PG-931, an analog of SHU 9119, is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R (IC50=2.4 nM). PG-931 can reverse haemorrhagic shock and prevent multiple organ damage in vivo.

2,3-Dehydro-3,4-dihydro ivermectin is an analog of ivermectin and an anthelmintic. 2,3-Dehydro-3,4-dihydro ivermectin has activity against L. amazonensis promastigotes and amastigotes (IC50s=13.8 and 3.6 µM, respectively) without inducing cytotoxicity to macrophages (IC50= 65.5 µM).

2,6-Dichlorodiphenylamine is an analogue of Diclofenac Sodium and has anti-Candida albicans activity. Diclofenac Sodium is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells.

[Ala17]-MCH, a MCH analogue, is a selective ligand for MCHR1 (Ki=0.16 nM) over MCHR2 (Ki=34 nM). [Eu3+ chelate-labeled [Ala17]-MCH shows high affnity for MCHR1 (Kd=0.37 nM) while has little demonstrable binding affnity for MCHR2.

[Ala17]-MCH TFA, a MCH analogue, is a selective ligand for MCHR1 (Ki=0.16 nM) over MCHR2 (Ki=34 nM). [Eu3+ chelate-labeled [Ala17]-MCH shows high affnity for MCHR1 (Kd=0.37 nM) while has little demonstrable binding affnity for MCHR2.

Resorufin pentyl ether (Pentoxyresorufin; 7-Pentoxyphenoxazone) is a Resazurin analogue. Resorufin pentyl ether acts as a substrate to distinguish between different induced cytochromes P-450. Resorufin pentyl ether maintains bactericidal activity against N. gonorrhoeae in vitro.

1,1,3-Tribromoacetone is an impurity of Methotrexate. Methotrexate, an antimetabolite and antifolate agent, inhibits the enzyme dihydrofolate reductase, thereby preventing the conversion of folic acid into tetrahydrofolate, and inhibiting DNA synthesis.

Phosphoramide mustard cyclohexanamine is the major metabolite for Cyclophosphamide, with anticancer activitiy. Phosphoramide mustard cyclohexanamine induces DNA adduct formation in ovarian granulosa cells, induces DNA damage and elicits the ovarian DNA repair response.

trans-R-138727MP (Prasugrel metabolite R-138727MP) is the active metabolite derivative of Prasugrel. Prasugrel, a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.

Valecobulin hydrochloride (CKD-516 hydrochloride) is a valine prodrug of S516 and a vascular disrupting agent (VDA). Valecobulin hydrochloride is a potent β-tubulin polymerization inhibitor with marked antitumor activity against murine and human solid tumors.

Thalifendine chloride is a metabolite of Berberine, with antiplasmodial and antiamoebic activities. Thalifendine chloride shows activity against P. falciparum and E. histolytica with IC50s of 7.91 μM and 116 μM, respectively.

Isopsoralenoside is a benzofuran glycoside from Psoralea corylifolia. Isopsoralenoside can be quickly metabolized to Psoralen in digestive tract contents. Isopsoralenoside show estrogen-like activity, osteoblastic proliferation accelerating activity, antitumor effects and antibacterial activity.

Phosphoramide mustard is the major metabolite for Cyclophosphamide, with anticancer activitiy. Phosphoramide mustard induces DNA adduct formation in ovarian granulosa cells, induces DNA damage and elicits the ovarian DNA repair response.

Nociceptin (1-7) TFA is the N-terminal bioactive fragment of nociceptin. Nociceptin (1-7) TFA is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) TFA combines with nociceptin reduces hyperalgesia in vivo.

(Rac)-PF-06256142 is the less effective enantiomer of PF-06256142. (Rac)-PF-06256142 is an agonist of D1 receptor, with an EC50 of 107 nM. (Rac)-PF-06256142 can be used for the research of schizophrenia and Parkinson's disease.

Nociceptin (1-7) is the N-terminal bioactive fragment of nociceptin. Nociceptin (1-7) is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia in vivo.

(R)-Bicalutamide is the (R)-enantiomer of Bicalutamide. (R)-Bicalutamide is an androgen receptor (AR) antagonist, with an antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer.

NHC-triphosphate tetraammonium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) as a triphosphate form. NHC-triphosphate tetraammonium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA.

Atorvastatin lactone D5 is a deuterated form of Atorvastatin lactone. Atorvastatin lactone is a prodrug form of atorvastatin. Atorvastatin is an orally active 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor.

NHC-triphosphate triammonium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) as a triphosphate form. NHC-triphosphate triammonium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA.

NHC-triphosphate tetrasodium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) as a triphosphate form. NHC-triphosphate tetrasodium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA.

Toltrazuril sulfoxide is a short-lived intermediary metabolite of Toltrazuril, and then can be metabolized to the reactive toltrazuril sulfone (TZR-SO2) in vivo. Toltrazuril is an antiprotozoal agent that acts upon Coccidia parasites.

Ursonic acid methyl ester is an esterified derivative of Ursolic acid. Ursonic acid methyl ester shows growth inhibitory activity against four tumor cell lines, HL-60, BGC, Bel-7402 and Hela with ED50 values of >100 μg/ml.

Amifostine thiol (WR-1065) is an active metabolite of the cytoprotector Amifostine. Amifostine thiol is a cytoprotective agent with radioprotective abilities. Amifostine thiol activates p53 through a JNK-dependent signaling pathway.

RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619. RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis.

Ferulic acid acyl-β-D-glucoside is a metabolite of Ferulic Acid. Ferulic acid is a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor with IC50s of 3.78 and 12.5 μM for FGFR1 and FGFR2, respectively.

(E)-10-Hydroxynortriptyline (E-10-OH-NT) is a metabolite of Nortriptyline. Nortriptyline is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and is used to relieve the symptoms of depression.

Dihydroseselin is a 7-hydroxycoumarin derivative. 7-hydroxycoumarin is a natural product of the coumarin family, is a fluorescing compound which can be used as a sunscreen agent

Picroside IV is an iridoid glycoside found in the underground parts of Picrorhiza scrophulariiflora. Picroside IV is a derivative of Catalpol. Catalpol has neuroprotective, hypoglycemic, anti-inflammatory, anti-cancer, anti-spasmodic, anti-oxidant effects and anti-HBV effects.

(S)-Pro-xylane ((S)-Hydroxypropyl tetrahydropyrantriol) is the S-enantiomer of Pro-xylane. Pro-xylane is a biologically active C-glycoside in aqueous media, acts as an activator of glycosaminoglycans (GAGs) biosynthesis.