Prazosin is an alpha-adrenergic blocker and is a sympatholytic drug used to treat high blood pressure and anxiety, PTSD, and panic disorder.Target: Adrenergic ReceptorPrazosin, is a sympatholytic drug used to treat high blood pressure and anxiety, PTSD, andpanic disorder. It is an alpha-adrenergic blocker that is specific for the alpha-1 receptors. These receptors are found on vascular smooth muscle, where they are responsible for the vasoconstrictive action of norepinephrine. They are also found throughout the central nervous system. As of 2013, prazosin is off-patent in the US, and the FDA has approved at least one generic manufacturer.In addition to its alpha-blocking activity, prazosin is an antagonist of the MT3 receptor (which is not present in humans), with selectivity for this receptor over the MT1 and MT2 receptors.Prazosin is orally active and has a minimal effect on cardiac function due to its alpha-1 receptor selectivity. However, when prazosin is initially started, heart rate and contractility go up in order to maintain the pre-treatment blood pressures because the body has reached homeostasis at its abnormally high blood pressure. The blood pressure lowering effect becomes apparent when prazosin is taken for longer periods of time. The heart rate and contractility go back down over time and blood pressure decreases.
Cbz-NH-PEG2-C2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].
Gelsemiol is the main active ingredient in Verbena littoralis H. B. K.. Gelsemiol enhanced nerve growth factor (NGF) -induced axonal elongation in PC12D cells[1].
Oxytocin free acid (9-Deamidooxytocin) is an analog of oxytocin in which the glycinamide residue at position 9 in oxytocin has been replaced by a glycine residue. Oxytocin is a pleiotropic, peptide hormone with broad implications for general health, adaptation, development, reproduction, and social behavior[1][2].
Heneicosane is an aroma component isolated from Streptomyces philanthi RL-1-178 or Serapias cordigera. Heneicosane is a pheromone and inhibits aflatoxin production[1][2][3].
Piflufolastat (DCFPYL) can be used to the preparation of piflufolastat F 18 (DCFPyL F-18). piflufolastat F 18. Piflufolastat F-18 is an 18F-labelled diagnostic imaging agent. Piflufolastat F-18 can be used for positron emission tomography (PET) that targets prostate-specific membrane antigen (PSMA)[1].
Thalidomide-Piperazine-PEG1-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].
Alisporivir (DEB-025) is a cyclophilin inhibitor molecule with potent anti-hepatitis C virus (HCV) activity.
C18:0 GM1 Ganglioside-d5 (ammonium) is deuterium labeled C18:0 GM1 Ganglioside (ammonium).
Tetrahydro-β-carboline (Tryptoline) is a metabolite of tryptamine, also is a competitive serotonin reuptake inhibitor with an Ki value of 6.1 µM[1].
Apocynol A is a sesquiterpenoid compound[1].
Butyric acid is a histone deacetylase (HDAC) inhibitor, with anti-tumor effects in several cancers.
ent-17-Hydroxykauran-3-one (ent-Kaurane-3-oxo-17β-ol; compound 7) is a kaurane-type diterpenoid that can be found in the roots of Euphorbia fischeriana[1].
Peptide 74 is a synthetic peptide containing the prodomain sequence of matrix metalloproteinase (MMP). Peptide 74 inhibits the activated form of the 72-kDa type IV collagenase in vitro[1].
TC-Mps1-12 is a potent and selective monopolar spindle 1 (Mps1) inhibitor, with an IC50 of 6.4 nM[1].
Faldaprevir-d7 is deuterium labeled Faldaprevir.
Mca-YVADAP-Lys(Dnp)-OH is a fluorogenic substrate for caspase-1 and angiotensin-converting enzyme 2 (ACE2)[1].
β-Aminopropionitrile is a specific and irreversible lysyl oxidase (LOX) inhibitor. β-Aminopropionitrile targets the active site of LOX or LOXL isoenzymes[1][2].
p,p'-DDE (4,4'-DDE), a major metabolite of persistent dichlorodiphenyltrichloroethane (DDT), is a potent androgen receptor antagonist, with an IC50 of 5 μM and a Ki of 3.5 μM[1].
