GDC-0276 |
Catalog No.GC39559
One-Click Copy Product Info
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GDC-0276 is a potent, selective, reversible, orally active voltage-gated sodium channel 1.7 (NaV1.7) inhibitor with an IC50 value of 0.4nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1494581-70-2
Sample solution is provided at 25 µL, 10mM.
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GDC-0276 is a potent, selective, reversible, orally active voltage-gated sodium channel 1.7 (NaV1.7) inhibitor with an IC50 value of 0.4nM[1]. NaV1.7 is a complex protein with multiple druggable sites that plays a vital role in the transmission of pain signals[2]. GDC-0276 is a class of acylsulfonamide NaV1.7 inhibitors with good tolerability and good pharmacokinetic properties[3, 4]. GDC-0276 can be used to treat pain and address the shortcomings of existing analgesics, such as addiction and off-target side effects[5].
References:
[1] Nguyen P T, Yarov-Yarovoy V. Towards structure-guided development of pain therapeutics targeting voltage-gated sodium channels[J]. Frontiers in pharmacology, 2022, 13: 842032.
[2] McKerrall S J, Sutherlin D P. Nav1. 7 inhibitors for the treatment of chronic pain[J]. Bioorganic & medicinal chemistry letters, 2018, 28(19): 3141-3149.
[3] Rothenberg M E, Tagen M, Chang J H, et al. Safety, tolerability, and pharmacokinetics of GDC-0276, a novel Na V 1.7 inhibitor, in a first-in-human, single-and multiple-dose study in healthy volunteers[J]. Clinical drug investigation, 2019, 39: 873-887.
[4] Safina B S, McKerrall S J, Sun S, et al. Discovery of acyl-sulfonamide NaV1. 7 inhibitors GDC-0276 and GDC-0310[J]. Journal of medicinal chemistry, 2021, 64(6): 2953-2966.
[5] Stumpf A, Cheng Z K, Beaudry D, et al. Improved synthesis of the Nav1. 7 inhibitor GDC-0276 via a highly regioselective SNAr reaction[J]. Organic Process Research & Development, 2019, 23(9): 1829-1840.
| Cas No. | 1494581-70-2 | SDF | |
| Canonical SMILES | O=C(NS(=O)(N1CCC1)=O)C2=CC(C3CC3)=C(OCC4(C5)CC6CC5CC(C6)C4)C=C2F | ||
| Formula | C24H31FN2O4S | M.Wt | 462.58 |
| Solubility | DMSO: 125 mg/mL (270.22 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1618 mL | 10.8089 mL | 21.6179 mL |
| 5 mM | 432.4 μL | 2.1618 mL | 4.3236 mL |
| 10 mM | 216.2 μL | 1.0809 mL | 2.1618 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)