| CAT # |
Product Name |
Description |
| CPDD0995 |
Bardoxolone methyl;RTA 402;NSC 713200;TP155;CDDOMe |
The synthetic oleanane triterpenoid CDDO (Item No. 81035) is a Nrf2 activator that inhibits proliferation and induces differentiation and apoptosis in various cancer cells. |
| CPD100616 |
Emricasan |
Emricasan, also known as IDN 6556 and PF 03491390, is a first-in-class caspase inhibitor in clinical trials for the treatment of liver diseases. Emricasan (IDN-6556) decreases liver injury and fibrosis in a murine model of non-alcoholic steatohepatitis. IDN6556 facilitates marginal mass islet engraftment in a porcine islet autotransplant model. Oral IDN-6556 may lower aminotransferase activity in patients with chronic hepatitis C. Orally-administered PF-03491390 is retained in the liver for prolonged periods with low systemic exposure, exerting a hepatoprotective effect against alpha-fas-induced liver injury in a mouse model. |
| CPD100615 |
Q-VD-Oph |
QVD-OPH, also known as Quinoline-Val-Asp-Difluorophenoxymethylketone, is a broad spectrum caspase inhibitor with potent antiapoptotic properties. Q-VD-OPh prevents neonatal stroke in P7 rat: a role for gender. Q-VD-OPh has anti-leukemia effects and can interact with vitamin D analogs to increase HPK1 signaling in AML cells. Q-VD-OPh reduces trauma-induced apoptosis and improves the recovery of hind-limb function in rats after spinal cord injury |
| CPD100614 |
Z-DEVD-FMK |
Z-DEVD-fmk is a cell-permeable, irreversible inhibitor of caspase-3. Caspase-3 is a cysteinyl aspartate-specific protease which plays a central role in apoptosis. |
| CPD100613 |
Z-IETD-FMK |
MDK4982, also known as Z-IETD-FMK, is a potent, cell-permeable, irreversible inhibitor of caspase-8 and granzyme B., The Caspase-8 Inhibitor II controls the biological activity of Caspase-8. MDK4982 effectively inhibits influenza virus-induced apoptosis in HeLa cells. MDK4982 also inhibits granzyme B. MDK4982 has CAS#210344-98-2. |
| CPD100612 |
Z-VAD-FMK |
Z-VAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor. Z-VAD-FMK inhibits caspase processing and apoptosis induction in tumor cells in vitro (IC50 = 0.0015 - 5.8 mM). |
| CPD100611 |
Belnacasan |
Belnacasan, also known as VX-765, is designed to inhibit Caspase, which is an enzyme that controls the generation of two cytokines, IL-1b and IL-18. VX-765 has been shown to inhibit acute seizures in preclinical models. In addition, VX-765 has shown activity in preclinical models of chronic epilepsy. VX-765 had been dosed in over 100 patients in phase-I and phase-IIa clinical trials relating to other diseases, including a 28-day phase-IIa clinical trial in patients with psoriasis. It has completed the treatment phase of a phase-IIa clinical trial of VX-765 that enrolled approximately 75 patients with treatment-resistant epilepsy. The double-blind, randomized, placebo-controlled clinical trial was designed to evaluate the safety, tolerability and clinical activity of VX-765. |
| CPD100610 |
Maraviroc |
Maraviroc is an antiviral, potent, non-competitive CKR-5 receptor antagonist that inhibits binding of HIV viral coat protein gp120. Maraviroc inhibits MIP-1β-stimulated γ-S-GTP binding to HEK-293 cell membranes, indicating its ability to inhibit chemokine-dependent stimulation of GDP-GTP exchange at the CKR-5/G protein complex. Maraviroc also inhibits the downstream event of chemokine-induced intracellular calcium redistribution. |
| CPD100609 |
Resatorvid |
Resatorvid, also known as TAK-242, is a cell-permeable inhibitor of TLR4 signaling, blocking LPS-induced production of NO, TNF-α, IL-6, and IL-1β in macrophages with IC50 values of 1-11 nM. Resatorvid binds selectively to TLR4 and interferes with interactions between TLR4 and its adaptor molecules. Resatorvid provides neuroprotection in experimental traumatic brain injury: implication in the treatment of human brain injury |
