| DC74765 |
Manidipine HCl |
Manidipine, also known as CV-4093, is a calcium channel blocker (dihydropyridine type) that is used clinically as an antihypertensive. Manidipine is a lipophilic, third-generation dihydropyridine calcium channel antagonist with a high degree of selectivity for the vasculature, thereby inducing marked peripheral vasodilation with negligible cardiodepression. In addition, manidipine does not significantly affect norepinephrine levels, suggesting a lack of sympathetic activation. Manidipine has shown antihypertensive efficacy and appears to be well tolerated in adult and elderly patients with mild or moderate essential hypertension. |
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| DC74766 |
ARTD3/PARP3-IN-1 |
ARTD3/PARP3-IN-1 is an unselective inhibitor of diphtheria toxin-like ADP-ribosyltransferase 3 (ARTD3)/PARP3. |
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| DC74767 |
NDM-1 inhibitor-3 |
NDM-1 inhibitor-3 (Compound 89) is a New Delhi Metallo-β-lactamase-1 (NDM-1) inhibitor |
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| DC74768 |
Tosufloxacin tosylate |
Tosufloxacin, also known as T-3262, is a fluoroquinolone antibiotic used to treat susceptible infections. It has a controversial safety profile in relation to other fluoroquinolones. It is associated with severe thrombocytopenia and nephritis, and hepatotoxicity. It is sold in Japan under the brand name Ozex. |
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| DC74769 |
NSC-87877 free acid |
NSC-87877 is a cell-permeable, inhibitor of both SHP-1 and SHP-2 (IC50 = 355 and 318 nM, respectively). NSC-87877 shows effective growth inhibition and induction of apoptosis in NB cell lines. In an intrarenal mouse model of NB, NSC-87877 treatment results in decreased tumor growth and increased p53 and p38 activity. DUSP26 inhibition with NSC-87877 is an effective strategy to induce NB cell cytotoxicity in vitro and in vivo through activation of the p53 and p38 mitogen-activated protein kinase (MAPK) tumor-suppressor pathways. |
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| DC74770 |
Tubulin inhibitor 32 |
Tubulin inhibitor 32 is a potent and orally active tubulin inhibitor. |
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| DC74771 |
Ulipristal acetate |
Ulipristal acetate, also known as CDB-2914, is a selective progesterone receptor modulator (SPRM) approved for contraception, and for uterine fibroid. As a SPRM, ulipristal acetate has partial agonistic as well as antagonistic effects on the progesterone receptor. It also binds to the glucocorticoid receptor, but is only a weak antiglucocorticoid relative to mifepristone, and has no relevant affinity to the estrogen, androgen and mineralocorticoid receptors. |
|
| DC74772 |
SLx-2119 |
SLx-2119, also known as KD-025 and Belumosudil, is an orally bioavailable inhibitor of ROCK-II that is greater than 200-fold selective over ROCK-I (IC50s = 105 nM and 24 µM, respectively). |
|
| DC74773 |
VU0364572 free base |
VU0364572 free base is an orally active and selective allosteric agonist of the M1 muscarinic receptor. |
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| DC74774 |
SHP099 HCl |
SHP099 is a potent, selective, orally bioavailable, and efficacious SHP2 inhibitor with IC50 =0.07 μM and p-ERK modulation in cells IC50 = 0.250 μM. SHP099 exhibits dose-dependent pathway inhibition and antitumor activity in xenograft models. SHP2 is a nonreceptor protein tyrosine phosphatase (PTP) encoded by the PTPN11 gene involved in cell growth and differentiation via the MAPK signaling pathway. SHP2 also purportedly plays an important role in the programmed cell death pathway (PD-1/PD-L1). Because it is an oncoprotein associated with multiple cancer-related diseases, as well as a potential immunomodulator, controlling SHP2 activity is of significant therapeutic interest. |
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| DC74775 |
VU0364572 TFA |
VU0364572 TFA is an orally active and selective allosteric agonist of the M1 muscarinic receptor. |
|
| DC74776 |
HT-61 |
HT-61, also known as HY-50A, is a pyrroloquinolone antibiotic potentially for the treatment of staphylococcal infections. HT61 was effective at reducing biofilm viability and was associated with increased expression of cell wall stress and division proteins, confirming its potential as a treatment for S. aureus biofilm infections. HT61 enhances the effect of tobramycin against Pseudomonas aeruginosa in vitro and in vivo. |
|
| DC74777 |
Ivermectin |
