Talnetant
Based on 3 publication(s) in Google Scholar
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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- Purity: 99.38%
- CAS No.: 174636-32-9
- 화학식: C25H22N2O2
- 분자량:382.45
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Talnetant
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Biological Activity
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NK3R |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
2.4 nM
Compound: 1
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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
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[PMID: 16950620] |
| CHO | IC50 |
8.4 nM
Compound: 1a
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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
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[PMID: 27298001] |
| HEK293 | IC50 |
16.6 nM
Compound: SB-223412
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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
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[PMID: 21047106] |
| HEK293 | IC50 |
6.1 nM
Compound: SB-223412
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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
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[PMID: 21047106] |
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.
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Animal Model:Male Dunkin-Hartley guinea pig[3]
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Dosage:1, 3, 10, 30 or 100 mg/kg
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Administration:Intraperitoneal injection; 1 h
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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.
Chemical Information
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CAS No. 174636-32-9
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Appearance Solid
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분자량 382.45
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화학식 C25H22N2O2
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Color White to off-white
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SMILES
OC1=C(C(N[C@H](C2=CC=CC=C2)CC)=O)C3=C(N=C1C4=CC=CC=C4)C=CC=C3
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Synonyms
SB 223412
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
용액&용해도
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (281 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Handling Instructions (2659 KB)
References
[1]. Giardina GA, et al. Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 2. Identification of (S)-N-(1-phenylpropyl)-3-hydroxy-2-phenylquinoline-4-carboxamide (SB 223412). J Med Chem. 1999 Mar 25;42(6):1053-65. [Content Brief]
[2]. Houghton LA, et al. Effect of the NK(3) receptor antagonist, talnetant, on rectal sensory function and compliance in healthy humans. Neurogastroenterol Motil. 2007 Sep;19(9):732-43. [Content Brief]
[3]. Dawson LA, et al. In vitro and in vivo characterization of the non-peptide NK3 receptor antagonist SB-223412 (talnetant): potential therapeutic utility in the treatment of schizophrenia. Neuropsychopharmacology. 2008 Jun;33(7):1642-52. [Content Brief]
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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