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PAMPA

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By Targets:	5-HT Receptor (1) Cholinesterase (ChE) (1) CXCR (1) E1/E2/E3 Enzyme (1) Epigenetic Reader Domain (1) FAAH (2) Fluorescent Dye (1) HIV (1) ICMT (2) MAGL (2) mTOR (1) NO Synthase (1) PI3K (1) PROTACs (1) Sodium Channel (1) Sodium Phosphate Cotransporter (1)
By Research Areas:	Cancer (6) Infection (1) Inflammation/Immunology (1) Metabolic Disease (1) Neurological Disease (3)

抑制剂 & 激动剂

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Cat. No.	Product Name	Target	Research Area	Chemical Structure

HY-146341

FAAH-IN-5	FAAH MAGL	Neurological Disease
FAAH-IN-5 (Compound 7) 是一种相对选择性的、不可逆的脂肪酸酰胺水解酶 (FAAH) 抑制剂，IC₅₀ 值为 10.5 nM。FAAH-IN-5 具有低 PAMPA (平行人工膜渗透性试验) 透过性。

HY-146342

FAAH/MAGL-IN-3	FAAH MAGL	Neurological Disease
FAAH/MAGL-IN-3 (Compound 10) 是一种不可逆的脂肪酸酰胺水解酶 (FAAH) 和单酰基甘油脂酶 (MAGL) 双重抑制剂，对 FAAH 和 MAGL 的 IC₅₀ 分别为 179 和 759 nM。FAAH/MAGL-IN-3 具有很低的 PAMPA (平行人工膜渗透性试验) 透过性。

HY-D2060

ATTO 740	Fluorescent Dye	Others
ATTO 740 是一种近红外染料 (Ex/Em：740/764 nm)。ATTO 740 可和 Cetuximab 抗体 (HY-P9905) 偶联。

HY-144285

CXCR4 antagonist 4	CXCR HIV	Inflammation/Immunology
CXCR4 antagonist 4 是一种有效，具有口服活性的 CXCR4 拮抗剂 (IC₅₀=24 nM)，可降低 CYP 2D6 的活性，提高 PAMPA 的通透性，有效抑制人类免疫缺陷病毒的进入 (IC₅₀=7 nM).

HY-117776

CAY10677	ICMT	Cancer
CAY10677 (compound 15) 是强效的 ICMT 抑制剂，可抑制癌细胞增殖。CAY10677 具有良好 PAMPA 渗透性。

HY-149729

ICMT-IN-53	ICMT	Cancer
ICMT-IN-53 (compound 12) 是一种 ICMT 抑制剂 (IC₅₀=0.96 μM)，具有 PAMPA 渗透性和抗增殖活性。ICMT-IN-53 抑制 MDA-MB-231 和 PC3 的增殖，IC50s 分别为 5.14 μM 和 5.88 μM。

HY-168241

Flucopride	Cholinesterase (ChE) 5-HT Receptor	Infection
Flucopride (Compound 4a) 是一种 AChE 抑制剂 (IC₅₀: 24 nM)，也是一种部分 5-HT₄R 激动剂 (对 (h)5-HT4R 的 Ki 为 9.6 nM)。Flucopride 可促进瞬时表达 (h)5-HT₄R 的 COS-7 细胞中 APP 的非淀粉样变性加工 (EC₅₀: 23.0 nM)。Flucopride 可能具有良好的胃肠道 (GIT) 渗透性和血脑屏障 (BBB) 跨膜渗透性 (PAMPA 实验测定)。

HY-142957

NaPi2b-IN-1	Sodium Channel Sodium Phosphate Cotransporter	Metabolic Disease
NaPi2b-IN-1 是一种钠依赖性磷酸盐转运蛋白 2b (NaPi2b) 抑制剂，IC₅₀为 64 nM。NaPi2b-IN-1 可抑制钠依赖性磷酸盐摄取，并减少大鼠空肠袢中的肠道磷酸盐吸收。NaPi2b-IN-1 可用于高磷血症的研究。

HY-181711

nNOS-IN-6	NO Synthase	Neurological Disease Cancer
nNOS-IN-6 是一种人源神经元型一氧化氮合酶 (hnNOS) 抑制剂，其对人源 hnNOS 和大鼠 rnNOS 的 K_i 分别为 16 nM 和 34 nM。nNOS-IN-6 在 PAMPA-BBB 实验中表现出高有效通透性，且在小鼠体内药代动力学研究中显示出持续的全身暴露、低清除率和良好的脑穿透性。nNOS-IN-6 可用于神经退行性疾病、黑色素瘤的研究。

HY-181710

LASSBio-2337	mTOR PI3K	Cancer
LASSBio-2337 是一种双重泛 PI3K/mTOR 抑制剂，能够功能性地调控 mTOR 及所有 PI3K 亚型，其对 mTOR 的 IC₅₀ 值为 5.8 μM。LASSBio-2337 在急性淋巴细胞白血病、慢性粒细胞白血病及乳腺癌细胞（包括多药耐药株）中表现出显著的细胞毒作用，同时对非肿瘤性人外周血单个核细胞无杀伤活性，显示出良好的选择性。LASSBio-2337 存在不溶于水、在大鼠肝微粒体中代谢稳定性较低以及仅具中等 PAMPA-GIT 通透性等理化局限，但 LASSBio-2337 是研究白血病和乳腺癌的重要工具分子。

