Setmelanotide |cas 920014-72-8
DC Chemicals, Website: www.dcchemicals.com
Product Name: Setmelanotide|Cas Number: 920014-72-8| Catalog Number: DC10323|Other Nmaes: RM-493; BIM-22493; IRC-022493)
Setmelanotide (RM-493;BIM-22493;IRC-022493) is a melanocortin 4 receptor (MC4R) agonist with an EC50 of 0.27 nM for human MC4R.
Melanocortin receptor agonists act in the brain to regulate food intake and body weight and, independently of these actions, affect insulin sensitivity. Setmelanotide exhibits agonist activity to human and rat MC4R with Kis of 2.1 and 2.7 nM and EC50s of 0.27 and 0.28 nM, respectively[1].Inhibition of refeeding after an overnight fast by BIM-22493 is dependent on functional MC4R, and does not require MC3R. BIM-22493 acutely improves glucose homeostasis. Lepob/Lepob mice treated with BIM-22493 exhibits significantly improved glucose clearance when compared to controls. Chronic BIM-22493 treatment was associated with significantly lower levels of serum insulin, glucose and HOMA-IR values, suggesting an improvement in insulin sensitivity[1]. Treatment with setmelanotide results in transient decreases in food intake (35%), with persistent weight loss over 8 weeks of treatment (13.5%) in a diet-induced obese nonhuman primate model[2].
2017年11月29日星期三
Saroglitazar |cas 495399-09-2
Saroglitazar |cas 495399-09-2
DC Chemicals, Website: www.dcchemicals.com
Product Name: Saroglitazar|Cas Number: 495399-09-2| Catalog Number: DC10322
Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
In db/db mice, 12-day treatment with Saroglitazar (0.01-3 mg/kg per day, orally) causes dose-dependent reductions in serum triglycerides (TG), free fatty acids (FFA), and glucose. The ED50 for these effects is found to be 0.05, 0.19, and 0.19 mg/kg, respectively with highly significant (91%) reduction in serum insulin and AUC-glucose following oral glucose administration (59%) at 1 mg/kg dose. A 90-day repeated dose comparative study in Wistar rats and marmosets confirms efficacy (TG lowering) potential of Saroglitazar and has indicated low risk of PPAR-associated side effects in humans. Based on efficacy and safety profile, Saroglitazar appears to have good potential as novel[1].
DC Chemicals, Website: www.dcchemicals.com
Product Name: Saroglitazar|Cas Number: 495399-09-2| Catalog Number: DC10322
Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
In db/db mice, 12-day treatment with Saroglitazar (0.01-3 mg/kg per day, orally) causes dose-dependent reductions in serum triglycerides (TG), free fatty acids (FFA), and glucose. The ED50 for these effects is found to be 0.05, 0.19, and 0.19 mg/kg, respectively with highly significant (91%) reduction in serum insulin and AUC-glucose following oral glucose administration (59%) at 1 mg/kg dose. A 90-day repeated dose comparative study in Wistar rats and marmosets confirms efficacy (TG lowering) potential of Saroglitazar and has indicated low risk of PPAR-associated side effects in humans. Based on efficacy and safety profile, Saroglitazar appears to have good potential as novel[1].
Sermorelin |cas 86168-78-7
Sermorelin |cas 86168-78-7
DC Chemicals, Website: www.dcchemicals.com
Product Name: Sermorelin|Cas Number: 86168-78-7| Catalog Number: DC10321|Other Nmaes: GHRH (1-29); Growth Hormone Releasing Factor Fragment 1-29 amide human
Sermorelin is a Growth Hormone Releasing Hormone (GHRH) produced by the brain that stimulates the production and release of Growth Hormone (GH).
DC Chemicals, Website: www.dcchemicals.com
Product Name: Sermorelin|Cas Number: 86168-78-7| Catalog Number: DC10321|Other Nmaes: GHRH (1-29); Growth Hormone Releasing Factor Fragment 1-29 amide human
Sermorelin is a Growth Hormone Releasing Hormone (GHRH) produced by the brain that stimulates the production and release of Growth Hormone (GH).
