1. Metabolic Enzyme/Protease
  2. Acetyl-CoA Carboxylase

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

Cat. No.: HY-16901 Purity: 98.72%
Handling Instructions

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

For research use only. We do not sell to patients.

ND-630 Chemical Structure

ND-630 Chemical Structure

CAS No. : 1434635-54-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 338 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
1 mg USD 110 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
5 mg USD 270 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 450 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
25 mg USD 1040 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 1850 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 2850 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

ND-630 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]

In Vitro

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. ND-630 inhibits ACC activity by interacting within the phosphopeptide-acceptor and dimerization site of the enzyme to prevent dimerization. ND-630 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].

In Vivo

Chronical administration of 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 ND-630 Zucker diabetic fatty rats, ND-630 reduces hepatic steatosis, improves glucose-stimulated insulin secretion, and reduces hemoglobin A1c (0.9% reduction). ND-630 exhibits an aqueous solubility of 594 μM and human and rat plasma protein binding of 98.5% and 98.6%, respectively. Pharmacokinetic evaluation of ND-630 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[1].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume 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
Please refer to the solubility information to select the appropriate solvent.
Animal Administration
[1]

Rats: ND-630 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 ND-630 (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 has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

569.63

Formula

C₂₈H₃₁N₃O₈S

CAS No.

1434635-54-7

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 50 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.72%

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Product Name:
ND-630
Cat. No.:
HY-16901
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