| DC75762 |
SUVN-911 HCl |
SUVN-911 is a potent and selective α4β2 nAChR antagonist. SUVN-911 showed excellent ADME properties with no drug-drug interaction liability and robust efficacy in animal models of depression. it is a potent α4β2 receptor ligand with a Ki value of 1.5 nM. It showed >10 μM binding affinity toward the ganglionic α3β4 receptor apart from showing selectivity over 70 other targets. It is orally bioavailable and showed good brain penetration in rats. |
|
| DC75763 |
PYR-6502 |
PYR-6502, CAS#27226-50-2, is a useful intermediate for chemical synthesis of a number of biologically important molecules, including porphyrins, bile pigments, photosensitizers, anticancer drugs. |
|
| DC75764 |
Pimavanserin free base |
Pimavanserin, also known as ACP-103, is an inverse agonist on the serotonin receptor subtype 5-HT2A, with 40x selectivity over 5-HT2C, and no significant affinity or activity at 5-HT2B or dopamine receptors. Pimavanserin is a novel drug candidate for Parkinson's psychosis.Parkinson's disease psychosis (PDP) is a condition that may develop in up to 60 % of Parkinson's patients, and is a major reason for nursing home placement for those affected. |
|
| DC75765 |
PYR-8535 |
PYR-8535, CAS#62618-53-5, is pyrrole derivative, and is a useful intermediate for chemical synthesis of a number of biologically important molecules, including porphyrins, bile pigments, photosensitizers, anticancer drugs. |
|
| DC75766 |
PYR-5120 |
PYR-5120, CAS#59435-12-0, is a useful intermediate for chemical synthesis of a number of biologically important molecules, including porphyrins, bile pigments, photosensitizers, anticancer drugs. |
|
| DC75767 |
Piboserod |
Piboserod, also known as SB-207266, is a selective 5-HT4 receptor antagonist which was marketed and manufactured by GlaxoSmithKline (GSK) under the trade name Serlipet for the management of atrial fibrillation and irritable bowel syndrome. In 2007 the Norwegian company Bio-Medisinsk Innovasjon AS (BMI) completed a clinical phase II study to investigate the effect of piboserod in patients with chronic heart failure. |
|
| DC75768 |
PYR-6921 |
PYR-6921, CAS#31896-92-1, is a useful intermediate for chemical synthesis of a number of biologically important molecules, including porphyrins, bile pigments, photosensitizers, anticancer drugs. |
|
| DC75769 |
PYR-0503 |
PYR-0503, CAS#16200-50-3, is a useful intermediate for chemical synthesis of a number of biologically important molecules, including porphyrins, bile pigments, photosensitizers, anticancer drugs. |
|
| DC75770 |
PYR-8750 |
PYR-8750, CAS#938-75-0, is a useful intermediate for chemical synthesis of a number of biologically important molecules, including porphyrins, bile pigments, photosensitizers, anticancer drugs. |
|
| DC75771 |
Pritelivir |
Pritelivir, also known as AIC-316 and BAY 57-1293, is a potent helicase primase inhibitor. BAY 57-1293 inhibits replication of herpes simplex virus (HSV) type 1 and type 2 in the nanomolar range in vitro by abrogating the enzymatic activity of the viral primase-helicase complex. In various rodent models of HSV infection the antiviral activity of BAY 57-1293 in vivo was found to be superior compared to all compounds currently used to treat HSV infections. The compound shows profound antiviral activity in murine and rat lethal challenge models of disseminated herpes, in a murine zosteriform spread model of cutaneous disease, and in a murine ocular herpes model. It is active in parenteral, oral, and topical formulations. |
|
| DC75772 |
Pseudouridimycin TFA |
Pseudouridimycin (PUM) is an antibiotic that inhibits bacterial RNA polymerase (RNAP). It is a nucleoside analog that is effective against both Gram-positive and Gram-negative bacteria. PUM has a low rate of resistance acquisition and a wide range of antibacterial activity. It is shown that PUM particularly inhibits bRNAP in vitro, with an IC50 of ∼0.1 μM and also with a minimum inhibitory concentration (MIC) of 4 to 6 μg/mL. In vitro bactericidal activity is reported for PUM against drug-sensitive, drug-resistant, and multidrug-resistant Streptococcus species. |
|
| DC75773 |
Bremelanotide acetate featured |
