SAGE-217|SAGE217|cas 1632051-40-1
DC Chemicals, Website:www.dcchemicals.com
Product Name: SAGE-217|CAS: 1632051-40-1|Cat No: DC10802|Other Names: SAGE-217; SAGE 217; SAGE217,1632051-40-1
SAGE-217 is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
Kinase assay demonstrates that SAGE-217 is a potent GABAA receptor agonist with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively. SAGE-217 is currently being studied in parallel phase 2 clinical trials for the treatment of postpartum depression (PPD) and major depressive disorder (MDD). SAGE-217 shows >30 μM inhibition in a cardiac panel of eight relevant cardiac ion channels. At 10 μM concentration of SAGE-217, only binding at the glycine (57%), sigma receptors (88%), and inhibition of the transient receptor potential vanilloid 1 (TRPV1, 95%) is noted.Acute administration of SAGE-217 (0.3 to 10 mg/kg, ip) effectively reduces pentylenetretazol (PTZ)-induced seizures in mice (MECplasma=85 nM) as well as produces a dose-dependent anticonvulsant effect in the mouse 6 Hz electrical stimulation model. In the rat lithium-pilocarpine model of status epilepticus (SE), SAGE-217 (0.3 to 5 mg, iv) abolishes both behavioral and electrographic seizure activity, even when administered 60 min after induction of SE. Additional PK studies of SAGE-217 in dog show low clearance (<10% of hepatic blood flow), resulting in excellent oral bioavailability (F=68%).
2018年5月18日星期五
AMPA/kainate antagonist-2
AMPA/kainate antagonist-2
DC Chemicals, Website:www.dcchemicals.com
Product Name: AMPA/kainate antagonist-2|CAS: 923271-87-8|Cat No: DC10801|Other Names:
A novel Non-competitive AMPA/kainate antagonist.
DC Chemicals, Website:www.dcchemicals.com
Product Name: AMPA/kainate antagonist-2|CAS: 923271-87-8|Cat No: DC10801|Other Names:
A novel Non-competitive AMPA/kainate antagonist.
AMPA/kainate antagonist-1
AMPA/kainate antagonist-1
DC Chemicals, Website:www.dcchemicals.com
Product Name: AMPA/kainate antagonist-1|CAS: 732277-05-3|Cat No: DC10800|Other Names:
A novel Non-competitive AMPA/kainate antagonist.
DC Chemicals, Website:www.dcchemicals.com
Product Name: AMPA/kainate antagonist-1|CAS: 732277-05-3|Cat No: DC10800|Other Names:
A novel Non-competitive AMPA/kainate antagonist.
D-Lin-MC3-DMA|for siRNA delivery|Supplier
D-Lin-MC3-DMA|for siRNA delivery|Supplier
DC Chemicals, Website:www.dcchemicals.com
Product Name: DLin-MC3-DMA|CAS: N/A|Cat No: DC10800|Other Names: D-Lin-MC3-DMA,DLinMC3DMA,D-Lin-MC-3-DMA,D-Lin-MC3-DMA
D-Lin-MC3-DMA(MC3) is the most potent cationic lipid that has been synthesized for Lipid nanoparticles (LNPs) to deliver the siRNA.
Technological advances in both siRNA (small interfering RNA) and whole genome sequencing have demonstrated great potential in translating genetic information into siRNA-based drugs to halt the synthesis of most disease-causing proteins. Despite its powerful promises as a drug, siRNA requires a sophisticated delivery vehicle because of its rapid degradation in the circulation, inefficient accumulation in target tissues and inability to cross cell membranes to access the cytoplasm where it functions. Lipid nanoparticle (LNP) containing ionizable amino lipids is the leading delivery technology for siRNA, with five products in clinical trials and more in the pipeline. Lipid nanoparticles (LNPs) formed by an ionizable cationic lipid (DLin-MC3-DMA), helper lipids (distearoylphosphatidylcholine, DSPC, and cholesterol), and a poly(ethylene glycol) (PEG) lipid have been identified as very promising delivery vectors of short interfering RNA (siRNA) in different clinical phases. DLin-MC3-DMA [14], which are 100-fold and 1000-fold more potent, respectively, in silencing of a hepatic gene (Factor VII) in comparison to the previous generation lipid DLin-DMA (1,2-dilinoleyloxy-N,N-dimethyl-3-aminopropane).The ED50 (median effective dose) for LNP containing DLin-MC3-DMA to silence Factor VII in mice and TTR in non-human primates was 0.005 mg/kg and 0.03 mg/kg, respectively. One of the key findings from these studies was the optimum lipid pKa value of 6.2–6.5 as a dominating factor in determining hepatic gene-silencing activity in vivo. DLin-MC3-DMA, having a pKa of 6.44, is currently the most active ionizable lipid being used in clinical trials.
DC Chemicals, Website:www.dcchemicals.com
Product Name: DLin-MC3-DMA|CAS: N/A|Cat No: DC10800|Other Names: D-Lin-MC3-DMA,DLinMC3DMA,D-Lin-MC-3-DMA,D-Lin-MC3-DMA
D-Lin-MC3-DMA(MC3) is the most potent cationic lipid that has been synthesized for Lipid nanoparticles (LNPs) to deliver the siRNA.