HY-P11621

JWP24	E1/E2/E3 Enzyme	Cancer
JWP24 是首个可穿透细胞膜的 MAGE-A4 肽类抑制剂，对人源 MAGE-A4 的 IC₅₀ 为 200 nM。JWP24 能结合细胞内靶点并维持结合活性，破坏 MAGE-A4 与 RAD18 之间的相互作用，且在有效浓度下不会诱导细胞毒性。JWP24 可用于癌症相关研究。

HY-181553

PROTAC BRD4 Degrader-44	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD4 Degrader-44 (compound 2a) 是一种靶向 BRD4 的 PROTAC 降解剂，具备膜通透性。PROTAC BRD4 Degrader-44 在添加 10% FBS 的培养基中可在 6 小时内保持稳定性。PROTAC BRD4 Degrader-44 可在 6 小时内呈现细胞内积累量递增的趋势，提示外排作用减弱。

Cat. No.	Product Name

HY-L0116V

Asinex Macrocycles for RNA Library	1,065 compounds
Macrocycles are promising scaffolds for the design of novel RNA targeting molecules. This collection of macrocycles for RNA consists of very diverse, drug-like molecules which incorporate certain known RNA-recognition elements (e.g. nucleobase ring systems and analogs) distributed within macrocyclic rings or peripheral fragments. As macrocyclic molecules tend to be larger than traditional screening molecules, it is vital to carefully assess and control their physicochemical properties. All macrocycles have been tested for aqueous and DMSO solubility with cutoffs applied at 10 mM in DMSO and 50 µM in PBS (pH 7.4); PAMPA permeability has also been tested for representative set of macrocycles.

Asinex Macrocycles for RNA Library

1,065 compounds

Macrocycles are promising scaffolds for the design of novel RNA targeting molecules. This collection of macrocycles for RNA consists of very diverse, drug-like molecules which incorporate certain known RNA-recognition elements (e.g. nucleobase ring systems and analogs) distributed within macrocyclic rings or peripheral fragments. As macrocyclic molecules tend to be larger than traditional screening molecules, it is vital to carefully assess and control their physicochemical properties. All macrocycles have been tested for aqueous and DMSO solubility with cutoffs applied at 10 mM in DMSO and 50 µM in PBS (pH 7.4); PAMPA permeability has also been tested for representative set of macrocycles.

HY-L0115V

Asinex Macrocycles Library	10,091 compounds
ASINEX has elaborated a library of diverse macrocycles using an effective tool box of synthetic methods. The resulting scaffolds are novel, tremendously diverse, medchem-relevant, macrocyclic frameworks. Macrocyles tend to be larger than traditional screening molecules which make them perfect discovery tools for targets with shallow or extended binding sites. At the same time, their unique character based on restricted flexibility and ability to form intra-molecular hydrogen bonds allows for design approaches effectively optimizing properties such asaqueous solubility and membrane permeability. Many of these macrocycles have been tested for aqueous and DMSO solubility with cut-offs applied at 10 mM in DMSO and 50 µM in PBS (pH 7.4) followed by PAMPA permeability assay.

Asinex Macrocycles Library

10,091 compounds

ASINEX has elaborated a library of diverse macrocycles using an effective tool box of synthetic methods. The resulting scaffolds are novel, tremendously diverse, medchem-relevant, macrocyclic frameworks.

Macrocyles tend to be larger than traditional screening molecules which make them perfect discovery tools for targets with shallow or extended binding sites. At the same time, their unique character based on restricted flexibility and ability to form intra-molecular hydrogen bonds allows for design approaches effectively optimizing properties such asaqueous solubility and membrane permeability. Many of these macrocycles have been tested for aqueous and DMSO solubility with cut-offs applied at 10 mM in DMSO and 50 µM in PBS (pH 7.4) followed by PAMPA permeability assay.

Cat. No.	Product Name	Type

HY-D2060

ATTO 740	Fluorescent Dye
ATTO 740 是一种近红外染料 (Ex/Em：740/764 nm)。ATTO 740 可和 Cetuximab 抗体 (HY-P9905) 偶联。

Cat. No.	Product Name	Target	Research Area

HY-144285

CXCR4 antagonist 4	CXCR HIV	Inflammation/Immunology
CXCR4 antagonist 4 是一种有效，具有口服活性的 CXCR4 拮抗剂 (IC₅₀=24 nM)，可降低 CYP 2D6 的活性，提高 PAMPA 的通透性，有效抑制人类免疫缺陷病毒的进入 (IC₅₀=7 nM).

HY-P11621

JWP24	E1/E2/E3 Enzyme	Cancer
JWP24 是首个可穿透细胞膜的 MAGE-A4 肽类抑制剂，对人源 MAGE-A4 的 IC₅₀ 为 200 nM。JWP24 能结合细胞内靶点并维持结合活性，破坏 MAGE-A4 与 RAD18 之间的相互作用，且在有效浓度下不会诱导细胞毒性。JWP24 可用于癌症相关研究。

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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