Ivermectin is a medication that is effective against many types of parasites. It is used to treat head lice, scabies, river blindness, strongyloidiasis, and lymphatic filariasis, among others. Ivermectin and other avermectins (insecticides most frequently used in home-use ant baits) are macrocyclic lactones derived from the bacterium Streptomyces avermitilis. Ivermectin kills by interfering with nervous system and muscle function, in particular by enhancing inhibitory neurotransmission. Ivermectin is a mixture of mostly avermectin H2B1a (CAS# 71827-03-7) with some avermectin H2B1b (CAS# 70209-81-3), which are macrolides from STREPTOMYCES avermitilis. |
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| DC74778 |
LY 43578 |
LY 43578 is an aromatase inhibitor. |
|
| DC74779 |
TASK-1-IN-1 |
TASK-1-IN-1 is a potent and selective TASK-1 inhibitor. |
|
| DC74780 |
Lefamulin free base |
Lefamulin is an antibiotic medication used it to treat adults with community-acquired bacterial pneumonia. It is a pleuromutilin antibiotic that inhibits the large subunit of bacterial ribosomes Lefamulin is used to treat adults with community-acquired bacterial pneumonia. It was also investigated for treatment of acute bacterial skin and skin-structure infections (ABSSSI). Lefamulin has in vitro activity against Streptococcus viridans, Moraxella catarrhalis, Enterococcus faecium, methicillin-resistant Staphylococcus aureus (MRSA), among other bacteria. . Lefamulin was approved in 2019. |
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| DC74781 |
PDCD4-IN-1 |
PDCD4-IN-1(compound 20031600) is a PDCD4 inhibitor. |
|
| DC74782 |
CDK8-IN-12 |
CDK8-IN-12 is an orally active, potent CDK8 inhibitor. |
|
| DC74783 |
Raxatrigine HCl |
Raxatrigine, also known as vixotrigine, GSK1014802, and CNV1014802, is a small molecule state-dependent sodium channel blocker; Nav1.7 sodium channel inhibitor. |
|
| DC74784 |
Beloxepin |
Beloxepin, also known as ADL-6906; ORG-4428, is an oral dual selective serotonin and norepinephrine uptake inhibitor. |
|
| DC74785 |
PARP-1-IN-4 |
PARP-1-IN-4 is a PARP-1 inhibitor. |
|
| DC74786 |
Physostigmine salicylate |
Physostigmine salicylate is a reversible cholinesterase inhibitor, a parasympathomimetic alkaloid. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity. |
|
| DC74787 |
LY 235959 new |
LY 235959 is a competitive NMDA receptor antagonist. |
|
| DC74788 |
PF-670462 HCl |
PF-670462 is a potent inhibitor of the CK1 isoforms CK1ε and CK1δ (IC50 = 7.7 and 14 nM, respectively), with applications towards treatment of bladder cancer. Inhibition of CKIepsilon yields a perturbation of oscillator function that forestalls light as a zeitgeber, and they demonstrate that pharmacological tools such as PF-670462 may yield valuable insight into clock function. Casein kinase Iepsilon (CKIepsilon) is an essential component of the biological clock, phosphorylating PER proteins, and in doing so regulating their turnover and nuclear entry in oscillator cells of the suprachiasmatic nucleus (SCN). |
|
| DC74789 |
CAY10462 HCl |
CAY10462 is the hydrochloride salt of CAY10434 and selective inhibitor of the 20-HETE synthase CYP4A11 exhibiting an IC50 of 8.8 nM when tested in human renal microsomes.4 CAY10434 is nearly 200 times less potent as an inhibitor of 1A, 1C, and 3A CYP450. |
|
| DC74790 |
PROTAC MDM2 Degrader-2 |
PROTAC MDM2 Degrader-2 is a MDM2 degrader based on PROTAC technology. |
|
| DC74791 |
Oxantel Pamoate |
Oxantel Pamoate is an anthelmintic used to treat Trichuris trichiura infection. |
|
| DC74792 |
KN62 |
KN62 is a P2X7R antagonist (hP2X7 IC50 = 51 nM) and Ca2+/calmodulin-dependent protein kinase II inhibitor. KN62 inhibits the invasiveness of cancer cells in vitro and in vivo KN62 causes retrograde amnesia in the rat. KN62 attenuates glutamate release by inhibiting voltage-dependent Ca(2+)-channels. The effect of KN62 on Ca(2+)-influx appears to be specific to slowly-or non-inactivating conductances, and therefore presents KN62 as a potentially useful tool. |
|
| DC74793 |
PF-5274857 freebase |
PF-5274857 is a potent, orally active and selective hedgehog (Hh) signaling pathway inhibitor with an IC50 of 5.8 nM and a Ki of 4.6 nM. PF-5274857 was found to effectively penetrate the blood-brain barrier and inhibit Smo activity in the brain of primary medulloblastoma mice, resulting in improved animal survival rates. PF-5274857 was orally available and metabolically stable in vivo. PF-5274857 is a potentially attractive clinical candidate for the treatment of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway. |
|
| DC74794 |
Otenabant free base |
Otenabant Hydrochloride is the salt of Otenabant, also known as CP-945,598, a drug which acts as a potent and highly selective CB1 antagonist. It was developed by Pfizer for the treatment of obesity, but development for this application has been discontinued following the problems seen during clinical use of the similar drug rimonabant. |
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