| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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). |
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| 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. |
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| DC75777 |
Ozagrel free acid |
Ozagrel, also known as KCT-0809 and Cataclot, is a thromboxane A2 synthase inhibitor used to treat cerebrovascular diseases. |
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| 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. |
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| DC75779 |
SRT3025 HCl |
SRT3025 is a Novel Sirtuin1 Activator, Down-Regulating Sclerostin and Rescuing Ovariectomy-Induced Bone Loss. |
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| 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. |
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| 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. |
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| 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. |
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| DC75783 |
Coumermycin |
Coumermycin is an antibacterial agent effective against Staphylococcus aureus and Staphylococcus epidermidis. |
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| 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. |
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| 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. |
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| 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. |
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| 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). |
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| DC75788 |
TP353 |
TP353 is a CDK7 inhibitor. |
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| 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. |
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| 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. |
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| 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. |
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| DC75792 |
Estriol |
Estriol is an estrogen, specifically an agonist of the estrogen receptors ERα and ERβ. It is a far less potent estrogen than is estradiol, and as such is a relatively weak estrogen. According to one in vitro study, the relative binding affinity (RBA) of estriol for the human ERα and ERβ was 11.3% and 17.6% of that estradiol, respectively, and the relative transactivational capacity of estriol at the ERα and ERβ was 10.6% and 16.6% of that of estradiol, respectively. Estriol is used as a medication, primarily in hormone therapy for menopausal symptoms. |
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| DC75793 |
Mardepodect free base |
Mardepodect, also known as PF-2545920, is a phosphodiesterase inhibitor selective for the PDE10A subtype, which is potentially useful for the treatment of schizophrenia. Phosphodiesterase 10A (PDE10A) is highly expressed in striatal medium spiny neurons of both the direct and indirect output pathways. PDE10A inhibitors have shown behavioral effects in rodent models that predict antipsychotic efficacy. PF-2545920 is active in a range of antipsychotic models, antagonizing apomorphine-induced climbing in mice, inhibiting conditioned avoidance responding in both rats and mice, and blocking N-methyl-D-aspartate antagonist-induced deficits in prepulse inhibition of acoustic startle response in rats, while improving baseline sensory gating in mice. |
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| DC75794 |
Eliglustat free base |
Eliglustat, also known as GENZ-112638, (trade name Cerdelga) is a treatment for Gaucher's disease developed by Genzyme Corp that was approved by the FDA August 2014. Commonly used as the tartrate salt, Eliglustat is believed to work by inhibition of glucosylceramide synthase. |
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| DC75795 |
Fasudil hydrochloride |
Fasudil, also known as HA-1077, is a potent Rho-kinase inhibitor and vasodilator. Since it was discovered, it has been used for the treatment of cerebral vasospasm, which is often due to subarachnoid hemorrhage, as well as to improve the cognitive decline seen in stroke victims. It has been found to be effective for the treatment of pulmonary hypertension. It was demonstrated in February 2009 that fasudil could also be used to enhance memory and improve the prognosis of Alzheimers patients. It is approved for use in Japan and China. |
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| DC75796 |
Oritavancin diphosphate |
Oritavancin, also known as LY333328, is a novel semisynthetic glycopeptide antibiotic. On August 6, 2014, the FDA approved oritavancin for treatment of skin infections. Oritavancin possesses potent and rapid bactericidal activity in vitro against a broad spectrum of both resistant and susceptible Gram-positive bacteria, including Staphylococcus aureus, MRSA, enterococci, and streptococci. Oritavancin was more active than either metronidazole or vancomycin against strains of Clostridium difficile tested. Oritavancin has potential use as a therapy for exposure to Bacillus anthracis, the Gram-positive bacterium that causes anthrax, having demonstrated efficacy in a mouse model both before and after exposure to the bacterium. The 4'-chlorobiphenylmethyl group disrupts the cell membrane of Gram-positive bacteria. It also acts by inhibition of transglycosylation and inhibition of transpeptidation. |
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| DC75797 |
Ritlecitinib tosylate |
Ritlecitinib, also known as PF-06651600, is a potent and selective JAK3 inhibitor. PF-06651600 is a potent and low clearance compound with demonstrated in vivo efficacy. The favorable efficacy and safety profile of this JAK3-specific inhibitor PF-06651600 led to its evaluation in several human clinical studies. JAK3 was among the first of the JAKs targeted for therapeutic intervention due to the strong validation provided by human SCID patients displaying JAK3 deficiencies. |
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| DC75798 |
Vorapaxar free base |
Vorapaxar, also known as SCH 530348, is a thrombin receptor (protease-activated receptor, PAR-1) antagonist based on the natural product himbacine. vorapaxar was approved in 2014. Vorapaxar is a new anti-platelet drug that is part of the PAR-1 antagonist family, a new class of anti-platelet drug. It functions by inhibiting thrombin-related platelet aggregation. This mechanism works by a different pathway than other anti-platelet medications such as aspirin and P2Y12 inhibitors. Unlike many other medication, vorapaxar does not affect ADP-mediated platelet aggregation, coagulation parameters, or bleeding time. |
|
| DC75799 |
Bobcat339 free base |
Bobcat339 is a novel cytosine-based TET enzyme inhibitor with IC50 of 33 uM (TET1) and 73 uM (TET2). Bobcat339 has mid-μM inhibitor activity against TET1 and TET2, but does not inhibit the DNA methyltransferase, DNMT3a. These new molecular tools will be useful to the field of epigenetics and serve as a starting point for new therapeutics that target DNA methylation and gene transcription. |
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