MK-571-d6 (L-660711-d6) sodium salt is the deuterium labeled MK-571 sodium salt. MK-571 sodium salt is a selective, orally active leukotriene D4 receptor antagonist, with Kis of 0.22 and 2.1 nM in guinea pig and human lung membranes[1][2].
Torcetrapib(CP-529414) is a CETP inhibitor with IC50 of 37 nM, elevates HDL-C and reduces nonHDL-C in plasma.IC50 value: 37 nM [1]Target: CETP inhibitorin vitro: Torcetrapib dose-dependently increases aldosterone release from H295R cells after either 24 or 48 h of treatment with an EC50 of approximately 80 nM, this effect is mediated by calcium channel as calcium channel blockers completely blocks torcetrapib-induced corticoid release and calcium increase. Torcetrapib (1 μM) significantly increases the expression of steroidogenic gene, CYP11B2 and CYP11B1, in H295R cell lines [2].in vivo: Torcetrapib (< 100 mg, daily) changes the plasma distribution of CETP, as the apparent molecular weight of the CETP has shifted to a larger form, by 2 hours after the dose in healthy young subjects. Torcetrapib treatment with 10 mg, 30 mg, 60 mg, and 120 mg daily and 120 mg twice daily results in 16%, 28%, 62%, 73%, and 91% increases in plasma HDL-C, respectively, with no significant changes in TPC in healthy young subjects. [1] Torcetrapib results in an increase of 72.1% in high-density lipoprotein cholesterol and a decrease of 24.9% in low-density lipoprotein cholesterol, in addition to an increase of 5.4 mm Hg in systolic blood pressure, a decrease in serum potassium, and increases in serum sodium, bicarbonate, and aldosterone, in patients at high cardiovascular risk after 12 months' treatment [3]. Torcetrapib (90 mg/kg/day) results in a 70% inhibition of CE transfer in rabbits fed an atherogenic diet. Torcetrapib (90 mg/kg/day) increases mean HDL-C levels by above 3-fold and apoA-I levels by 2.5-fold in plasma in rabbits fed an atherogenic diet. Torcetrapib-treated animal has a multiple-fold increase in HDL-C AUC and a corresponding reduction in aortic lesion area with 60% reduction of aortic free cholesterol (FC) and cholesteryl ester (EC) in rabbits fed an atherogenic diet. Torcetrapib-treated rabbits stimulate free cholesterol efflux to a significantly greater extent than does sera from control rabbits [4].
MDM2-IN-1 (Compound 30) is a synthetic MDM2-p53 interaction (MDM2) inhibitor and contains the trans (D-)configuration[1].
Guanylin(human), a 15-amino acid peptide, is an endogenous intestinal guanylate cyclase activator. Guanylin(human) is mainly found in gastrointestinal tract which regulates electrolytead water transport in intestinal and renal epithelia through cyclic GMP-dependent mechanism[1][2].
5,6-Diamino-N,N,N',N'-tetraethyl-rhodamin is a fluorescent indicator for NO[1].
Palmitoyl dipeptide-7 is a bioactive peptide with anti-aging effect and has been reported used as a cosmetic ingredient[1].
Phellamurin is a plant flavonone glycoside from the leaves of Phellodendron amurense and inhibits intestinal P-glycoprotein. Phellamurin also inhibits egg laying by Papilio protenor. Phellamurin induces cells apoptosis and has anti-tumor activity[1][2][3].
MCC is non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs), such as MCC-DM1[1].
HadAB-IN-1 is a potent HadAB inhibitor. HadAB-IN-1 inhibits HadAB enzyme complexes activity with an IC50 value of 0.03 μM. HadAB-IN-1 also affects mycolic acid biosynthesis in Mycobacterium tuberculosis (Mtb). HadAB-IN-1 can be used for the research of tuberculosis (TB)[1].
m-PEG5-Ms is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
SC144 is the first-in-class orally active small-molecule gp130 inhibitor; inhibits cell growth in a panel of human ovarian cancer cell lines with IC50 values in a submicromolar range.IC50 value: < 1 uM (Cell assay) [1]Target: gp130 inhibitorSC144 shows greater potency in human ovarian cancer cell lines than in normal epithelial cells. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. In addition, SC144 shows potent inhibition of gp130 ligand-triggered signaling. Oral administration of SC144 delays tumor growth in a mouse xenograft model of human ovarian cancer without significant toxicity to normal tissues.