Bremelanotide is a melanocortin receptor (MCR) agonist that nonselectively activates several receptor subtypes with the following order of potency: MC1R, MC4R, MC3R, MC5R, MC2R. At therapeutic dose levels, binding to MC1R and MC4R is most relevant. Neurons expressing MC4R are present in many areas of the central nervous system (CNS). The mechanism by which VYLEESI improves HSDD in women is unknown. The MC1R is expressed on melanocytes; binding at this receptor leads to melanin expression and increased pigmentation. Bremelanotide was approved in 6/21/2018 To treat hypoactive sexual desire disorder in premenopausal women. |
|
| DC75774 |
Dasabuvir (ABT-333) |
Dasabuvir, also known as ABT-333, is a non-nucleoside polymerase inhibitor currently under clinical trials for the treatment of Hepatitis C. In the United States, it is approved by the Food and Drug Administration for use in combination with ombitasvir, paritaprevir, and ritonavir in the product Viekira Pak. Dasabuvir acts as a NS5B (an RNA-directed RNA polymerase) inhibitor. |
|
| DC75775 |
Iptacopan free base |
Iptacopan, also known as LNP023, is a complement Factor B Inhibitor (IC50=10 nM). LNP023 improves LN in MRL/lpr mice. The mechanism is as follows: LNP023 binds to CFB to inhibit the activation of the alternative complement pathway. LNP023 treatment for LN may also play a role in regulating the protein expression of AKT, TNF-α, and STST3. LNP023 showed low clearance and high bioavailability (62.2%). Furthermore, four minor metabolites from rat plasma were detected and identified by LC combined with high-resolution mass spectrometry. The metabolic pathways were O-deethylation (M1), hydroxylation (M4), oxidation (M3), and acyl-glucuronidation (M2). |
|
| DC75776 |
PYR-7911 |
PYR-7911, CAS#124307-91-1, pyrrole derivative, and is a useful intermediate for chemical synthesis of a number of biologically important molecules, including porphyrins, bile pigments, photosensitizers, anticancer drugs. |
|
| DC75777 |
Ozagrel free acid |
Ozagrel, also known as KCT-0809 and Cataclot, is a thromboxane A2 synthase inhibitor used to treat cerebrovascular diseases. |
|
| DC75778 |
Alvelestat (AZD9688) |
Avelestat, also known as AZD9668 and MPH-966, is a novel, oral inhibitor of neutrophil elastase (NE), an enzyme implicated in the signs, symptoms, and disease progression in NE-driven respiratory diseases such as bronchiectasis and chronic obstructive pulmonary disease via its role in the inflammatory process, mucus overproduction, and lung tissue damage. In cell-based assays, AZD9668 inhibited plasma NE activity in zymosan-stimulated whole blood. AZD9668 has the potential to reduce lung inflammation and the associated structural and functional changes in human diseases. |
|
| DC75779 |
SRT3025 HCl |
SRT3025 is a Novel Sirtuin1 Activator, Down-Regulating Sclerostin and Rescuing Ovariectomy-Induced Bone Loss. |
|
| DC75780 |
BBT-594 |
BBT594, also known as NVP-BBT594, is potent and selective RET and JAK2 inhibitor. NVP-BBT594 impairs GDNF-RET signaling and GDNF-dependent growth of MCF7-LTED cells. NVP-BBT594 targets GDNF-RET signaling and sensitizes MCF7-2A cells to letrozole treatment. GDNF-RET signaling as a rational therapeutic target may be useful to combat or delay the onset of AI resistance in breast cancer. |
|
| DC75781 |
Aspoxicillin |
Aspoxicillin is classified under the β-lactam family of antibiotics and is a semisynthetic penicillin with a broad spectrum of antibacterial activities against Gram-positive and Gram-negative anaerobic bacteria. |
|
| DC75782 |
Dubermatinib |
Dubermatinib, also known as TP-0903, is a potent and selective AXL inhibitor. TP-0903 induces massive apoptosis in CLL B cells with LD50 values of nanomolar ranges. Combination of TP-0903 with BTK inhibitors augments CLL B-cell apoptosis AXL overexpression is a reoccurring theme observed in multiple tumor types that have acquired resistance to various agents. Treatment of cancer cells with TP-0903 reverses the mesenchymal phenotype in multiple models and sensitizes cancer cells to treatment with other targeted agents. Administration of TP-0903 either as a single agent or in combination with BTK inhibitors may be effective in treating patients with CLL. |
|
| DC75783 |
