2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. PF 04531083

PF 04531083 is an orally active and selective NaV1.8 blocker with an IC50 of 0.7 μM. PF 04531083 is a blood-brain barrier (BBB) penetrant compound. PF 04531083 can be used for the research of respiratory system and neuropathic/inflammatory pain.

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PF 04531083

PF 04531083 構造式

CAS 番号 : 1079400-07-9

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 110 在庫あり
Solution
10 mM * 1 mL in DMSO USD 110 在庫あり
Solid
5 mg $100 在庫あり
10 mg $180 在庫あり
25 mg $280 在庫あり
50 mg $420 在庫あり
100 mg $590 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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Based on 0 publication(s) in Google Scholar

Other Forms of PF 04531083:

PF 04531083 関連抗体

Top Publications Citing Use of Products

Sodium Channel アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Nav1.1 Nav1.2 Nav1.3 Nav1.4 Nav1.5 Nav1.6 Nav1.7 Nav1.8 Nav1.9

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

PF 04531083 is an orally active and selective NaV1.8 blocker with an IC50 of 0.7 μM. PF 04531083 is a blood-brain barrier (BBB) penetrant compound. PF 04531083 can be used for the research of respiratory system and neuropathic/inflammatory pain[1][2][3].

IC50 & Target[1]

Nav1.8

 

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.19 μM
Compound: 13
Inhibition of human Nav1.8/beta1 expressed in HEK293 cells by manual patch clamp electrophysiology
Inhibition of human Nav1.8/beta1 expressed in HEK293 cells by manual patch clamp electrophysiology
[PMID: 26101568]
HEK293 IC50
0.7 μM
Compound: 13
Inhibition of human Nav1.8 expressed in HEK293 cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
Inhibition of human Nav1.8 expressed in HEK293 cells assessed as reduction in blue fluorescent signal by VSP-FRET assay
[PMID: 26101568]
HEK293 IC50
36 μM
Compound: 13
Inhibition of human Nav1.7 expressed in HEK293 cells by FRET assay
Inhibition of human Nav1.7 expressed in HEK293 cells by FRET assay
[PMID: 26101568]
HEK293 IC50
37 μM
Compound: 13
Inhibition of human Nav1.1 expressed in HEK293 cells by IonWorks Quattro selectivity assay
Inhibition of human Nav1.1 expressed in HEK293 cells by IonWorks Quattro selectivity assay
[PMID: 26101568]
HEK293 IC50
37 μM
Compound: 13
Inhibition of human Nav1.5 expressed in HEK293 cells by IonWorks Quattro selectivity assay
Inhibition of human Nav1.5 expressed in HEK293 cells by IonWorks Quattro selectivity assay
[PMID: 26101568]
体外実験

PF 04531083 (1 μM) stimulates baseline activity by ~50% and the firing response to 10% CO2 in chemosensitive retrotrapezoid nucleus (RTN) neuron in a slice from a Tcf4tr/+ mice[3].
PF 04531083 blocks human Nav1.8, hNav1.1, hNav1.5, hNav1.7, TTX-r rat DRG, TTX-R hDRG, hERG with IC50 values of 0.19, 37, 37, 36, 0.54, 0.2, >30 μM, respectively[2].

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

PF 04531083 関連抗体
Parmacokinetics
Species Dose Route T1/2 Tmax Clearance (CL) Vd Bioavailability
Rat 1 mg/kg i.v. 3.9 h - 6.7 mL/min/kg 2.25 L/kg -
Rat 2 mg/kg p.o. N.D. 1.3 h 11.4 mL/min/kg - 59 %
体内実験

PF 04531083 (1 mg/kg, i.v.; or 2 mg/kg, p.o.) is a low clearance compound with good bioavailability ∼60% in rats[2].
PF 04531083 (40 mg/kg; 1.5 h) is efficacious in the tibial nerve transection (TNT) induced mechanical allodynia model in rat[2].
PF 04531083 inhibits native tetrodotoxin-resistant (TTX-R) currents in rodent dorsal root ganglion (DRG) neurons with an IC50 of 0.54 μM[2].
PF 04531083 (40 mg/kg; 1.5 h) improves baseline breathing in Tcf4tr/+ mice[3].
PF 04531083 (30 min before test) improves behavioral abnormalities associated with Pitt-Hopkins syndrome (PTHS) in Tcf4tr/+ mice[3].

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

Animal Model: Tcf4+/+ and Tcf4tr/+ mice [3]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection (i.p.), 1.5 h before test
Result: Decreased episodes of hyperventilation, increased the occurrence of spontaneous sighs, diminished duration of post-sigh apnea and improved the CO2 minute ventilatory response in Tcf4tr/+ mice.
Showed stable respiratory activity in Tcf4+/+ mice.
Showed a robust increase in respiratory activity (62.5% increase in minute ventilation from 3 to 7% CO2) in Tcf4tr/+ pups.
臨床実験
分子量

357.79

分子式

C17H16ClN5O2
CAS 番号
Appearance

Solid

Color

Light yellow to yellow

SMILES

ClC1=CC=C(OC)C=C1C2=C(N=C(NC(C3=CC=NN3C)=O)C=C2)N
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 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (279.49 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 2.7949 mL 13.9747 mL 27.9494 mL
5 mM 0.5590 mL 2.7949 mL 5.5899 mL
10 mM 0.2795 mL 1.3975 mL 2.7949 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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: ≥ 2.08 mg/mL (5.81 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.81 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
純度とドキュメンテーション

純度: 99.62%

COA (254 KB) LCMS (102 KB)

取扱説明書 (2659 KB)
参考文献

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7949 mL 13.9747 mL 27.9494 mL 69.8734 mL
5 mM 0.5590 mL 2.7949 mL 5.5899 mL 13.9747 mL
10 mM 0.2795 mL 1.3975 mL 2.7949 mL 6.9873 mL
15 mM 0.1863 mL 0.9316 mL 1.8633 mL 4.6582 mL
20 mM 0.1397 mL 0.6987 mL 1.3975 mL 3.4937 mL
25 mM 0.1118 mL 0.5590 mL 1.1180 mL 2.7949 mL
30 mM 0.0932 mL 0.4658 mL 0.9316 mL 2.3291 mL
40 mM 0.0699 mL 0.3494 mL 0.6987 mL 1.7468 mL
50 mM 0.0559 mL 0.2795 mL 0.5590 mL 1.3975 mL
60 mM 0.0466 mL 0.2329 mL 0.4658 mL 1.1646 mL
80 mM 0.0349 mL 0.1747 mL 0.3494 mL 0.8734 mL
100 mM 0.0279 mL 0.1397 mL 0.2795 mL 0.6987 mL
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PF 04531083 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

PF 045310831079400-07-9PF04531083PF-04531083Sodium ChannelNa channelsNa+ channelsinflammationrespiratoryblood-brain barrierInhibitorinhibitorinhibit

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製品番号:
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