2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. Navacaprant

Navacaprant  (Synonyms: BTRX-335140; CYM-53093)

製品番号: HY-124754 純度: 99.88%
COA 取扱説明書 Technical Support

Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Navacaprant

Navacaprant 構造式

CAS 番号 : 2244614-14-8

容量 価格（税別） 在庫状況 数量
5 mg $320 在庫あり
10 mg $520 在庫あり
50 mg $1750 在庫あり
100 mg $2480 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.

カスタマーレビュー

Based on 0 publication(s) in Google Scholar

Navacaprant 関連抗体

Top Publications Citing Use of Products

Opioid Receptor 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
μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively. Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy[1].

IC50 & Target

κ Opioid Receptor/KOR

0.8 nM (IC50)

μ Opioid Receptor/MOR

110 nM (IC50)

δ Opioid Receptor/DOR

6500 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
1 1
Compound: 58; CYM-53093, BTRX-335140
Inhibition of human ERG expressed in HEK293 cells at 10 uM by Qpatch clamp assay
Inhibition of human ERG expressed in HEK293 cells at 10 uM by Qpatch clamp assay
[PMID: 30707578]
U2OS IC50
0.8 1
Compound: 58; CYM-53093, BTRX-335140
Antagonist activity at GAL4-VP16-fused KOR (unknown origin) expressed in human U2OS cells co-expressing Tango-OPRK1-BLA assessed as inhibition of U-50488-induced beta-arrestin migration after 4 hrs by FRET assay
Antagonist activity at GAL4-VP16-fused KOR (unknown origin) expressed in human U2OS cells co-expressing Tango-OPRK1-BLA assessed as inhibition of U-50488-induced beta-arrestin migration after 4 hrs by FRET assay
[PMID: 30707578]
HEK293 IC50
1 1
Compound: 58; CYM-53093, BTRX-335140
Inhibition of human ERG expressed in HEK293 cells at 10 uM by Qpatch clamp assay
Inhibition of human ERG expressed in HEK293 cells at 10 uM by Qpatch clamp assay
[PMID: 30707578]
U2OS IC50
0.8 1
Compound: 58; CYM-53093, BTRX-335140
Antagonist activity at GAL4-VP16-fused KOR (unknown origin) expressed in human U2OS cells co-expressing Tango-OPRK1-BLA assessed as inhibition of U-50488-induced beta-arrestin migration after 4 hrs by FRET assay
Antagonist activity at GAL4-VP16-fused KOR (unknown origin) expressed in human U2OS cells co-expressing Tango-OPRK1-BLA assessed as inhibition of U-50488-induced beta-arrestin migration after 4 hrs by FRET assay
[PMID: 30707578]
HEK293 IC50
1 1
Compound: 58; CYM-53093, BTRX-335140
Inhibition of human ERG expressed in HEK293 cells at 10 uM by Qpatch clamp assay
Inhibition of human ERG expressed in HEK293 cells at 10 uM by Qpatch clamp assay
[PMID: 30707578]
U2OS IC50
110 1
Compound: 58; CYM-53093, BTRX-335140
Antagonist activity at GAL4-VP16-fused MOR (unknown origin) expressed in human U2OS cells assessed as inhibition of DAMGO-induced beta-arrestin migration preincubated for 30 mins followed by agonist addition and measured after 3 hrs by PathHunter assay
Antagonist activity at GAL4-VP16-fused MOR (unknown origin) expressed in human U2OS cells assessed as inhibition of DAMGO-induced beta-arrestin migration preincubated for 30 mins followed by agonist addition and measured after 3 hrs by PathHunter assay
[PMID: 30707578]
U2OS IC50
110 1
Compound: 58; CYM-53093, BTRX-335140
Antagonist activity at GAL4-VP16-fused MOR (unknown origin) expressed in human U2OS cells assessed as inhibition of DAMGO-induced beta-arrestin migration preincubated for 30 mins followed by agonist addition and measured after 3 hrs by PathHunter assay
Antagonist activity at GAL4-VP16-fused MOR (unknown origin) expressed in human U2OS cells assessed as inhibition of DAMGO-induced beta-arrestin migration preincubated for 30 mins followed by agonist addition and measured after 3 hrs by PathHunter assay
[PMID: 30707578]
U2OS IC50
6500 1
Compound: 58; CYM-53093, BTRX-335140
Antagonist activity at GAL4-VP16-fused DOR (unknown origin) expressed in human U2OS cells assessed as inhibition of DAMGO-induced beta-arrestin migration preincubated for 30 mins followed by agonist addition and measured after 3 hrs by PathHunter assay
Antagonist activity at GAL4-VP16-fused DOR (unknown origin) expressed in human U2OS cells assessed as inhibition of DAMGO-induced beta-arrestin migration preincubated for 30 mins followed by agonist addition and measured after 3 hrs by PathHunter assay
[PMID: 30707578]
U2OS IC50
6500 1
Compound: 58; CYM-53093, BTRX-335140
Antagonist activity at GAL4-VP16-fused DOR (unknown origin) expressed in human U2OS cells assessed as inhibition of DAMGO-induced beta-arrestin migration preincubated for 30 mins followed by agonist addition and measured after 3 hrs by PathHunter assay
Antagonist activity at GAL4-VP16-fused DOR (unknown origin) expressed in human U2OS cells assessed as inhibition of DAMGO-induced beta-arrestin migration preincubated for 30 mins followed by agonist addition and measured after 3 hrs by PathHunter assay
[PMID: 30707578]
U2OS IC50
0.8 1
Compound: 58; CYM-53093, BTRX-335140
Antagonist activity at GAL4-VP16-fused KOR (unknown origin) expressed in human U2OS cells co-expressing Tango-OPRK1-BLA assessed as inhibition of U-50488-induced beta-arrestin migration after 4 hrs by FRET assay
Antagonist activity at GAL4-VP16-fused KOR (unknown origin) expressed in human U2OS cells co-expressing Tango-OPRK1-BLA assessed as inhibition of U-50488-induced beta-arrestin migration after 4 hrs by FRET assay
[PMID: 30707578]
U2OS IC50
110 1
Compound: 58; CYM-53093, BTRX-335140
Antagonist activity at GAL4-VP16-fused MOR (unknown origin) expressed in human U2OS cells assessed as inhibition of DAMGO-induced beta-arrestin migration preincubated for 30 mins followed by agonist addition and measured after 3 hrs by PathHunter assay
Antagonist activity at GAL4-VP16-fused MOR (unknown origin) expressed in human U2OS cells assessed as inhibition of DAMGO-induced beta-arrestin migration preincubated for 30 mins followed by agonist addition and measured after 3 hrs by PathHunter assay
[PMID: 30707578]
U2OS IC50
6500 1
Compound: 58; CYM-53093, BTRX-335140
Antagonist activity at GAL4-VP16-fused DOR (unknown origin) expressed in human U2OS cells assessed as inhibition of DAMGO-induced beta-arrestin migration preincubated for 30 mins followed by agonist addition and measured after 3 hrs by PathHunter assay
Antagonist activity at GAL4-VP16-fused DOR (unknown origin) expressed in human U2OS cells assessed as inhibition of DAMGO-induced beta-arrestin migration preincubated for 30 mins followed by agonist addition and measured after 3 hrs by PathHunter assay
[PMID: 30707578]
体外実験

