Firsocostat (Synonyms: ND-630; GS-0976; NDI-010976)

Name: Firsocostat
Brand: MedChemExpress
SKU: HY-16901
Rating: 5.0 (23 reviews)

Cat. No.: HY-16901 Purity: 99.96%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Firsocostat (ND-630; GS-0976; NDI-010976) is an acetyl-CoA carboxylase (ACC) inhibitor; inhibits human ACC1 and ACC2 with IC₅₀ values of 2.1 and 6.1 nM, respectively.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No. : 1434635-54-7

사이즈	재고	수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
1 mg	해외재고보유	Estimated Time of Arrival: December 31
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

or 대량구매 문의

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 23 publication(s) in Google Scholar

Other Forms of Firsocostat:

Firsocostat (S enantiomer) In-stock
Firsocostat (Standard) 견적 받기

23 Publications Citing Use of MCE Firsocostat

Cell Imaging/Staining

In Vivo Efficacy Study

Flow Cytometry

Bio/Physico-chemical Assay

IHC

: Firsocostat purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Aug;10(23):e2301094. [Abstract]; Hepatic Ac‐CoA level in young mice, aged mice, and aged mice treated with Firsocostat (10 mg/kg, oral, daily, 28 days) at 0 and 36 h after partial hepatectomy (PH; n = 6 mice per group).

: Firsocostat purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Aug;10(23):e2301094. [Abstract]; Serum alanine aminotransferase (ALT) levels in young mice, aged mice, and aged mice treated with Firsocostat (10 mg/kg, oral, daily, 28 days) at 0 and 36 h after PH.

: Firsocostat purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Aug;10(23):e2301094. [Abstract]; BrdU and Ki67 staining of liver tissues from young mice, aged mice, and aged mice treated with Firsocostat (10 mg/kg, oral, daily, 28 days) at 36 h after PH. Scale bar, 50 µm.

: Firsocostat purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2020 Sep 3;5(1):187. [Abstract]; Inhibitor of ACC1 can suppress Erastin or RSL3-induced ferroptosis. MEFs were treated as indicated for 10 h and cell death was measured by PI staining. Erastin (10 μM), RSL3 (0.5 μM), Firsocostat (ND-630, 5 μM)

: Firsocostat purchased from MedChemExpress. Usage Cited in: Signal Transduct Target Ther. 2020 Sep 3;5(1):187. [Abstract]; Inhibitor of ACC1 can suppress Erastin or RSL3-induced ferroptosis in LKB1 KO MEFs and AMPK DKO MEFs. Cells were treated as indicated for 8 h and cell death was determined by PI staining coupled with flow cytometry. Erastin (10 μM), RSL3 (1 μM), Firsocostat (ND-630, 5 μM).

: Firsocostat purchased from MedChemExpress. Usage Cited in: PeerJ. 2019 Dec 20;7:e8115. [Abstract]; GS-0976 reduces lipid accumulation and expression of profibrogenic genes. Oil Red O staining is performed in LO2 cells after treatment with the indicated GS-0976 in the presence of 0.8 mM FFA for 24 h. Original magnification , 400 ×.

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Biological Activity
Protocol
순도&문서
References
고객리뷰

제품 설명

Firsocostat (ND-630; GS-0976; NDI-010976) is an acetyl-CoA carboxylase (ACC) inhibitor; inhibits human ACC1 and ACC2 with IC₅₀ values of 2.1 and 6.1 nM, respectively.

IC₅₀ & Target

IC50: 2.1 nM (hACC1); 6.1 nM (hACC2)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	<100 nM Compound: 46	Inhibition of fatty acid synthesis in human HepG2 cells Inhibition of fatty acid synthesis in human HepG2 cells	[PMID: 25333641]