Saroglitazar (Magnesium) |cas 1639792-20-3
Saroglitazar (Magnesium) |cas 1639792-20-3
DC Chemicals, Website: www.dcchemicals.com
Product Name: Saroglitazar (Magnesium)|Cas Number: 1639792-20-3| Catalog Number: DC10320
Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
In db/db mice, 12-day treatment with Saroglitazar (0.01-3 mg/kg per day, orally) causes dose-dependent reductions in serum triglycerides (TG), free fatty acids (FFA), and glucose. The ED50 for these effects is found to be 0.05, 0.19, and 0.19 mg/kg, respectively with highly significant (91%) reduction in serum insulin and AUC-glucose following oral glucose administration (59%) at 1 mg/kg dose. A 90-day repeated dose comparative study in Wistar rats and marmosets confirms efficacy (TG lowering) potential of Saroglitazar and has indicated low risk of PPAR-associated side effects in humans. Based on efficacy and safety profile, Saroglitazar appears to have good potential as novel therapeutic agent for treatment of dyslipidemia and diabetes[1].
DC Chemicals, Website: www.dcchemicals.com
Product Name: Saroglitazar (Magnesium)|Cas Number: 1639792-20-3| Catalog Number: DC10320
Saroglitazar magnesium is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively.
In db/db mice, 12-day treatment with Saroglitazar (0.01-3 mg/kg per day, orally) causes dose-dependent reductions in serum triglycerides (TG), free fatty acids (FFA), and glucose. The ED50 for these effects is found to be 0.05, 0.19, and 0.19 mg/kg, respectively with highly significant (91%) reduction in serum insulin and AUC-glucose following oral glucose administration (59%) at 1 mg/kg dose. A 90-day repeated dose comparative study in Wistar rats and marmosets confirms efficacy (TG lowering) potential of Saroglitazar and has indicated low risk of PPAR-associated side effects in humans. Based on efficacy and safety profile, Saroglitazar appears to have good potential as novel therapeutic agent for treatment of dyslipidemia and diabetes[1].
GLP-17-3|cas 107444-51-9
GLP-17-3|cas 107444-51-9
DC Chemicals, Website: www.dcchemicals.com
Product Name: GLP-17-3|Cas Number: 107444-51-9| Catalog Number: DC10319|Other Nmaes: Human GLP-1-(7-36)-amide; Insulinotropin; MKC253; Glucagon-like Peptide 1 (7-36) amide; GLP-1 (7-36) amide
GLP-1(7-36) is a major intestinal hormone that stimulates glucose-induced insulin secretion from β cells.
DC Chemicals, Website: www.dcchemicals.com
Product Name: GLP-17-3|Cas Number: 107444-51-9| Catalog Number: DC10319|Other Nmaes: Human GLP-1-(7-36)-amide; Insulinotropin; MKC253; Glucagon-like Peptide 1 (7-36) amide; GLP-1 (7-36) amide
GLP-1(7-36) is a major intestinal hormone that stimulates glucose-induced insulin secretion from β cells.
Acelarin|cas 840506-29-8
Acelarin|cas 840506-29-8
DC Chemicals, Website: www.dcchemicals.com
Product Name: Acelarin|Cas Number: 840506-29-8| Catalog Number: DC10318|Other Nmaes: NUC-1031; NUC1031; NUC 1031
Acelarin (NUC-1031) is a ProTide transformation and enhancement of the widely-used nucleoside analogue, gemcitabine.
Gemcitabine is a nucleoside analogue commonly used in cancer therapy but with limited efficacy due to a high susceptibility to cancer cell resistance. The addition of a phosphoramidate motif to the gemcitabine can protect it against many of the key cancer resistance mechanisms. A series of gemcitabine phosphoramidate prodrugs are synthesized and screened for cytostatic activity in a range of different tumor cell lines. Among the synthesized compounds, NUC-1031 is shown to be potent in vitro.The ProTide demonstrates a significant reduction in tumor size against pancreatic xenograft models compared with the gemcitabine treated group, and less adverse effects on body weight, indicating a better safety profile. Data strongly suggests that the ProTides are not reliant on kinases or nucleoside transporters to exert their activity inside tumor cells and remain stable in the presence of deaminases. The ProTide NUC-1031 is currently advancing through phase I/II clinical studies and has already generated strong pharmacokinetic data that confirm significantly higher intracellular levels of gemcitabine triphosphate, together with promising early efficacy signals and a favorable safety profile. The phosphoramidate chemistry is potentially a great source of new and very effective anticancer agents, bringing a considerable array of advanced treatments specifically designed to overcome cancer resistance mechanisms that will benefit a greater proportion of patients[1].
