2. GPCR/G Protein Neuronal Signaling
  3. Neurokinin Receptor
  4. Talnetant

Talnetant  (Synonyms: SB 223412)

製品番号: HY-14552 純度: 99.38%
COA 取扱説明書 Technical Support

Talnetant (SB 223412) is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant can be used in schizophrenia-related studies.

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Talnetant

Talnetant 構造式

CAS 番号 : 174636-32-9

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 114 在庫あり
Solution
10 mM * 1 mL in DMSO USD 114 在庫あり
Solid
5 mg $104 在庫あり
10 mg $162 在庫あり
25 mg $350 在庫あり
50 mg $677 在庫あり
100 mg $950 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

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カスタマーレビュー

Based on 3 publication(s) in Google Scholar

Other Forms of Talnetant:

Talnetant 関連抗体

Top Publications Citing Use of Products

Neurokinin 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
NK1R NK2R NK3R

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製品説明

Talnetant (SB 223412) is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant can be used in schizophrenia-related studies[1][2][3].

IC50 & Target

NK3R

 

Cellular Effect
Cell Line Type Value Description References
CHO IC50
2.4 nM
Compound: 1
Displacement of [125I]neurokinin B from cloned human NK3 receptor expressed in CHO cells
Displacement of [125I]neurokinin B from cloned human NK3 receptor expressed in CHO cells
[PMID: 16950620]
CHO IC50
8.4 nM
Compound: 1a
Displacement of [125I]His3-MePhe7)-NKB from human NK3R expressed in CHO cell membranes by topcounting method
Displacement of [125I]His3-MePhe7)-NKB from human NK3R expressed in CHO cell membranes by topcounting method
[PMID: 27298001]
HEK293 IC50
16.6 nM
Compound: SB-223412
Antagonist activity against human NK3 receptor expressed in HEK293 cells assessed as inhibition of NKB-induced increase of intracellular calcium level by fluorescent plate-reader analysis
Antagonist activity against human NK3 receptor expressed in HEK293 cells assessed as inhibition of NKB-induced increase of intracellular calcium level by fluorescent plate-reader analysis
[PMID: 21047106]
HEK293 IC50
6.1 nM
Compound: SB-223412
Antagonist activity against human NK3 receptor expressed in HEK293 cells assessed as inhibition of increase of intracellular calcium level by fluorescent plate-reader analysis
Antagonist activity against human NK3 receptor expressed in HEK293 cells assessed as inhibition of increase of intracellular calcium level by fluorescent plate-reader analysis
[PMID: 21047106]
体外実験

Talnetant (SB 223412) (0.1-1?μM) can reduce the accumulation of NKB-induced IP in U-2OS cells expressing the human NK3 receptor[3].

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

Talnetant 関連抗体
体内実験

Talnetant (SB 223412) (0.5-2 mg/kg i.v., 2 min pretreatment) can inhibit the miosis induced by senktide (25 μg, i.v.) in a dose-dependent manner with an ED50 of 0.44mg/kg in conscious rabbits[1].
Talnetant (SB 223412) (i.p., 1-100 mg/kg, 1 h) can significantly attenuate senktide-induced "wet dog wagging" behavior in a dose-dependent manner, significantly increase extracellular dopamine and norepinephrine in the medial prefrontal cortex and reduce haloperidol-induced increases in dopamine levels in the vomeronasal nucleus of freely moving guinea pigs[3].

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

Animal Model: Male Dunkin-Hartley guinea pig[3]
Dosage: 1, 3, 10, 30 or 100 mg/kg
Administration: Intraperitoneal injection; 1 h
Result: Showed a significant attenuation of wet dog shake (WDS) behavior from 31.1 to 16.7 at 30 mg/kg.
Significantly increased extracellular DA levels to 238% and NE levels to 227.1%, without affecting 5-HT levels.
分子量

382.45

分子式

C25H22N2O2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

OC1=C(C(N[C@H](C2=CC=CC=C2)CC)=O)C3=C(N=C1C4=CC=CC=C4)C=CC=C3
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 (261.47 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6147 mL 13.0736 mL 26.1472 mL
5 mM 0.5229 mL 2.6147 mL 5.2294 mL
10 mM 0.2615 mL 1.3074 mL 2.6147 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
×
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: ≥ 2.5 mg/mL (6.54 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.
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: 99.38%

COA (256 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, 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 2.6147 mL 13.0736 mL 26.1472 mL 65.3680 mL
5 mM 0.5229 mL 2.6147 mL 5.2294 mL 13.0736 mL
10 mM 0.2615 mL 1.3074 mL 2.6147 mL 6.5368 mL
15 mM 0.1743 mL 0.8716 mL 1.7431 mL 4.3579 mL
20 mM 0.1307 mL 0.6537 mL 1.3074 mL 3.2684 mL
25 mM 0.1046 mL 0.5229 mL 1.0459 mL 2.6147 mL
30 mM 0.0872 mL 0.4358 mL 0.8716 mL 2.1789 mL
40 mM 0.0654 mL 0.3268 mL 0.6537 mL 1.6342 mL
50 mM 0.0523 mL 0.2615 mL 0.5229 mL 1.3074 mL
60 mM 0.0436 mL 0.2179 mL 0.4358 mL 1.0895 mL
80 mM 0.0327 mL 0.1634 mL 0.3268 mL 0.8171 mL
100 mM 0.0261 mL 0.1307 mL 0.2615 mL 0.6537 mL
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Talnetant 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:

Talnetant174636-32-9SB 223412SB223412SB-223412Neurokinin ReceptorNK receptorTachykinin receptorNK3 receptorhNK-3-CHOhNK-2schizophreniaInhibitorinhibitorinhibit

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