| CPD100608 |
ASK1-Inhibitor-10 |
ASK1 Inhibitor 10 is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1). It is selective for ASK1 over ASK2 as well as MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, and B-RAF. It inhibits streptozotocin-induced increases in JNK and p38 phosphorylation in INS-1 pancreatic β cells in a concentration-dependent manner. |
| CPD100607 |
K811 |
K811 is an ASK1-specific inhibitor that prolongs survival in a mouse model of amyotrophic lateral sclerosis. K811 efficiently prevented cell proliferation in cell lines with high ASK1 expression and in HER2-overexpressing GC cells. Treatment with K811 reduced sizes of xenograft tumors by downregulating proliferation markers. |
| CPD100606 |
K812 |
K812 is an ASK1-specific inhibitor discovered to prolong survival in a mouse model of amyotrophic lateral sclerosis. |
| CPD100605 |
MSC-2032964A |
MSC 2032964A is a potent and selective ASK1 inhibitor (IC50 = 93 nM). It blocks LPS-induced ASK1 and p38 phosphorylation in cultured mouse astrocytes and suppresses neuroinflammation in a mouse EAE model. MSC 2032964A is orally bioavailable and brain penetrant. |
| CPD100604 |
Selonsertib |
Selonsertib, also known as GS-4997, is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. GS-4997 targets and binds to the catalytic kinase domain of ASK1 in an ATP-competitive manner, thereby preventing its phosphorylation and activation. GS-4997 prevents the production of inflammatory cytokines, down-regulates the expression of genes involved in fibrosis, suppresses excessive apoptosis and inhibits cellular proliferation. |
| CPD100603 |
MDK36122 |
MDK36122, also known as H-PGDS Inhibitor I, is a Prostaglandin D Synthase (hematopoietic-type) Inhibitor. MDK36122 has no code name, and has CAS#1033836-12-2. The last 5-digit was used for name for easy communication. MDK36122 selectively blocks HPGDS (IC50s = 0.7 and 32 nM in enzyme and cellular assays, respectively) with little activity against the related human enzymes L-PGDS, mPGES, COX-1, COX-2, and 5-LOX. |
| CPD100602 |
Tepoxalin |
Tepoxalin, also known as ORF-20485; RWJ-20485; is a 5-lipoxygenase inhibitor potentially for the treatment of asthma, osteoarthritis (OA). Tepoxalin has in vivo inhibitory activity against COX-1, COX-2, and 5-LOX in dogs at the current approved recommended dosage.Tepoxalin inhibits inflammation and microvascular dysfunction induced by abdominal irradiation in rats. Tepoxalin enhances the activity of an antioxidant, pyrrolidine dithiocarbamate, in attenuating tumor necrosis factor alpha-induced apoptosis in WEHI 164 cells. |
| CPD100601 |
Tenidap |
Tenidap, also known as CP-66248, is a COX/5-LOX inhibitor and cytokine-modulating anti-inflammatory drug candidate that was under development by Pfizer as a promising potential treatment for rheumatoid arthritis, but Pfizer halted development after marketing approval was rejected by the FDA in 1996 due to liver and kidney toxicity, which was attributed to metabolites of the drug with a thiophene moiety that caused oxidative damage. |
| CPD100600 |
PF-4191834 |
PF-4191834 is a novel, potent and selective non-redox 5-lipoxygenase inhibitor effective in inflammation and pain. PF-4191834 exhibits good potency in enzyme- and cell-based assays, as well as in a rat model of acute inflammation. Enzyme assay results indicate that PF-4191834 is a potent 5-LOX inhibitor, with an IC(50) = 229 +/- 20 nM. Furthermore, it demonstrated approximately 300-fold selectivity for 5-LOX over 12-LOX and 15-LOX and shows no activity toward the cyclooxygenase enzymes. In addition, PF-4191834 inhibits 5-LOX in human blood cells, with an IC(80) = 370 +/- 20 nM. |