Navacaprant (BTRX-335140) (0-10 μM; 4 h) shows selective antagonist activity towards Kappa Opioid Receptor[1].

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

Navacaprant 関連抗体

Cell Viability Assay[1]

Cell Line: OPRK1-BLA U2OS cells
Concentration: 0-10 μM
Incubation Time: 4 hours
Result: Exibited antagonist activity to KOR, DOR and MOR with IC50 values of 0.8, 110 and 6500 nM respectively, and showed selective antagonist activity to KOR.
体内実験

Navacaprant (BTRX-335140) (0.01-3 mg/kg; p.o. once) reduces U69,593- stimulated plasma prolactin secretion to levels of without U69,593 treatment[1].
Navacaprant (BTRX-335140) (1 mg/kg; i.p. once) blocks U-50488-induced antinociception from hot water[1].
1.19 Pharmacokinetic Parameters of BTRX-335140 in rodents[1].

Rats
IV 1 mg/kg		 Mice
IV 3 mg/kg		 Rats
PO 5 mg/kg		 Mice
PO 10 mg/kg
CL (mL/min/kg) 105 66.5
t1/2 (h) 1.81 1.91 6.19 2.57
AUC0-t (h•ng/mL) 153 725 265 232
Vss (L/kg) 13.8 7.72
F (%) 30.2 12

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

Animal Model: Rat PRL model[1]
Dosage: 0.01, 0.03, 0.1, 0.3, 1 and 3 mg/kg
Administration: Oral gavage; 0.01-3 mg/kg once
Result: Effectively decreased the high level prolactin caused by U69,593 even at a dosage of 0.1 mg/kg.
Animal Model: Adult male ICR mice with tail dipped into 50°C hot water[1]
Dosage: 1 mg/kg
Administration: Intraperitoneal injection; 1 mg/kg once
Result: Blocked the U-50488-induced antinociception at 1 h but not at 24 h pretreatment time and showed a medication-like duration of action in blocking the KOR.
分子量

453.56

分子式

C25H32FN5O2
CAS 番号
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC1=NOC(C2=C(C)C3=CC(CC)=CC(F)=C3N=C2N4CCC(NC5CCOCC5)CC4)=N1
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 : 3.85 mg/mL (8.49 mM; ultrasonic and warming and adjust pH to 4 with HCl and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

1 M HCl : 3.33 mg/mL (7.34 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2048 mL 11.0239 mL 22.0477 mL
5 mM 0.4410 mL 2.2048 mL 4.4095 mL
10 mM --- --- ---
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    90% Corn Oil

    Solubility: ≥ 1.67 mg/mL (3.68 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 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 (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

  • Protocol 2

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1 mg/mL (2.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
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: 99.88%

COA (248 KB) HNMR (427 KB) LCMS (99 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
1 M HCl / DMSO 1 mM 2.2048 mL 11.0239 mL 22.0477 mL 55.1193 mL
5 mM 0.4410 mL 2.2048 mL 4.4095 mL 11.0239 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Navacaprant 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:

Navacaprant2244614-14-8BTRX-335140 CYM-53093BTRX335140BTRX 335140CYM53093CYM 53093CYM-53093Opioid ReceptororalCNSU69593neurobehavioral disorderU2OSInhibitorinhibitorinhibit

最近チェックした製品:

オンラインお問い合わせ

Your information is safe with us. * Required Fields.

製品名

  

カスタマ需要量 *

お名前 *

 

タイトル

メールアドレス *

 

電話番号 *

デパートメント

 

組纖名 *

市区町村

都道府県

国或いは地域 *

      

必ず会社名を記載ください。個人への返信は行いません。

備考

バルクお問い合わせ

Inquiry Information

製品名:
Navacaprant
製品番号:
HY-124754
数量:
MCE 日本正規代理店:

カスタマーレビュー

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

製品名

  

Lot #

お名前 *

 

メールアドレス *

電話番号 *

 

部門 *

組纖名 *

 

国或いは地域 *

備考

Request for HNMR Report

We have received your request and will respond to you as soon as possible.