DC Chemicals, Website: www.dcchemicals.com
Product Name: Acelarin|Cas Number: 840506-29-8| Catalog Number: DC10318|Other Nmaes: NUC-1031; NUC1031; NUC 1031
Acelarin (NUC-1031) is a ProTide transformation and enhancement of the widely-used nucleoside analogue, gemcitabine.
Gemcitabine is a nucleoside analogue commonly used in cancer therapy but with limited efficacy due to a high susceptibility to cancer cell resistance. The addition of a phosphoramidate motif to the gemcitabine can protect it against many of the key cancer resistance mechanisms. A series of gemcitabine phosphoramidate prodrugs are synthesized and screened for cytostatic activity in a range of different tumor cell lines. Among the synthesized compounds, NUC-1031 is shown to be potent in vitro.The ProTide demonstrates a significant reduction in tumor size against pancreatic xenograft models compared with the gemcitabine treated group, and less adverse effects on body weight, indicating a better safety profile. Data strongly suggests that the ProTides are not reliant on kinases or nucleoside transporters to exert their activity inside tumor cells and remain stable in the presence of deaminases. The ProTide NUC-1031 is currently advancing through phase I/II clinical studies and has already generated strong pharmacokinetic data that confirm significantly higher intracellular levels of gemcitabine triphosphate, together with promising early efficacy signals and a favorable safety profile. The phosphoramidate chemistry is potentially a great source of new and very effective anticancer agents, bringing a considerable array of advanced treatments specifically designed to overcome cancer resistance mechanisms that will benefit a greater proportion of patients[1].
LF3 |cas 664969-54-4
LF3 |cas 664969-54-4
DC Chemicals, Website: www.dcchemicals.com
Product Name: LF3|Cas Number: 664969-54-4| Catalog Number: DC10317|Other Nmaes: LF-3; LF 3
LF3 is an antagonist of the β-Catenin/TCF4 interaction with antitumor activity; has an IC50 of 1.65 μM.
LF3 inhibits Wnt/β-catenin signals in cells with exogenous reporters and in colon cancer cells with endogenously high Wnt activity. LF3 also suppresses features of cancer cells related to Wnt signaling, including high cell motility, cell-cycle progression, and the overexpression of Wnt target genes. However, LF3 does not cause cell death or interfere with cadherin-mediated cell-cell adhesion. Remarkably, the self-renewal capacity of cancer stem cells is blocked by LF3 in concentration-dependent manners[1].LF3 reduces tumor growth and induces differentiation in a mouse xenograft model of colon cancer. Tumor growth is significantly reduced when mice with GFPhigh cells are treated with LF3 at 50 mg/kg. LF3 treatment does not disturb the normal histology of the gut of mice[1].
DC Chemicals, Website: www.dcchemicals.com
Product Name: LF3|Cas Number: 664969-54-4| Catalog Number: DC10317|Other Nmaes: LF-3; LF 3
LF3 is an antagonist of the β-Catenin/TCF4 interaction with antitumor activity; has an IC50 of 1.65 μM.
LF3 inhibits Wnt/β-catenin signals in cells with exogenous reporters and in colon cancer cells with endogenously high Wnt activity. LF3 also suppresses features of cancer cells related to Wnt signaling, including high cell motility, cell-cycle progression, and the overexpression of Wnt target genes. However, LF3 does not cause cell death or interfere with cadherin-mediated cell-cell adhesion. Remarkably, the self-renewal capacity of cancer stem cells is blocked by LF3 in concentration-dependent manners[1].LF3 reduces tumor growth and induces differentiation in a mouse xenograft model of colon cancer. Tumor growth is significantly reduced when mice with GFPhigh cells are treated with LF3 at 50 mg/kg. LF3 treatment does not disturb the normal histology of the gut of mice[1].
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