2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. DS-1971a

DS-1971a is a potent, selective, and orally active NaV1.7 inhibitor, with IC50s of 22.8 and 59.4 nM for hNaV1.7 and mNaV1.7, respectively. DS-1971a exerts analgesic effects.

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

DS-1971a Chemical Structure

DS-1971a Chemical Structure

CAS No. : 1450595-86-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 359 In-stock
Solution
10 mM * 1 mL in DMSO USD 359 In-stock
Solid
1 mg USD 166 In-stock
5 mg USD 350 In-stock
10 mg USD 550 In-stock
25 mg USD 1050 In-stock
50 mg USD 1650 In-stock
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Based on 1 publication(s) in Google Scholar

DS-1971a Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

DS-1971a is a potent, selective, and orally active NaV1.7 inhibitor, with IC50s of 22.8 and 59.4 nM for hNaV1.7 and mNaV1.7, respectively. DS-1971a exerts analgesic effects[1].

IC50 & Target

hNav1.7

22.8 nM (IC50)

mNav1.7

59.4 nM (IC50)

In Vivo

DS-1971a exhibits a favorable toxicological profile[1].
DS-1971a (0.1-1 mg/kg; p.o.) shows mitigated thermal hyperalgesia in a dose-dependent manner in partial sciatic nerve ligation (PSL) mice[1].

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

Animal Model: Male Slc:ddY mice (PSL model)[1]
Dosage: 0.1, 0.3, and 1 mg/kg
Administration: P.o.
Result: A significant dose-dependent suppression of thermal hyperalgesiain 0.3 and 1 mg/kg administered groups. The ED50 of DS-1971a at the peak efficacy was 0.32 mg/kg.
Clinical Trial
Molecular Weight

465.93

Formula

C20H21ClFN5O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC(Cl)=C(O[C@@H]2[C@@H](C3=CC=NN3C)CCCC2)C=C1F)(NC4=NC=NC=C4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (214.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1462 mL 10.7312 mL 21.4625 mL
5 mM 0.4292 mL 2.1462 mL 4.2925 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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.
Purity & Documentation
References

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1462 mL 10.7312 mL 21.4625 mL 53.6561 mL
5 mM 0.4292 mL 2.1462 mL 4.2925 mL 10.7312 mL
10 mM 0.2146 mL 1.0731 mL 2.1462 mL 5.3656 mL
15 mM 0.1431 mL 0.7154 mL 1.4308 mL 3.5771 mL
20 mM 0.1073 mL 0.5366 mL 1.0731 mL 2.6828 mL
25 mM 0.0858 mL 0.4292 mL 0.8585 mL 2.1462 mL
30 mM 0.0715 mL 0.3577 mL 0.7154 mL 1.7885 mL
40 mM 0.0537 mL 0.2683 mL 0.5366 mL 1.3414 mL
50 mM 0.0429 mL 0.2146 mL 0.4292 mL 1.0731 mL
60 mM 0.0358 mL 0.1789 mL 0.3577 mL 0.8943 mL
80 mM 0.0268 mL 0.1341 mL 0.2683 mL 0.6707 mL
100 mM 0.0215 mL 0.1073 mL 0.2146 mL 0.5366 mL
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DS-1971a Related Classifications

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:

DS-1971a1450595-86-4Sodium ChannelNa channelsNa+ channelsthermalhyperalgesiamechanicalhypersensitivitytoxicityInhibitorinhibitorinhibit

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