Technological advances in both siRNA (small interfering RNA) and whole genome sequencing have demonstrated great potential in translating genetic information into siRNA-based drugs to halt the synthesis of most disease-causing proteins. Despite its powerful promises as a drug, siRNA requires a sophisticated delivery vehicle because of its rapid degradation in the circulation, inefficient accumulation in target tissues and inability to cross cell membranes to access the cytoplasm where it functions. Lipid nanoparticle (LNP) containing ionizable amino lipids is the leading delivery technology for siRNA, with five products in clinical trials and more in the pipeline. Lipid nanoparticles (LNPs) formed by an ionizable cationic lipid (DLin-MC3-DMA), helper lipids (distearoylphosphatidylcholine, DSPC, and cholesterol), and a poly(ethylene glycol) (PEG) lipid have been identified as very promising delivery vectors of short interfering RNA (siRNA) in different clinical phases. DLin-MC3-DMA [14], which are 100-fold and 1000-fold more potent, respectively, in silencing of a hepatic gene (Factor VII) in comparison to the previous generation lipid DLin-DMA (1,2-dilinoleyloxy-N,N-dimethyl-3-aminopropane).The ED50 (median effective dose) for LNP containing DLin-MC3-DMA to silence Factor VII in mice and TTR in non-human primates was 0.005 mg/kg and 0.03 mg/kg, respectively. One of the key findings from these studies was the optimum lipid pKa value of 6.2–6.5 as a dominating factor in determining hepatic gene-silencing activity in vivo. DLin-MC3-DMA, having a pKa of 6.44, is currently the most active ionizable lipid being used in clinical trials.
SSR-240612|SSR240612|cas 464930-42-5
SSR-240612|SSR240612|cas 464930-42-5
DC Chemicals, Website:www.dcchemicals.com
Product Name: SSR-240612 HCl |CAS: 464930-42-5|Cat No: DC10799|Other Names: SSR-240612; SSR240612; SSR 240612
SSR-240612 is a bradykinin B1 receptor antagonist potentially for the treatment of chronic pain.
SSR240612 blocked tactile and cold allodynia at 3h (ID50=5.5and 7.1mg/kg,respectively) in glucose‐fed rats but had no effect in control rats. The antagonist (10mg/kg) had no effect on plasma glucose and insulin, insulin resistance (HOMA index) and aortic superoxide anion production in glucose-fed rats.
DC Chemicals, Website:www.dcchemicals.com
Product Name: SSR-240612 HCl |CAS: 464930-42-5|Cat No: DC10799|Other Names: SSR-240612; SSR240612; SSR 240612
SSR-240612 is a bradykinin B1 receptor antagonist potentially for the treatment of chronic pain.
SSR240612 blocked tactile and cold allodynia at 3h (ID50=5.5and 7.1mg/kg,respectively) in glucose‐fed rats but had no effect in control rats. The antagonist (10mg/kg) had no effect on plasma glucose and insulin, insulin resistance (HOMA index) and aortic superoxide anion production in glucose-fed rats.
p38-α MAPK-IN-1 |MAPK14 inhibitor|443913-15-3
p38-α MAPK-IN-1 |MAPK14 inhibitor|443913-15-3
DC Chemicals, Website:www.dcchemicals.com
Product Name: p38-α MAPK-IN-1|CAS: 443913-15-3|Cat No: DC10798|Other Names: MAPK14 inhibitor
p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.
DC Chemicals, Website:www.dcchemicals.com
Product Name: p38-α MAPK-IN-1|CAS: 443913-15-3|Cat No: DC10798|Other Names: MAPK14 inhibitor
p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay.
AB423|AB-423||Hepatitis B Virus Capsid Assembly inhibitor
AB423|AB-423||Hepatitis B Virus Capsid Assembly inhibitor
DC Chemicals, Website:www.dcchemicals.com
Product Name: AB423|CAS: 1572510-80-5|Cat No: DC10797|Other Names: AB423,AB-423,AB 423
AB-423 is the first-generation Hepatitis B Virus Capsid Assembly inhibitor, which was generally safe and well tolerated in Phase 1 healthy volunteer studies.
AB-423 is a potent, highly seletive inhibitor of HBV replication through a block of pgRNA encapsidation. AB-423 in combination with EVT has shown synergistic antiviral activity in vitro in primary human hepatocytes. Furthermore, AB-423 alone and in combination with entecavir has shown potent in vivo activity in a hydrodynamic injection (HDI) mouse model of HBV.The HBV capsid inhibitor AB-423 exhibits a dual mode of inhibition:inhibited encapsidation of pgRNA during ongoing infection; inhibited cccDNA synthesis presumably via inhibition of the capsid uncoating step.In vitro AB-423 showed: pan-genotypic activity; potent activity against HBV in combination with Nucs, IFN, and RNAi agents;no significant activity against unrelated viruses.
DC Chemicals, Website:www.dcchemicals.com
Product Name: AB423|CAS: 1572510-80-5|Cat No: DC10797|Other Names: AB423,AB-423,AB 423
AB-423 is the first-generation Hepatitis B Virus Capsid Assembly inhibitor, which was generally safe and well tolerated in Phase 1 healthy volunteer studies.
AB-423 is a potent, highly seletive inhibitor of HBV replication through a block of pgRNA encapsidation. AB-423 in combination with EVT has shown synergistic antiviral activity in vitro in primary human hepatocytes. Furthermore, AB-423 alone and in combination with entecavir has shown potent in vivo activity in a hydrodynamic injection (HDI) mouse model of HBV.The HBV capsid inhibitor AB-423 exhibits a dual mode of inhibition:inhibited encapsidation of pgRNA during ongoing infection; inhibited cccDNA synthesis presumably via inhibition of the capsid uncoating step.In vitro AB-423 showed: pan-genotypic activity; potent activity against HBV in combination with Nucs, IFN, and RNAi agents;no significant activity against unrelated viruses.
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