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)
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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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]. |
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. |
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. |
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 |
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 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
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