In Vitro

Firsocostat (ND-630) inhibits hACC1 (IC₅₀=2.1±0.2 nM) and hACC2 (IC₅₀=6.1±0.8 nM). Inhibition is reversible and highly specific for ACC. Firsocostat inhibits ACC activity by interacting within the phosphopeptide-acceptor and dimerization site of the enzyme to prevent dimerization. Firsocostat inhibits fatty acid synthesis with an EC₅₀ of 66 nM in HepG2 cells without altering the total cell number, cellular protein concentration, and incorporation of acetate into cholesterol^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Chronical administration of Firsocostat (ND-630) to rats with diet-induced obesity reduces hepatic steatosis, improves insulin sensitivity, reduces weight gain without affecting food intake, and favorably affects dyslipidemia. Chronical administration of Firsocostat Zucker diabetic fatty rats, Firsocostat reduces hepatic steatosis, improves glucose-stimulated insulin secretion, and reduces hemoglobin A1c (0.9% reduction). Firsocostat exhibits an aqueous solubility of 594 μM and human and rat plasma protein binding of 98.5% and 98.6%, respectively. Pharmacokinetic evaluation of Firsocostat in male Sprague-Dawley rats [i.v. 3 mg/kg; orally (p.o.) 10 mg/kg] yields a plasma t_1/2 of 4.5 h, bioavailability of 37%, clearance of 33 mL/min/kg, volume of distribution of 1.9 L/kg, oral time of maximum plasma concentration of 0.25 h^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

분자량

569.63

화학식

C₂₈H₃₁N₃O₈S

CAS No.

1434635-54-7

Appearance

Solid

Color

White to light yellow

SMILES

O=C(C(C(C)=C(C1=NC=CO1)S2)=C2N3C[C@H](OC4CCOCC4)C5=C(OC)C=CC=C5)N(C(C)(C)C(O)=O)C3=O

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

용액&용해도

In Vitro:

DMSO : ≥ 50 mg/mL (87.78 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.7555 mL	8.7776 mL	17.5553 mL
5 mM	0.3511 mL	1.7555 mL	3.5111 mL
10 mM	0.1756 mL	0.8778 mL	1.7555 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

몰농도 계산기
농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: 0.5 mg/mL (0.88 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

순도&문서

Purity: 99.96%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (259 KB) HNMR (287 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Harriman G, 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 Mar 29;113(13):E1796-805. [Content Brief]

Animal Administration
^[1]

Rats: Firsocostat is prepared in aqueous saline solution containing 1% Tween 80 and 0.5% methyl cellulose. Eight-week-old male ZDF rats are given either vehicle or Firsocostat (0.5, 1.5, 5 mg/kg) in vehicle by oral gavage b.i.d. for 37 d. Blood glucose is measured by glucometer at baseline and weekly just before dosing. Blood is collected at baseline, after 3 wk of treatment, and at the end of the study, 6 h after dosing and after a 6-h fast, for measurement of the indicated parameters. After 3 wk of treatment, animals received an oGTT (1 g/kg glucose). At the end of the study animals are killed, and liver cholesterol, triglycerides, and free fatty acids are determined^[1].

MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.

References

[1]. Harriman G, 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 Mar 29;113(13):E1796-805. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7555 mL	8.7776 mL	17.5553 mL	43.8881 mL
	5 mM	0.3511 mL	1.7555 mL	3.5111 mL	8.7776 mL
	10 mM	0.1756 mL	0.8778 mL	1.7555 mL	4.3888 mL
	15 mM	0.1170 mL	0.5852 mL	1.1704 mL	2.9259 mL
	20 mM	0.0878 mL	0.4389 mL	0.8778 mL	2.1944 mL
	25 mM	0.0702 mL	0.3511 mL	0.7022 mL	1.7555 mL
	30 mM	0.0585 mL	0.2926 mL	0.5852 mL	1.4629 mL
	40 mM	0.0439 mL	0.2194 mL	0.4389 mL	1.0972 mL
	50 mM	0.0351 mL	0.1756 mL	0.3511 mL	0.8778 mL
	60 mM	0.0293 mL	0.1463 mL	0.2926 mL	0.7315 mL
	80 mM	0.0219 mL	0.1097 mL	0.2194 mL	0.5486 mL

Firsocostat Related Classifications

Metabolic Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Firsocostat1434635-54-7ND-630 GS-0976 NDI-010976ND630ND 630GS0976GS 0976GS-0976NDI010976NDI 010976NDI-010976Acetyl-CoA CarboxylaseACC, Acetyl Coenzyme A CarboxylaseInhibitorinhibitorinhibit

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Firsocostat (Synonyms: ND-630; GS-0976; NDI-010976)

고객리뷰

Other Forms of Firsocostat:

Firsocostat Related Antibodies

23 Publications Citing Use of MCE Firsocostat

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

순도&문서

References

고객리뷰

Firsocostat Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

Firsocostat Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report