| CPD100599 |
MK-886 |
MK-886, also known as L 663536, is a leukotriene antagonist. It may perform this by blocking the 5-lipoxygenase activating protein (FLAP), thus inhibiting 5-lipoxygenase (5-LOX), and may help in treating atherosclerosis. MK-886 inhibits cyclooxygenase-1 activity and suppresses platelet aggregation. MK-886 induces changes in cell cycle and increases apoptosis after photodynamic therapy with hypericin. MK-886 enhances tumour necrosis factor-alpha-induced differentiation and apoptosis. |
| CPD100598 |
L-691816 |
L 691816 is a potent inhibitor of the 5-LO reaction both in vitro and in a range of in vivo models. |
| CPD100597 |
CMI-977 |
CMI-977, also know as LPD-977 and MLN-977, is a potent 5-lipoxygenase inhibitor that intervenes in the production of leukotrienes and is presently being developed for the treatment of chronic asthma. CMI-977 inhibits the 5-lipoxygenase (5-LO) cellular inflammation pathway to block the generation of leukotrienes, which play a key role in triggering bronchial asthma. |
| CPD100596 |
CJ-13610 |
CJ-13610 is an orally active inhibitor of 5-lipoxygenase (5-LO) . CJ-13610 inhibits the biosynthesis of leukotriene B4 and regulates the IL-6 mRNA expression in macrophages. It is efficacious in preclinical models of pain. |
| CPD100595 |
BRP-7 |
BRP-7 is a 5-LO activating protein (FLAP) inhibitor. |
| CPD100594 |
TT15 |
TT15 is an agonist of the GLP-1R. |
| CPD100593 |
VU0453379 |
VU0453379 is a CNS-penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM) |
| CPD100592 |
PF-06882961 |
PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor (GLP-1R). |
| CPD100591 |
PF-06372222 |
PF-06372222 is a small-molecule negative allosteric modulator (NAM) of glucagon receptor (GCGR). Antagonists of GCGR may be helpful in treating type 2 diabetes mellitus because they regulate plasma glucose levels by decreasing or slowing hepatic glucose production by signaling in the liver, intestinal smooth muscle, kidney, brain, and adipose tissue. PF-06372222 is also an antagonist for glucagon-like peptide-1 receptor GLP-1R, which inhibits glucagon secretion and glucose-dependent insulin secretion and may also play a role in hormonal release leading to acute and chronic stress and anxiety. By negatively modulating GLP-1R, PF-06372222 could treat type 2 diabetes mellitus and stress and anxiety. |
| CPD100590 |
NNC0640 |
NNC0640 is a negative allosteric modulator of glucagon-like peptide-1 receptor (GLP-1R). |
| CPD100589 |
HTL26119 |
HTL26119 is a novel allosteric antagonist of the glucagon-like peptide-1 receptor (GLP-1R). |
| CPD100587 |
Phlorizin |
Phlorizin, also referred to as phloridzin, is a glucoside of phloretin, a dihydrochalcone, a family of bicyclic flavonoids, which in turn is a subgroup in the diverse phenylpropanoid synthesis pathway in plants. Phlorizin is a competitive inhibitor of SGLT1 and SGLT2 because it competes with D-glucose for binding to the carrier; this reduces renal glucose transport, lowering the amount of glucose in the blood. Phlorizin was studied as a potential pharmaceutical treatment for type 2 diabetes, but has since been superseded by more selective and more promising synthetic analogs, such as canagliflozin and dapagliflozin. |
| CPD0045 |
Ipragliflozin |
Ipragliflozin, also known as ASP1941, is a potent and selective SGLT2 inhibitor for treatment of type 2 diabetes. Ipragliflozin treatment improved glycaemic control when added to metformin therapy and may be associated with weight loss and reductions in blood pressure compared to placebo. Ipragliflozin improves not only hyperglycemia but also diabetes/obesity-associated metabolic abnormalities in type 2 diabetic mice. It was approved for use in Japan in 2014 |
