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胍基丙酸

胍基丙酸用途

【用途一】
用作食品、饮料、饲料添加剂，营养强化剂，化妆品用表面活性剂和医药原料等

胍基丙酸名称

[ CAS 号 ]:
353-09-3

[ 中文名 ]:
beta-丙酸胍

[ 英文名 ]:
RGX-202

[中文别名 ]:

胍基丙酸

[英文别名 ]:

EINECS 206-530-0
β-Alanine, N-(aminoiminomethyl)-
3-(diaminomethylideneamino)propanoic acid
n-carbamimidoyl-|A-alanine
beta-Guanidinopropionic acid
3-Guanidinopropanoate
3-carbamimidamidopropanoic acid
N-Carbamimidoyl-β-alanine
N-(Aminomethyl)-β-alanine
MFCD00045939

胍基丙酸生物活性

[ 描述 ]:

RGX-202是一种口服小分子SLC6A8转运体抑制剂。RGX-202在体外和体内强烈抑制肌酸输入,降低细胞内磷酸肌酸和ATP水平,并诱导肿瘤细胞凋亡。RGX-202可用于癌症研究[1]。

[ 相关类别 ]:

研究领域 >> 癌症

[ 靶点 ]

Human Endogenous Metabolite

[体外研究]

RGX-202(10μM；96小时)可减少细胞生长,并显示出磷酸肌酸几乎完全耗尽(>99%),细胞内肌酸减少超过79%,细胞内ATP水平相对于缺氧时的对照细胞显著降低(46%)[1]。

[体内研究]

RGX-202(800 mg/kg；p.o.35天)降低B6129SF1/J小鼠的UN-KPC-961胰腺肿瘤肌酸水平[1]。RGX-202(约650 mg/kg；连续14天每天腹腔注射)治疗可将NOD-SCID小鼠的Lvm3b细胞肝转移定植减少八倍[1]。动物模型：UN-KPC-961胰腺肿瘤B6129SF1/J小鼠[1]剂量：800 mg/kg给药：p.o.持续35天结果：在800 mg/kg剂量下,肿瘤d3肌酸进口抑制50%。动物模型：6至9周龄C57BL/6J雄性野生型小鼠[1]剂量：100、250、500 mg/KG无菌0.9%氯化钠给药：p.o.持续35天结果：在500 mg/KG剂量下,以剂量依赖性方式抑制组织对d3肌酸的摄取高达75%。

[参考文献]

[1]. Kurth I, et al. Therapeutic targeting of SLC6A8 creatine transporter suppresses colon cancer progression and modulates human creatine levels. Sci Adv. 2021 Oct 8;7(41):eabi7511.

胍基丙酸物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
299.1±42.0 °C at 760 mmHg

[ 熔点 ]:
222 °C (dec.)(lit.)

[ 分子式 ]:
C₄H₉N₃O₂

[ 分子量 ]:
131.133

[ 闪点 ]:
134.7±27.9 °C

[ 精确质量 ]:
131.069473

[ PSA ]:
99.20000

[ LogP ]:
-1.68

[ 外观性状 ]:
白色结晶粉末

[ 蒸汽压 ]:
0.0±1.3 mmHg at 25°C

[ 折射率 ]:
1.575

[ 储存条件 ]:
−20°C

胍基丙酸MSDS

详细MSDS(安全技术说明书)

胍基丙酸安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi:Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
AY3157500

[ 海关编码 ]:
2925290090

胍基丙酸合成路线

详细合成路线

胍基丙酸上下游产品

胍基丙酸上游产品

胍基丙酸下游产品

胍基丙酸海关

[ 海关编码 ]: 2925290090

[ 中文概述 ]:
2925290090 其他亚胺及其衍生物，以及它们的盐。监管条件:无。增值税率:17.0%。退税率:9.0%。最惠国关税:6.5%。普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2925290090 other imines and their derivatives; salts thereof。Supervision conditions:None。VAT:17.0%。Tax rebate rate:9.0%。MFN tariff:6.5%。General tariff:30.0%

胍基丙酸文献

Novel parent structures for inhibitors of the murine GABA transporters mGAT3 and mGAT4.

Eur. J. Pharmacol. 519(1-2) , 43-7, (2005)

Searching for potent and subtype selective parent structures of the murine gamma-aminobutyric acid (GABA) transporter subtypes mGAT3 and mGAT4 a series of amino acids was characterised in a uniform [3...

Three-dimensional quantitative structure-activity relationship analyses of substrates of the human proton-coupled amino acid transporter 1 (hPAT1).

Bioorg. Med. Chem. 19 , 6409-18, (2011)

The proton-coupled amino acid transporter hPAT1 has recently gained much interest due to its ability to transport small drugs thereby allowing their oral administration. A three-dimensional quantitati...

Accumulation of methylguanidine and changes in guanidino compound levels in plasma, urine, and kidneys of furosemide-treated rats.

Metab. Clin. Exp. 57(6) , 802-10, (2008)

Antidiuresis and renal diseases alter the levels of guanidino compounds (GCs) in various tissues. Therefore, we hypothesized that diuresis could also disturb GC metabolism, storage, and elimination. I...

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