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Firsocostat

货号:A512642 同义名: ND-630; GS-0976

Firsocostat(ND-630)是一种乙酰辅酶A羧化酶(ACC)二聚体化的变构抑制剂,可抑制ACC1和ACC2的活性(IC50分别为2.1 nM和6.1 nM)

Firsocostat 化学结构 CAS号:1434635-54-7
Firsocostat 化学结构
CAS号:1434635-54-7
Firsocostat 3D分子结构
CAS号:1434635-54-7
Firsocostat 化学结构 CAS号:1434635-54-7
Firsocostat 3D分子结构 CAS号:1434635-54-7
规格 价格 库存 数量
50μL*10mM(DMSO) ¥219 咨询
100μL*10mM(DMSO) ¥349 咨询
250μL*10mM(DMSO) ¥699 咨询
500μL*10mM(DMSO) ¥1159 咨询
10mM*1mL(DMSO) ¥1754 咨询
1mg ¥598 咨询
2mg ¥718 咨询
5mg ¥1260 咨询
10mg ¥2016 咨询
25mg ¥2800 咨询
50mg ¥3360 咨询
100mg ¥6719 咨询
1g ¥51443 咨询
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Firsocostat 纯度/质量文件 产品仅供科研

货号:A512642 标准纯度:
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Firsocostat 生物活性

描述 Fatty acid metabolism dysregulated through elevated fatty acid synthesis (FASyn), impaired fatty acid oxidation (FAOxn), or both is a hallmark of various metabolic disorders. ACC (acetyl-CoA carboxylase) catalyzes the ATP-dependent carboxylation of acetyl-CoA to form malonyl-CoA, the rate-limiting and first committed reaction in FASyn. ND-630, a reversible and highly specific ACC inhibitor, inhibits hACC1 with an IC50 of 2.1 ± 0.2 nM and hACC2 with an IC50 of 6.1 ± 0.8 nM. When ND-630 and [14C]acetate were administered to Hep-G2 cells for 4 h, ND-630 inhibited FASyn with EC50 values of 66 nM in cells cultured in medium containing 10% serum and 8.7 nM when assessed in serum-free medium. When ND-630 and [14C]palmitate were administered to C2C12 cells for 6 h, ND-630 increased both the release of [14C]O2 and the production of [14C]acid-soluble material. ND-630 exhibited an aqueous solubility of 594 μM and human and rat plasma protein binding of 98.5% and 98.6%, respectively. When chow-fed male Sprague–Dawley rats were treated orally with ND-630 for 1 h, hepatic malonyl-CoA was dose-dependently reduced with an ED50 of 0.8 mg/kg. When chow-fed male Sprague–Dawley rats treated orally with ND-630 for 1 h were given an i.p. bolus of [14C]acetate, ND-630 reduced hepatic FASyn with an ED50 of 0.14 mg/kg. Moreover, ND-630 increased whole-body FAOxn, assessed as a reduction in respiratory quotient (RQ). As a consequence of FASyn inhibition and FAOxn stimulation, ND-630 dose-dependently reduced the hepatic steatosis produced by the HSD (high-sucrose diet) without altering either hepatic cholesterol or glycogen. ND-630 also dose-dependently reduced the elevated plasma triglycerides and free fatty acids produced by the HSD[1].
作用机制 ND-630 interacts within the acetyl-CoA carboxylase subunit phosphopeptide acceptor and dimerization site to prevent dimerization and inhibit enzymatic activity[1].

Firsocostat 细胞实验

Cell Line
Concentration Treated Time Description References
Mouse RPE-choroid tissue 100 nM 1 hour Firsocostat increases fatty acid oxidation, decreases intracellular lipid levels, diminishes lipoprotein release, and increases TEER. J Biol Chem. 2024 Oct;300(10):107772.
3D liver microtissues (hLiMTs) 0.5 µM and 10 µM 10 days Firsocostat significantly decreased TG levels and reduced lipid accumulation in NASH hLiMTs. Sci Rep. 2021 Nov 23;11(1):22765.
Candida albicans SC5314 25 µM 24 hours To evaluate the growth-inhibitory effect of Firsocostat on C. albicans SC5314, results showed Firsocostat exhibited antifungal activity Antimicrob Agents Chemother. 2024 Jan 10;68(1):e0113123.
Candida albicans C5 25 µM 24 hours To evaluate the growth-inhibitory effect of Firsocostat on C. albicans C5, results showed Firsocostat exhibited antifungal activity Antimicrob Agents Chemother. 2024 Jan 10;68(1):e0113123.
Human iPSC-RPE cells 1 to 1000 nM 6 hours Firsocostat increases fatty acid oxidation, remodels lipid composition, and decreases apolipoprotein export by RPE cells. J Biol Chem. 2024 Oct;300(10):107772.
Huh7 cells 1% DMSO Overnight To evaluate the effect of Firsocostat in combination with other PPAR agonists on fatty acid oxidation (FAO), results showed that Firsocostat significantly increased FAO. Hepatol Commun. 2022 Sep;6(9):2298-2309.

Firsocostat 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Rats Dyslipidemic rat model induced by high-fat diet Oral 10 or 30 mg/kg Once daily for 4 weeks To evaluate the effect of Firsocostat on liver and circulating triglycerides (TG), results showed that Firsocostat significantly reduced liver TG but increased circulating TG. Hepatol Commun. 2022 Sep;6(9):2298-2309.
C57BL/6 mice Systemic candidiasis model Intravenous injection 4 mg/kg For three consecutive days To evaluate the therapeutic effect of Firsocostat alone or in combination with VOR on systemic candidiasis, results showed the combination therapy significantly reduced fungal burden in kidneys and spleens Antimicrob Agents Chemother. 2024 Jan 10;68(1):e0113123.

Firsocostat 参考文献

[1]Harriman G, Greenwood J, Bhat S, et al. Acetyl-CoA carboxylase inhibition by ND-630 reduces hepatic steatosis, improves insulin sensitivity, and modulates dyslipidemia in rats. Proc Natl Acad Sci U S A. 2016;113(13):E1796-E1805.

Firsocostat 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.76mL

0.35mL

0.18mL

8.78mL

1.76mL

0.88mL

17.56mL

3.51mL

1.76mL

Firsocostat 技术信息

CAS号1434635-54-7
分子式C28H31N3O8S
分子量 569.63
SMILES Code O=C(O)C(C)(C)N(C(N(C[C@@H](C1=CC=CC=C1OC)OC2CCOCC2)C3=C4C(C)=C(C5=NC=CO5)S3)=O)C4=O
MDL No. MFCD28963986
别名 ND-630; GS-0976; ND630. NDI-010976; NDI-010976
运输蓝冰
InChI Key ZZWWXIBKLBMSCS-FQEVSTJZSA-N
Pubchem ID 71528744
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

DMSO: 50 mg/mL(87.78 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
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