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19

抑制剂 & 化合物

2

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Cat. No. Product Name Target Signaling Pathways
T6048 Dalcetrapib

JTT-705,达塞曲匹,RO4607381

CETP Metabolism
Dalcetrapib (RO4607381) 是rhCETP 抑制剂(IC50:0.2 μM),具有增加血浆中HDL 胆固醇含量的作用。
T2499 Torcetrapib

CP-529414,托彻普

CETP Metabolism
是胆固醇酯转移蛋白 (CETP) 选择性抑制剂。根据人血浆的抑制曲线,Torcetrapib (CP-529414) 对CETP 的最有效浓度为 37 nM。
T15549 Icosabutate

Others Others
Icosabutate is a structurally engineered and orally active ω-3 polyunsaturated fatty acid. Icosabutate is well tolerated, and efficacious in lowering non-high-density lipoprotein cholesterol (non-HDL-C) levels in persistent hypertriglyceridemia.
T1928 Anacetrapib

安塞曲匹,MK-0859

CETP Metabolism
Anacetrapib (MK-0859) 是 CETP 的抑制剂,能够抑制 rhCETP (IC50:7.9±2.5 nM) 和 C13S CETP 突变型 (IC50:11.8±1.9 nM) 的活性。
T6262 Evacetrapib

LY2484595

CETP Metabolism
Evacetrapib (LY2484595) 是 CETP 的选择性抑制剂,在人血浆中,抑制人重组 CETP 蛋白 (IC50:5.5 nM) 和 CETP (IC50:36 nM) 活性。
T1415 Gemfibrozil

吉非罗齐,CI-719,Jezil,Decrelip,Lopid

P450; Adrenergic Receptor; PPAR DNA Damage/DNA Repair; GPCR/G Protein; Metabolism; Neuroscience
Gemfibrozil (CI-719) 是一种PPAR-α激活剂,可作为降脂药。它也是P450非选择性抑制剂,对 CYP2C9、2C19、2C8 和 1A2 的Ki 值分别为 5.8、24、69 和 82 μM。
T30588 Brl 26314

Brl-26314,Brl26314

Brl 26314 can elevate HDL-cholesterol in rats.
T10771 CETP-IN-3

Others Others
CETP-IN-3 is an inhibitor of the plasma glycoprotein cholesterol ester transfer protein (CETP), elevating HDL-C through inhibition of CETP.
T69408 GW590735 sodium

GW590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ. GW590735 significantly increased HDL cholesterol, decreased LDL and VLDL cholesterol, and significantly reduced triglycerides. Maximal increases in HDL cholesterol were 37%, 53%, and 84% with fenofibrate, torcetrapib, and GW590735, respectively.
T11386 Gemcabene calcium

PD-72953 calcium

Others Others
Gemcabene calcium , a first-in-class lipid-lowering agent, lowers low-density lipoprotein cholesterol (LDL-C), decreases triglycerides, and raises high-density lipoprotein cholesterol (HDL-C) andexerting anti-inflammatory activity, lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP).
T68504 Obicetrapib calcium

Obicetrapib calcium is a cholesteryl ester transfer protein (CETP) inhibitor. CETP inhibitors substantially increase the concentration of high-density lipoprotein cholesterol (HDL-C), which may have a possible beneficial effect for cardiovascular disease risk reduction.
T68503 Obicetrapib potassium

Obicetrapib potassium is a cholesteryl ester transfer protein (CETP) inhibitor. CETP inhibitors substantially increase the concentration of high-density lipoprotein cholesterol (HDL-C), which may have a possible beneficial effect for cardiovascular disease risk reduction.
T68505 Obicetrapib sodium

Obicetrapib sodium is a cholesteryl ester transfer protein (CETP) inhibitor. CETP inhibitors substantially increase the concentration of high-density lipoprotein cholesterol (HDL-C), which may have a possible beneficial effect for cardiovascular disease risk reduction.
T70661 Azalanstat mesylate

Azalanstat mesylate is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat mesylate has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. When administered orally to hamsters fed regular chow, RS-21607 (50 mg/kg/day) lowered serum cholesterol in a dose-dependent manner (ED50 = 62 mg/kg) in a period of 1 week. It preferentially...
T68695 (R)-Bambuterol