| CPD100585 |
Tofogliflozin |
Tofogliflozin, also known as CSG 452, is a potent and high selective SGLT2 inhibitor under development the treatment of diabetes mellitus. Tofogliflozin improves glycaemic control and lowers body weight in patients with type 2 diabetes mellitus. Tofogliflozin dose-dependently suppressed glucose entry into tubular cells. High glucose exposure (30?mM) for 4 and 24?h significantly increased oxidative stress generation in tubular cells, which were suppressed by the treatment of tofogliflozin or an antioxidant N-acetylcysteine (NAC). |
| CPD100583 |
Empagliflozin |
Empagliflozin, also known as BI10773 (trade name Jardiance), is drug approved for the treatment of type 2 diabetes in adults in 2014. It was developed by Boehringer Ingelheim and Eli Lilly and Company. Empagliflozin is an inhibitor of the sodium glucose co-transporter-2 (SGLT-2), and causes sugar in the blood to be absorbed by the kidneys and eliminated in urine. Empagliflozin is an inhibitor of the sodium glucose co-transporter-2 (SGLT-2), which is found almost exclusively in the proximal tubules of nephronic components in the kidneys. SGLT-2 accounts for about 90 percent of glucose reabsorption into the blood. |
| CPD100582 |
Canagliflozin |
Canagliflozin (INN, trade name Invokana) is a drug for the treatment of type 2 diabetes. It was developed by Mitsubishi Tanabe Pharma and is marketed under license by Janssen, a division of Johnson & Johnson. Canagliflozin is an inhibitor of subtype 2 sodium-glucose transport protein (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine. In March 2013, canagliflozin became the first SGLT2 inhibitor to be approved in the United States |
| CPD0003 |
Dapagliflozin |
Dapagliflozin, also known as BMS-512148, is a drug used to treat type 2 diabetes approved in 2012 by FDA. Dapagliflozin inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2) which are responsible for at least 90% of the glucose reabsorption in the kidney. Blocking this transporter mechanism causes blood glucose to be eliminated through the urine. In clinical trials, dapagliflozin lowered HbA1c by 0.6 versus placebo percentage points when added to metformin |
| CPD9470 |
Obeticholic-Acid |
Obeticholic Acid (INT747; 6-ECDCA) is a novel derivative of cholic acid which acts as a potent and selective FXR agonist displaying anticholeretic activity in an in vivo rat model of cholestasis. It inhibits vascular smooth muscle cell inflammation and migration as well as promotes adipocyte differentiation and regulates adipose cell function in vivo. |
| CPD100579 |
fexaramine |
Fexaramine is an agonist of the farnesoid X receptor (FXR), which is a bile acid-activated nuclear receptor that controls bile-acid synthesis, conjugation and transport, as well as lipid metabolism through actions in the liver and intestine. Fexaramine has 100-fold greater affinity for FXR than natural compounds and described the genomic targets and binding site on FXR. When administered orally to mice, fexaramine produced selective actions through FXR receptors in the intestines. |
| CPD100577 |
Lithocholic-acid |
Levallorphan, also known as levallorphan tartate (USAN), is an opioid modulator of the morphinan family used as an opioid analgesic and opioid antagonist/antidote. It acts as an antagonist of the μ-opioid receptor (MOR) and as an agonist of the κ-opioid receptor (KOR), and as a result, blocks the effects of stronger agents with greater intrinsic activity such as morphine whilst simultaneously producing analgesia. As an agonist of the KOR, levallorphan can produce severe mental reactions at sufficient doses including hallucinations, dissociation, and other psychotomimetic effects, dysphoria, anxiety, confusion, dizziness, disorientation, derealization, feelings of drunkenness, and bizarre, unusual, or disturbing dreams. (Source: https://en.wikipedia.org/wiki/Levallorphan). |
