironil reduces liver fibrogenesis by inhibiting HSC activation[1][2].
AzddMeC (CS-92) is an antiviral nucleoside analogue and a potent potent, selective and orally active HIV-1 reverse transcriptase and HIV-1 replication inhibitor. In HIV-1-infected human PBM cells and HIV-1-infected human macrophages, the EC50 values of AzddMeC are 9 nM and 6 nM, respectively[1][2].