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GDC-0276

Alias: GDC0276; GDC 0276
Cat No.:V37847 Purity: ≥98%
GDC-0276 is a potent, selective, reversible, orally bioactive NaV1.7 inhibitor (antagonist) with IC50 of 0.4 nM.
GDC-0276
GDC-0276 Chemical Structure CAS No.: 1494581-70-2
Product category: New2
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
Other Sizes
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
GDC-0276 is a potent, selective, reversible, orally bioactive NaV1.7 inhibitor (antagonist) with IC50 of 0.4 nM. GDC-0276 is well tolerated and displays favorable pharmacokinetic characteristics. GDC-0276 is indicated for pain and related research that addresses deficiencies in existing analgesic active molecules, like addiction and off-target side effects.
Biological Activity I Assay Protocols (From Reference)
ln Vivo
GDC-0276 (Wall; 0.5–5 mg/kg) exhibits a specific activity of 22.6 μCi/mg and 14C enrichment. Guns tested negative for GDC-0276; nevertheless, stolen artifacts tested positive for 14C enrichment, with a specific activity of 19.6 μCi/mg [3].
Animal Protocol
Animal/Disease Models: 6 drug-naïve beagles, 4 dogs in group 1 (n=2 of each sex) and 2 BDC dogs in group 2 (n=2 males) [3]
Doses: 0.5, 1 , 2, 3, 4, 5 mg/kg
Route of Administration: Oral
Experimental Results: Mean specific activity was 12.2 µCi/mg (24% enriched) (n=4 animals) and 23.5 µCi/mg Groups 1 and 2 mg (139% enrichment) for 2 groups respectively (n=2 animals).
References

[1]. Safety, Tolerability, and Pharmacokinetics of GDC-0276, a Novel NaV1.7 Inhibitor, in a First-in-Human, Single- and Multiple-Dose Study i.

[2]. Nav1.7 inhibitors for the treatment of chronic pain. Bioorganic & Medicinal Chemistry Letters (2018).

[3]. Unequal Absorption of Radiolabeled and Nonradiolabeled Drug from the Oral Dose Leads to Incorrect Estimates of Drug Absorption and Circulating Metabolites in a Mass Balance Study.Drug Metab Lett. 2019;13(1):37-44.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H31FN2O4S
Molecular Weight
462.577348947525
Exact Mass
462.198
CAS #
1494581-70-2
PubChem CID
91809347
Appearance
White to off-white solid powder
LogP
4.7
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
6
Rotatable Bond Count
7
Heavy Atom Count
32
Complexity
809
Defined Atom Stereocenter Count
0
SMILES
S(NC(C1=C(C=C(C(=C1)C1CC1)OCC12CC3CC(CC(C3)C1)C2)F)=O)(N1CCC1)(=O)=O
InChi Key
PTCBNPULJWGSML-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H31FN2O4S/c25-21-10-22(31-14-24-11-15-6-16(12-24)8-17(7-15)13-24)19(18-2-3-18)9-20(21)23(28)26-32(29,30)27-4-1-5-27/h9-10,15-18H,1-8,11-14H2,(H,26,28)
Chemical Name
4-(1-adamantylmethoxy)-N-(azetidin-1-ylsulfonyl)-5-cyclopropyl-2-fluorobenzamide
Synonyms
GDC0276; GDC 0276
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~125 mg/mL (~270.22 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 6.25 mg/mL (13.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1618 mL 10.8089 mL 21.6179 mL
5 mM 0.4324 mL 2.1618 mL 4.3236 mL
10 mM 0.2162 mL 1.0809 mL 2.1618 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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