| CPD100575 |
Turofexorate-Isopropyl |
Turofexorate isopropyl, also known as WAY-362450 and XL335, is a highly potent, selective, and orally active agonist of the farnesoid X receptor (FXR) (EC(50) = 4 nM, Eff = 149%), which attenuates liver inflammation and fibrosis in murine model of non-alcoholic steatohepatitis |
| CPD100574 |
GW4064 |
GW4064是一种farnesoid X receptor (FXR)激动剂，CV1细胞系中EC50为65 nM。浓度达到1 μM时，对其他核受体没有活性。 |
| CPD100569 |
PF-05231023 |
PF-05231023 is a long-acting FGF21 mimetic. PF-05231023 decreases body weight and improves lipid profile in non-human primates and in type 2 diabetic subjects. |
| CPD100567 |
GW501516 |
GW501516 is a synthetic PPARδ-specific agonist that displays high affinity for PPARδ (Ki=1.1 nM) with > 1000 fold selectivity over PPARα and PPARγ. |
| CPD100566 |
GFT505 |
Elafibranor, also known as GFT-505, is a dual PPARα/δ agonist. Elafibranoris currently being studied for the treatment of cardiometabolic diseases including diabetes, insulin resistance, dyslipidemia, and non-alcoholic fatty liver disease (NAFLD). |
| CPD100565 |
Bavachinina |
Bavachinina is a novel natural pan-PPAR agonist from the fruit of the traditional Chinese glucose-lowering herb malaytea scurfpea. It shows stronger activities with PPAR-γ than with PPAR-α and PPAR-β/δ (EC50?=?0.74 μmol/l, 4.00 μmol/l and 8.07 μmol/l in 293T cells, respectively). |
| CPD100564 |
Troglitazone |
Troglitazone, also known as CI991, is a potent PPAR agonist. Troglitazone is an antidiabetic and anti-inflammatory drug, and a member of the drug class of the thiazolidinediones. It was prescribed for patients with diabetes mellitus type 2 in Japan Troglitazone, like the other thiazolidinediones (pioglitazone and rosiglitazone), works by activating peroxisome proliferator-activated receptors (PPARs). Troglitazone is a ligand to both PPARα and – more strongly – PPARγ |
| CPD100563 |
Glabridin |
Glabridin, one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory. |
| CPD100561 |
Pseudoginsenoside-F11 |
Pseudoginsenoside F11, a natural product found in American ginseng but not in Asian ginseng, is a novel partial PPARγ agonist. |
| CPD100560 |
Bezafibrate |
Bezafibrate is an agonist of peroxisome proliferator-activated receptor alpha (PPARalpha) with antilipidemic activity. Bezafibrate is a fibrate drug used for the treatment of hyperlipidaemia. Bezafibrate decreases triglyceride levels, increases high density lipoprotein cholesterol levels, and decreases total and low density lipoprotein cholesterol levels. It is commonly marketed as Bezalip |
| CPD100559 |
GW0742 |
GW0742, also known as GW610742 and GW0742X is a PPARδ/β agonist. GW0742 Induces Early Neuronal Maturation of Cortical Post-Mitotic Neurons. GW0742 prevents hypertension, vascular inflammatory and oxidative status, and endothelial dysfunction in diet-induced obesity. GW0742 has direct protective effects on right heart hypertrophy.GW0742 may enhance lipid metabolism in heart both in vivo and in vitro. |
| CPD100558 |
Pioglitazone |
Pioglitazone Hydrochloride is a thiazolidinedione compound described to produce antiinflammatory and antiarteriosclerotic effects. Pioglitazone is demonstrated to prevent L-NAME-induced coronary inflammation and arteriosclerosis and to suppress increased TNF-α mRNA produced by aspirin-induced gastric mucosal injury. Pioglitazone Hydrochloride is an activator of PPAR γ |