Bambuterol is a prodrug of β2-agonist commonly used for the treatment of asthma and chronic obstructive pulmonary disease (COPD) with the advantage of once daily dosing and favorable side effect profile. Administration of a single-dose of R-bambuterol resulted in dose-dependent reductions in the levels of plasma LDL-C, high-density lipoprotein cholesterol (HDL-C), total cholesterol (TC), apolipoprotein B (ApoB) and apolipoprotein A1 (ApoA1) at Tmax. R-bambuterol can lower the plasma levels of LD...
T70660 Azalanstat HCl

Azalanstat HCl is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat HCl has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. When administered orally to hamsters fed regular chow, RS-21607 (50 mg/kg/day) lowered serum cholesterol in a dose-dependent manner (ED50 = 62 mg/kg) in a period of 1 week. It preferentially lowered l...
T35813 CAY10592

Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism. Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys. CAY10592 is a full PPARδ agonist (EC50 = 30 nM) ...
T83757 RG33 TFA

RG33是一种33个氨基酸的合成肽,与apolipoprotein A1 (ApoA1)的C-末端域中两个Y类螺旋的209-219和220-241氨基酸相对应。它能溶解含有1,2-dimyristoyl-sn-glycero-3-PC (DMPC)的多层囊泡(MLVs),形成重组HDL。与脂质结合的RG33在J774巨噬细胞中诱导胆固醇外流。RG33 (12 mg/kg)可降低胰岛素抵抗性小鼠的血糖水平。
T35632 Pinolenic Acid

Pinolenic acid is a polyunsaturated fatty acid found in Korean pine (Pinus orientalis) and maritime pine (Pinus pinaster) seed oils. Both oils have been found to have lipid-lowering properties. A diet containing maritime pine seed oil (MPSO) lowered HDL and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to diminish cholesterol efflux in vitro.[1] Korean pine seed oil supplements may help in obesity by reduction of appetite. People taking this oil had an increase in the sa...

化合物

Dalcetrapib
Cat.No: T6048
Synonym: JTT-705,达塞曲匹,RO4607381
Target: CETP
Torcetrapib
Cat.No: T2499
Synonym: CP-529414,托彻普
Target: CETP
Icosabutate
Cat.No: T15549
Synonym:
Target: Others
Anacetrapib
Cat.No: T1928
Synonym: 安塞曲匹,MK-0859
Target: CETP
Evacetrapib
Cat.No: T6262
Synonym: LY2484595
Target: CETP
Gemfibrozil
Cat.No: T1415
Synonym: 吉非罗齐,CI-719,Jezil,Decrelip,Lopid
Target: P450, Adrenergic Receptor, PPAR
Brl 26314
Cat.No: T30588
Synonym: Brl-26314,Brl26314
Target:
CETP-IN-3
Cat.No: T10771
Synonym:
Target: Others
GW590735 sodium
Cat.No: T69408
Synonym:
Target:
Gemcabene calcium
Cat.No: T11386
Synonym: PD-72953 calcium
Target: Others
Obicetrapib calcium
Cat.No: T68504
Synonym:
Target:
Obicetrapib potassium
Cat.No: T68503
Synonym:
Target:
Obicetrapib sodium
Cat.No: T68505
Synonym:
Target:
Azalanstat mesylate
Cat.No: T70661
Synonym:
Target:
(R)-Bambuterol
Cat.No: T68695
Synonym:
Target:
Azalanstat HCl
Cat.No: T70660
Synonym:
Target:
CAY10592
Cat.No: T35813
Synonym:
Target:
RG33 TFA
Cat.No: T83757
Synonym:
Target:
Pinolenic Acid
Cat.No: T35632
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T3771 Methyl protodioscin

山药,Smilax saponin B,NSC-698790

Apoptosis Apoptosis
Methyl protodioscin (Smilax saponin B) 是一种甾二糖苷,能诱导细胞周期阻滞,具有抗肿瘤活性。
TN3397 Alpinumisoflavone

ERK; LDL; NF-κB; MEK; MAPK; Antifection MAPK; Metabolism; Microbiology/Virology; NF-κB
Alpinumisoflavone has atheroprotective effects, may result from their ability to upregulate mechanisms promoting HDL-cholesterol and bile acid formation, it is endowed with estrogenic properties accounting, at least in part, for E. lysistemon effects. Alp

天然产物

Methyl protodioscin
Cat.No: T3771
Synonym: 山药,Smilax saponin B,NSC-698790
Target: Apoptosis
Alpinumisoflavone
Cat.No: TN3397
Synonym:
Target: ERK, LDL, NF-κB, MEK, MAPK, Antifection
TargetMol Loading
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