製品番号: HY-131182

DS-1971a

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

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.

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純度: 99.30%
CAS 番号: 1450595-86-4
分子式: C₂₀H₂₁ClFN₅O₃S
分子量:465.93

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

DS-1971a 構造式

CAS 番号: 1450595-86-4

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生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体内実験
- 臨床実験
化学情報
Publications (1)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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

hNa_v1.7

22.8 nM (IC₅₀)

mNa_v1.7

59.4 nM (IC₅₀)

Sodium Channel アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	>100000 nM Compound: 6o; DS-1971a	Inhibition of human Nav1.3 expressed in CHO cells with -120 mV holding potential by whole cell manual patch clamp method Inhibition of human Nav1.3 expressed in CHO cells with -120 mV holding potential by whole cell manual patch clamp method	[PMID: 32392056]
CHO	IC₅₀	>100000 nM Compound: 6o; DS-1971a	Inhibition of human Nav1.4/beta1/beta2 expressed in CHO cells with -120 mV holding potential by whole cell manual patch clamp method Inhibition of human Nav1.4/beta1/beta2 expressed in CHO cells with -120 mV holding potential by whole cell manual patch clamp method	[PMID: 32392056]
CHO	IC₅₀	>100000 nM Compound: 6o; DS-1971a	Inhibition of human Nav1.5 expressed in CHO cells with -140 mV holding potential by whole cell manual patch clamp method Inhibition of human Nav1.5 expressed in CHO cells with -140 mV holding potential by whole cell manual patch clamp method	[PMID: 32392056]
CHO	IC₅₀	1960 nM Compound: 6o; DS-1971a	Inhibition of human Nav1.2 expressed in CHO cells with -120 mV holding potential by whole cell manual patch clamp method Inhibition of human Nav1.2 expressed in CHO cells with -120 mV holding potential by whole cell manual patch clamp method	[PMID: 32392056]
CHO	IC₅₀	22.8 nM Compound: 6o; DS-1971a	Inhibition of human Nav1.7 expressed in CHO cells with -120 mV holding potential by whole cell manual patch clamp method Inhibition of human Nav1.7 expressed in CHO cells with -120 mV holding potential by whole cell manual patch clamp method	[PMID: 32392056]
CHO	IC₅₀	475 nM Compound: 6o; DS-1971a	Inhibition of human Nav1.6 expressed in CHO cells with -120 mV holding potential by whole cell manual patch clamp method Inhibition of human Nav1.6 expressed in CHO cells with -120 mV holding potential by whole cell manual patch clamp method	[PMID: 32392056]
CHO	IC₅₀	>100000 nM Compound: 6o; DS-1971a	Inhibition of human Nav1.1 expressed in CHO cells with -120 mV holding potential by whole cell manual patch clamp method Inhibition of human Nav1.1 expressed in CHO cells with -120 mV holding potential by whole cell manual patch clamp method	[PMID: 32392056]
HEK293	IC₅₀	>100000 nM Compound: 6o; DS-1971a	Inhibition of human ERG expressed in HEK293 cells with -80 mV holding potential by whole cell manual patch clamp method Inhibition of human ERG expressed in HEK293 cells with -80 mV holding potential by whole cell manual patch clamp method	[PMID: 32392056]
HEK293-A	IC₅₀	>100000 nM Compound: 6o; DS-1971a	Inhibition of mouse Nav1.1/beta1/beta2 expressed in HEK293A cells with -120 mV holding potential by whole cell manual patch clamp method Inhibition of mouse Nav1.1/beta1/beta2 expressed in HEK293A cells with -120 mV holding potential by whole cell manual patch clamp method	[PMID: 32392056]
HEK293-A	IC₅₀	>100000 nM Compound: 6o; DS-1971a	Inhibition of mouse Nav1.5/beta1/beta2 expressed in HEK293A cells with -140 mV holding potential by whole cell manual patch clamp method Inhibition of mouse Nav1.5/beta1/beta2 expressed in HEK293A cells with -140 mV holding potential by whole cell manual patch clamp method	[PMID: 32392056]
HEK293-A	IC₅₀	59.4 nM Compound: 6o; DS-1971a	Inhibition of mouse Nav1.7/beta1/beta2 expressed in HEK293A cells with -120 mV holding potential by whole cell manual patch clamp method Inhibition of mouse Nav1.7/beta1/beta2 expressed in HEK293A cells with -120 mV holding potential by whole cell manual patch clamp method	[PMID: 32392056]
HEK293-A	IC₅₀	>100000 nM Compound: 6o; DS-1971a	Inhibition of human NaV1.1/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method Inhibition of human NaV1.1/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method	[PMID: 32392056]
HEK293-A	IC₅₀	>100000 nM Compound: rac-6o	Inhibition of human NaV1.5/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method Inhibition of human NaV1.5/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method	[PMID: 32392056]
HEK293-A	IC₅₀	93 μM Compound: 6o; DS-1971a	Inhibition of human NaV1.5/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method Inhibition of human NaV1.5/beta1/beta2 expressed in HEK293A cells by Ionworks high-throughput electrophysiology method	[PMID: 32392056]

体内実験

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.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1450595-86-4
性状 Solid
分子量 465.93
分子式 C₂₀H₂₁ClFN₅O₃S
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
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175

溶剤 & 溶解度

体外:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1462 mL

10.7312 mL

21.4625 mL

5 mM

0.4292 mL

2.1462 mL

4.2925 mL

10 mM

0.2146 mL

1.0731 mL

2.1462 mL

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.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (275 KB)
SDS (394 KB)
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- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Shinozuka T, et al. Discovery of DS-1971a, a Potent, Selective NaV1.7 Inhibitor [published online ahead of print, 2020 May 26]. J Med Chem. 2020;10.1021/acs.jmedchem.0c00259. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

DS-1971a

1 Cited Publications

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DS-1971a

Membrane Transporter/Ion Channel Compound Library

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MedChemExpress（MCE）の使用を引用している文献 DS-1971a

Sodium Channel アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (1)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

DS-1971a

Membrane Transporter/Ion Channel Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Chemical Probe Library

Neuroprotective Compound Library

Sodium Channel Blocker Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

MedChemExpress（MCE）の使用を引用している文献 DS-1971a

Sodium Channel アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (1)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

DS-1971a 関連分類

HY-131182 関連分類