2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein
  3. GlyT 5-HT Receptor P2X Receptor
  4. Opiranserin hydrochloride

Opiranserin hydrochloride  (Synonyms: VVZ-149 hydrochloride)

製品番号: HY-109067A 純度: 99.62%
COA 取扱説明書 Technical Support

Opiranserin (VVZ-149) hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin hydrochloride shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain.

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Opiranserin hydrochloride

Opiranserin hydrochloride 構造式

CAS 番号 : 1440796-75-7

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 319 在庫あり
Solution
10 mM * 1 mL in DMSO USD 319 在庫あり
Solid
5 mg $290 在庫あり
10 mg $460 在庫あり
25 mg $830 在庫あり
50 mg $1180 在庫あり
100 mg $1650 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Opiranserin hydrochloride 関連抗体

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製品説明

Opiranserin (VVZ-149) hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin hydrochloride shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain[1][2][3].

IC50 & Target[2]

P2X3 Receptor

 

5-HT2A Receptor

 

GlyT2

0.86 μM (IC50)

rP2X3

0.87 μM (IC50)

5-HT2A Receptor

1.3 μM (IC50)

体内実験

Opiranserin hydrochloride (25 mg/kg, s.c.) effectively reduced mechanical allodynia and pain-related behaviors with efficacy comparable to 3 mg/kg Morphine[3].
Opiranserin hydrochloride (80 mg/kg, p.o.) reduced mechanical allodynia in a rat spinal nerve ligation model[4].

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

430.97

分子式

C21H35ClN2O5
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC(OC)=C(OCCCC)C(OC)=C1)NCC2(CCOCC2)N(C)C.[H]Cl
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
体外: 

DMSO : 50 mg/mL (116.02 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 2.3203 mL 11.6017 mL 23.2035 mL
5 mM 0.4641 mL 2.3203 mL 4.6407 mL
10 mM 0.2320 mL 1.1602 mL 2.3203 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 (sealed storage, away from moisture). 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
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Concentration
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Volume
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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: ≥ 2.5 mg/mL (5.80 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 (5.80 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

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(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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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
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 (sealed storage, away from moisture). 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 2.3203 mL 11.6017 mL 23.2035 mL 58.0087 mL
5 mM 0.4641 mL 2.3203 mL 4.6407 mL 11.6017 mL
10 mM 0.2320 mL 1.1602 mL 2.3203 mL 5.8009 mL
15 mM 0.1547 mL 0.7734 mL 1.5469 mL 3.8672 mL
20 mM 0.1160 mL 0.5801 mL 1.1602 mL 2.9004 mL
25 mM 0.0928 mL 0.4641 mL 0.9281 mL 2.3203 mL
30 mM 0.0773 mL 0.3867 mL 0.7734 mL 1.9336 mL
40 mM 0.0580 mL 0.2900 mL 0.5801 mL 1.4502 mL
50 mM 0.0464 mL 0.2320 mL 0.4641 mL 1.1602 mL
60 mM 0.0387 mL 0.1934 mL 0.3867 mL 0.9668 mL
80 mM 0.0290 mL 0.1450 mL 0.2900 mL 0.7251 mL
100 mM 0.0232 mL 0.1160 mL 0.2320 mL 0.5801 mL
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Opiranserin hydrochloride 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:

Opiranserin1440796-75-7VVZ-149VVZ149VVZ 149GlyT5-HT ReceptorP2X ReceptorGlycine transportersSerotonin Receptor5-hydroxytryptamine ReceptorP2XRspainanalgesicnon-opioidnon-non-steroidalanti-inflammatorypostoperativeInhibitorinhibitorinhibit

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