Coumermycin |
Coumermycin is an antibacterial agent effective against Staphylococcus aureus and Staphylococcus epidermidis. |
|
| DC75784 |
BLZ945 |
Sotuletinib, also known as BLZ945, is a potent and selective CSF-1R kinase inhibitor. BLZ945 showed effects of CSF1R inhibition on other tumor-infiltrating immune cells. BLZ945 attenuates the turnover rate of TAMs while increasing the number of CD8+ T cells that infiltrate cervical and breast carcinomas. BLZ945 decreases the growth of malignant cells in the mouse mammary tumor virus-driven polyomavirus middle T antigen (MMTV-PyMT) model of mammary carcinogenesis. BLZ945 prevents tumor progression in the keratin 14-expressing human papillomavirus type 16 (K14-HPV-16) transgenic model of cervical carcinogenesis. |
|
| DC75785 |
Duvoglustat HCl |
Duvoglustat, also known as AT2220, 1-Deoxynojirimycin, Moranoline, deoxynojirimycin or DNJ, is a potent and selective alpha-glucosidase inhibitor, most commonly found in mulberry leaves. Duvoglustat is used to suppress the elevation of postprandial hyperglycemia. Duvoglustat acts as an antihyperglycemic agent by slowing the rate of carbohydrate degradation to monosaccharides. Duvoglustat inhibits glucose absorption by suppressing intestinal glucose transport. Duvoglustat accelerates glucose utilization by regulating hepatic glucose metabolism enzymes. Duvoglustat directly regulates expression of hepatic enzymes involved in glucose metabolism. |
|
| DC75786 |
BAI1 inhibitor |
Brain-specific angiogenesis inhibitor 1 is a protein that in humans is encoded by the BAI1 gene. It is a member of the adhesion-GPCR family of receptors. |
|
| DC75787 |
Olverembatinib (GZD824) |
Olverembatinib, also known as GZD824, is a novel orally bioavailable inhibitor against a broad spectrum of Bcr-Abl mutants including T315I. GZD824 tightly bound to Bcr-Abl(WT) and Bcr-Abl(T315I) with K(d) values of 0.32 and 0.71 nM, respectively, and strongly inhibited the kinase functions with nanomolar IC(50) values. GZD824 potently suppressed proliferation of Bcr-Abl-positive K562 and Ku812 human CML cells with IC(50) values of 0.2 and 0.13 nM, respectively. GZD824 also displayed good oral bioavailability (48.7%), a reasonable half-life (10.6 h), and promising in vivo antitumor efficacy. It induced tumor regression in mouse xenograft tumor models driven by Bcr-Abl(WT) or the mutants and significantly improved the survival of mice bearing an allograft leukemia model with Ba/F3 cells harboring Bcr-Abl(T315I). |
|
| DC75788 |
TP353 |
TP353 is a CDK7 inhibitor. |
|
| DC75789 |
SGC2085 free base |
SGC2085 is a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor with an IC50 of 50 nM and more than undred-fold selectivity over other PRMTs. CARM1 is an important positive modulator of Wnt/β-catenin transcription and neoplastic transformation in colorectal cancer as well as a critical factor in estrogen-stimulated breast cancer growth, and its depletion results in decreased proliferation of myeloid leukemia cells in vivo. |
|
| DC75790 |
SAG (Smo agonist) free base |
SAG is a potent Smoothened (Smo) receptor agonist (Kd = 59 nM); sag antagonizes cyclopamine action at the Smo receptor. SAG potently activates the Hedgehog signaling pathway in Shh-light 2 cells (EC50 ~ 3 nM). SAG induces pathway activation independently of Ptch proteins. The Smoothened receptor (SMO) mediates signal transduction in the hedgehog pathway, which is implicated in normal development and carcinogenesis. SMO antagonists can suppress the growth of some tumours. |
|
| DC75791 |
Fabomotizole mesylate |
Fabomotizole, also known as Afobazole, is an anxiolytic drug launched in Russia in the early 2000s. It produces anxiolytic and neuroprotective effects without any sedative or muscle relaxant actions. Its mechanism of action remains poorly defined however, with GABAergic, NGF- and BDNF-release-promoting, MT1 receptor agonism, MT3 receptor antagonism, and sigma agonism suggested as potential mechanisms. Fabomotizole was shown to inhibit MAO-A reversibly and there might be also some involvement with serotonin receptors. Clinical trials have shown fabomotizole to be well tolerated and reasonably effective for the treatment of anxiety. |
|
