BiochemProbe — Life Science Research Reagents

ND-630 free base · Synonyms: Firsocostat | GS-0976 | NDI-010976

ND-630 is an acetyl-CoA carboxylase inhibitor.

For research use only. Not for human or veterinary use.

Target Acetyl-CoA Carboxylase
Research area Metabolic Disease
Purity >98% Stock Inquire
Data Sheet SDS COA

ND-630 structure

CAS No.: 1434635-54-7

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
250 mg USD 480.00 BP-01888-250mg In stock Get quote
500 mg USD 750.00 BP-01888-500mg In stock Get quote
1 g USD 1,250.00 BP-01888-1g In stock Get quote
2 g Inquire BP-01888-2g Inquire Inquire
5 g Inquire BP-01888-5g Inquire Inquire

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Description

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

Biological activity

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. 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 t1/2 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.

Identifiers

SMILES
COC1=C(C=CC=C1)[C@H](CN1C2=C(C(C)=C(S2)C2=NC=CO2)C(=O)N(C1=O)C(C)(C)C(O)=O)OC1CCOCC1
InChIKey
ZZWWXIBKLBMSCS-FQEVSTJZSA-N

Specifications

MW (average)
569.6260
Formula
C28H31N3O8S
CAS No.
1434635-54-7
Physical state
Solid
Color
White to light yellow
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage
Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO >50 mg/mL

Documents

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.

Same target

Search Acetyl-CoA Carboxylase

Same research area

Search Metabolic Disease