| DC75748 |
Ivarmacitinib free base |
Ivarmacitinib, also known as SHR0302, is a novel potent JAK inhibitor which blocks JAK/STAT3 signaling, suppresses proliferation, migration and collagen production, and induces the apoptosis of hepatic stellate cells. SHR0302 may attenuate the severity of AA rats, partially through reducing Th17 function and total B cell proportion by inhibiting JAK1-STAT3 phosphorylation. |
|
| DC75749 |
Acalabrutinib (ACP-196) |
Acalabrutinib, also known as ACP-196, is an orally available inhibitor of Bruton’s tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, ACP-196 inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B lymphocyte development, activation, signaling, proliferation and survival. |
|
| DC75750 |
WIC1 |
WIC1 is a novel potent Wnt inhibitor, promoting airway basal stem cell homeostasis, acting to repress phosphorylation of β-cateninY489 and Tp63 expression. |
|
| DC75751 |
Osimertinib mesylate |
Osimertinib, also known as mereletinib and AZD-9291, is a third-generation EGFR inhibitor, showed promise in preclinical studies and provides hope for patients with advanced lung cancers that have become resistant to existing EGFR inhibitors. AZD9291 is highly active in preclinical models and is well tolerated in animal models. It inhibits both activating and resistant EGFR mutations while sparing the normal form of EGFR that is present in normal skin and gut cells, thereby reducing the side effects encountered with currently available medicines. Osimertinib was approved on Nov. 2015. |
|
| DC75752 |
ICI-118551 HCl |
ICI-118551, also known as ICI-118,551 and ICI 111581, is a selective beta-2 (β2) adrenergic receptor antagonist. ICI-118551 binds to the β2 subtype with at least 100 times greater affinity than β1 or β3, the two other known subtypes of the beta adrenoceptor. The compound was developed by Imperial Chemical Industries, which was acquired by AkzoNobel in 2008. ICI-118,551 has no known therapeutic use in humans although it has been used widely in research to understand the action of the β2 adrenergic receptor, as few other specific antagonists for this receptor are known. |
|
| DC75753 |
Enasidenib (AG-221) |
Enasidenib, also known as AG-221 and CC-90007, is a potent and selective IDH2 inhibitor with potential anticancer activity (IDH2 = Isocitrate dehydrogenase 2). The mutations of IDH2 present in certain cancer cells result in a new ability of the enzyme to catalyze the NAPH-dependent reduction of α-ketoglutarate to R(-)-2-hydroxyglutarate (2HG). The production of 2HG is believed to contribute to the formation and progression of cancer . The inhibition of mutant IDH2 and its neoactivity is therefore a potential therapeutic treatment for cancer. |
|
| DC75754 |
DPY-9309 |
DPY-9309, CAS#511529-30-9, is a useful intermediate for chemical synthesis of a number of biologically important molecules, including porphyrins, N-confused porphyrin, bile pigments, photosensitizers, anticancer drugs. |
|
| DC75755 |
GSK-1292263 |
GSK-1292263 is a novel GPR119 agonist that is currently under development for the treatment of type 2 diabetes. GSK1292263 improves glucose regulation in animal models of diabetes, but has no effect on plasma glucose in type 2 diabetics. Unexpectedly, GSK1292263 lowered fasting LDLc and triglycerides (TG), while increasing HDLc in the diabetic subjects. GSK1292263 has significant effects on plasma lipids and lipoprotein particles in dyslipidemic patients when dosed alone and with atorvastatin. |
|
| DC75756 |
H3B-5942 free base |
H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist. In vitro comparisons of H3B-5942 with standard-of-care (SoC) and experimental agents confirmed increased antagonist activity across a panel of ERαWT and ERαMUT cell lines. In vivo, H3B-5942 demonstrated significant single-agent antitumor activity in xenograft models representing ERαWT and ERαY537S breast cancer that was superior to fulvestrant. |
|
| DC75757 |
Evacetrapib |
Evacetrapib (LY2484595) is a novel benzazepine-based CETP inhibitor |
|
| DC75758 |
GSK-189254 free base |
GSK-189254 is a potent and selective H3-receptor inverse agonist. It has subnanomolar affinity for the H3 receptor and selectivity of over 10,000x for H3 over other histamine receptor subtypes. Animal studies have shown it to possess not only stimulant and nootropic effects, but also analgesic action suggesting a role for H3 receptors in pain processing in the spinal cord. GSK-189,254 and several other related drugs are currently being investigated as a treatment for Alzheimer's disease and other forms of dementia, as well as possible use in the treatment of conditions such as narcolepsy, or neuropathic pain which do not respond well to conventional analgesic drugs. |
|
| DC75759 |
Ivabradine HCl |
Ivabradine is a novel medication used for the symptomatic management of stable angina pectoris. Ivabradine acts by reducing the heart rate via specific inhibition of the funny channel, a mechanism different from that of beta blockers and calcium channel blockers, two commonly prescribed antianginal drugs. Ivabradine is a cardiotonic agent. Ivabradine was approved in 2015. Ivabradine acts on the If (f is for "funny", so called because it had unusual properties compared with other current systems known at the time of its discovery) ion current, which is highly expressed in the sinoatrial node. If is a mixed Na+–K+ inward current activated by hyperpolarization and modulated by the autonomic nervous system. It is one of the most important ionic currents for regulating pacemaker activity in the sinoatrial (SA) node. Ivabradine selectively inhibits the pacemaker If current in a dose-dependent manner. Blocking this channel reduces cardiac pacemaker activity, slowing the heart rate and allowing more time for blood to flow to the myocardium. |
|
| DC75760 |
ML204 |
ML204 is a novel and potential TRPC4 Channel inhibitor. ML204 inhibited TRPC4β-mediated intracellular Ca(2+) rise with an IC(50) value of 0.96 μm and exhibited 19-fold selectivity against muscarinic receptor-coupled TRPC6 channel activation. ML204 represents an excellent novel tool for investigation of TRPC4 channel function and may facilitate the development of therapeutics targeted to TRPC4. |
|
| DC75761 |
VTP50469 free base |
VTP-50469 is a novel, potent, selective, orally-available Menin MLL1 inhibitor, being effectively against MLL-rearranged and NPM1c+ leukemia, selectively killing cell lines with MLL rearrangements and NPM1c+ mutations. Cell lines carrying MLL rearrangements were selectively responsive to VTP50469. VTP50469 displaced Menin from protein complexes and inhibited chromatin occupancy of MLL at select genes. Loss of MLL binding led to changes in gene expression, differentiation, and apoptosis. Patient-derived xenograft (PDX) models derived from patients with either MLL-r acute myeloid leukemia or MLL-r acute lymphoblastic leukemia (ALL) showed dramatic reductions of leukemia burden when treated with VTP50469. |
|
| 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. |
|
